Linsitinib (OSI-906)

Linsitinib (OSI-906)は一種の選択性的なIGF-1R阻害剤で、無細胞実験で、IC50値が35 nMです。OSI-906 (Linsitinib)はInsRを適合に抑制して、このIC50値が75 nMになリますが、Abl、ALK、BTK、EGFR、FGFR1/2とPKA等に抑制活性を表しません。臨床3期。

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Linsitinib (OSI-906) 化学構造
分子量: 421.49

高品質保証

カスタマーフィードバック(3)

MSDS

製品説明

  • Compare IGF-1R Inhibitors
    IGF-1R製品生物活性の比較
  • 研究分野

製品の説明

生物活性

製品説明 Linsitinib (OSI-906)は一種の選択性的なIGF-1R阻害剤で、無細胞実験で、IC50値が35 nMです。OSI-906 (Linsitinib)はInsRを適合に抑制して、このIC50値が75 nMになリますが、Abl、ALK、BTK、EGFR、FGFR1/2とPKA等に抑制活性を表しません。臨床3期。
ターゲット IGF-1R InsR
IC50 35 nM 75 nM [1]
In vitro試験 OSI-906 inhibits IGF-1R autophosphorylation and activation of the downstream signaling proteins Akt, ERK1/2 and S6 kinase with IC50 of 0.028 to 0.13 μM. OSI-906 enables an intermediate conformation of the target protein through interactions with the C-helix. OSI-906 displays favorable metabolic stability in liver microsomes. OSI-906 fully inhibits both IR and IGF-1R phosphorylation at a concentration of 1 μM. OSI-906 inhibits proliferation of several tumor cell lines including non-small-cell lung cancer and colorectal cancer (CRC) tumor cell line with EC50 of 0.021 to 0.810 μM. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
A4-Fuk MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDkVIkyUUN3ME2wMlAzQDB4IN88US=> MX\TRW5ITVJ?
KS-1 NWTSTlFtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVXJR|UxRTBwMEO4N|Uh|ryP M1vFeHNCVkeHUh?=
TE-11 M3PvUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHvJcnJKSzVyPUCuNFc5OjJizszN NHnXcIpUSU6JRWK=
EW-1 NWnZO2o3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;mSXhIUUN3ME2wMlA5PTh3IN88US=> MlLWV2FPT0WU
HMV-II NWP2Z3NvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV64dGc2UUN3ME2wMlA5QDR4IN88US=> M2WwSHNCVkeHUh?=
COLO-205 NWXxZWpmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlPZTWM2OD1yLkGwOFU1KM7:TR?= M2DS[3NCVkeHUh?=
ES1 NV;RW45ST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHlTWM2OD1yLkGwOlk3KM7:TR?= MofKV2FPT0WU
GDM-1 Ml2xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYS2UFJ3UUN3ME2wMlE{Pjd{IN88US=> MVfTRW5ITVJ?
ML-2 NFrYNGdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnX0TWM2OD1yLkG1PFk3KM7:TR?= Ml\RV2FPT0WU
Saos-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\GR2N5UUN3ME2wMlE3PTJ4IN88US=> NHG0bWxUSU6JRWK=
NCI-H1355 M4XjSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnUN|hKSzVyPUCuNVgyOzVizszN NWe1ZphDW0GQR1XS
G-401 NYmyXZFIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XvOWlEPTB;MD6xPFI{KM7:TR?= MmHXV2FPT0WU
EW-16 M2PxbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnkXG9PUUN3ME2wMlE5Pzd5IN88US=> M3HtNHNCVkeHUh?=
EW-7 NH\2WZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DwTGlEPTB;MD6xPFg5OSEQvF2= NYn0T2J3W0GQR1XS
NCI-H727 NEe4OHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF23fHFKSzVyPUCuNVk4QTRizszN M3XLcnNCVkeHUh?=
LCLC-97TM1 M4TsRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvwO3h{UUN3ME2wMlIxQTV3IN88US=> NFHpVZdUSU6JRWK=
NCI-H650 NY\sT3ZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUPJR|UxRTBwMkGzPFQh|ryP NX7UcXVHW0GQR1XS
NCI-H2122 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULXbGlbUUN3ME2wMlI{Ojl7IN88US=> NVuxeopxW0GQR1XS
SK-N-DZ M4fyUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\QRWlEPTB;MD6yN|Y6QCEQvF2= MojSV2FPT0WU
HT-29 MnTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTBwMkSyOFgh|ryP M4\aNXNCVkeHUh?=
LB771-HNC MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnjLTWM2OD1yLkK1PVE2KM7:TR?= MormV2FPT0WU
HT-144 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M17PUmlEPTB;MD6yOlE6OSEQvF2= M2LUS3NCVkeHUh?=
LAN-6 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LpVmlEPTB;MD6yOlM1QCEQvF2= MYDTRW5ITVJ?
EW-18 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTBwMkewNFEh|ryP MUPTRW5ITVJ?
LS-1034 M331W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFS1V4JKSzVyPUCuNlcyOzJizszN NYTpUHVyW0GQR1XS
EW-11 NWLOdWdPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwMki0N|Ih|ryP M4XmWHNCVkeHUh?=
SNU-C1 NHfnXVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3naNmlEPTB;MD6yPVMyOyEQvF2= NEm5UZZUSU6JRWK=
RS4-11 NH\LT|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojNTWM2OD1yLkOzO|U5KM7:TR?= NFj1dXdUSU6JRWK=
ES4 MnnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE[zUWZKSzVyPUCuOFExOzhizszN NUDFfZhnW0GQR1XS
COLO-320-HSR NXfYVIRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYfJR|UxRTBwNEGzOlgh|ryP M3nvfXNCVkeHUh?=
NB10 NYjzVmI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;JTWM2OD1yLkS1OFM4KM7:TR?= NU\zRoZPW0GQR1XS
BFTC-905 MmfsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkTrTWM2OD1yLkS2O|U5KM7:TR?= MX;TRW5ITVJ?
A375 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTBwNEe2NVch|ryP NUnIV3ZrW0GQR1XS
SJRH30 NXnMOZBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnHYTWM2OD1yLkWwPFIzKM7:TR?= M3XSPHNCVkeHUh?=
NOS-1 NYjremJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRTBwNUKyOlch|ryP NGHV[otUSU6JRWK=
SIG-M5 NIPx[FdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnZcoVKSzVyPUCuOVM2PTdizszN NG\4[m9USU6JRWK=
DOK M124e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXHU|RKSzVyPUCuOVU3KM7:TR?= NEjqSIhUSU6JRWK=
NB69 NFrHXWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFjITmNKSzVyPUCuOVgzPTdizszN M{fwdXNCVkeHUh?=
SK-NEP-1 NXewfFdjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWj3blRQUUN3ME2wMlYxOjN4IN88US=> Mm\uV2FPT0WU
SK-MM-2 NWPwOIRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXu1eFJNUUN3ME2wMlY2PDlzIN88US=> NUTu[JJlW0GQR1XS
NCI-H358 NWn5NFlXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvzOXlKSzVyPUCuOlcxQDJizszN NGrDXnhUSU6JRWK=
RH-1 NYDFXmZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\0TWM2OD1yLke0PFU6KM7:TR?= MUPTRW5ITVJ?
NH-12 M4DEdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fIdmlEPTB;MD63OlA1PiEQvF2= M1fvW3NCVkeHUh?=
TE-12 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MofRTWM2OD1yLke2OFg3KM7:TR?= NFm2bnhUSU6JRWK=
COLO-668 M1n4e2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWnJR|UxRTBwOES2OlYh|ryP MUDTRW5ITVJ?
PANC-08-13 NEfKTVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTBwOE[zO|ch|ryP NXe5U4tRW0GQR1XS
HCC2998 MmHOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFzZOZRKSzVyPUCuPFgzPjNizszN NGXpVo9USU6JRWK=
ABC-1 M3Sy[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVLrflJGUUN3ME2wMlkxOzV{IN88US=> MUPTRW5ITVJ?
ES6 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGHId3hKSzVyPUCuPVExPjZizszN M37MfHNCVkeHUh?=
SNU-387 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIK5[ZNKSzVyPUCuPVk{QTNizszN NGPyTnRUSU6JRWK=
CMK M1;RfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWD0elRQUUN3ME2wMlk6QTJ7IN88US=> MkfVV2FPT0WU
SJSA-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHm1T3NKSzVyPUGuNFM3PTNizszN NYDtPFFvW0GQR1XS
SIMA MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonpTWM2OD1zLkC2PFI2KM7:TR?= NVzwPJNrW0GQR1XS
ES3 M3SwXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVr3ZmtmUUN3ME2xMlEzOjl5IN88US=> MW\TRW5ITVJ?
IGROV-1 MlTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTOSnY2UUN3ME2xMlE2PDR2IN88US=> M3nYdHNCVkeHUh?=
MEL-JUSO NIroZW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTFwMUW3OVkh|ryP MUfTRW5ITVJ?
T84 M{LRXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoLtTWM2OD1zLkKwPVE1KM7:TR?= M2XHbXNCVkeHUh?=
CAL-85-1 MkHCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlTQTWM2OD1zLkKzNVM5KM7:TR?= M{P1OHNCVkeHUh?=
RD NGjqO5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXDenlKSzVyPUGuNlY1PTVizszN NVi0S|VWW0GQR1XS
TE-8 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFO0dXVKSzVyPUGuN|E1PjJizszN M1PjSHNCVkeHUh?=
L-363 M4\IN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mnm4TWM2OD1zLkO0NlA5KM7:TR?= M4jvcHNCVkeHUh?=
EKVX Mn23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoTiTWM2OD1zLkO0OVY5KM7:TR?= Ml\SV2FPT0WU
SK-MEL-3 NIrk[GZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkfzTWM2OD1zLkS4OVU3KM7:TR?= MYDTRW5ITVJ?
TGBC24TKB MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHxN3AyUUN3ME2xMlUxOTl|IN88US=> MnvZV2FPT0WU
NCI-H1770 MknHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml22TWM2OD1zLkWxNVE{KM7:TR?= MnK5V2FPT0WU
HuH-7 M2jpVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2T3emlEPTB;MT62NFA6QCEQvF2= MnPxV2FPT0WU
HL-60 MnzoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwNk[5Nlgh|ryP MmDYV2FPT0WU
TE-1 M{\JTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTFwN{C5OFUh|ryP M1T1bHNCVkeHUh?=
LC-2-ad M3\Ub2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFwN{O4PFch|ryP NVX1eYZRW0GQR1XS
LB647-SCLC NFG0N|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTFwN{[1PFMh|ryP NHWxdFZUSU6JRWK=
NCI-H2171 NF:wc2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTFwN{e3NVYh|ryP NWHZZlBsW0GQR1XS
SK-PN-DW Ml3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTFwOUGyPVgh|ryP NGnJeYNUSU6JRWK=
MC-IXC NYn3ZlB7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV3JR|UxRTFwOUi5PEDPxE1? M{DxdXNCVkeHUh?=
LS-513 MlnPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33LSWlEPTB;Mj6wOVMxPSEQvF2= MmnCV2FPT0WU
EW-3 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3rpR2lEPTB;Mj6wPVg1PCEQvF2= NHnjbHdUSU6JRWK=
OPM-2 MkT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTJwMUCyJO69VQ>? M3nTdnNCVkeHUh?=
LP-1 Ml7VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXHJR|UxRTJwMkW4NFch|ryP NXHG[GY6W0GQR1XS
LU-134-A M3XHTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEj2PIxKSzVyPUKuNlc4KM7:TR?= M37rXXNCVkeHUh?=
CP66-MEL MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7jTWM2OD1{LkK5NFE1KM7:TR?= MlfFV2FPT0WU
HCC1143 M4fTXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmfPTWM2OD1{LkS1N|Y5KM7:TR?= MUHTRW5ITVJ?
LOXIMVI NX7Md2JkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYrJR|UxRTJwNkCyNUDPxE1? MoT4V2FPT0WU
TE-10 NHnYfmNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofCTWM2OD1{LkewPFM5KM7:TR?= MWLTRW5ITVJ?
NCI-H1882 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3ZNINoUUN3ME2yMlc2OjJ5IN88US=> MoHBV2FPT0WU
CHP-126 MmnrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTJwN{[zNVch|ryP MmjYV2FPT0WU
NCI-H1623 NIH0VllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrvdoxKSzVyPUKuPVIxOjRizszN MnnGV2FPT0WU
GB-1 M4D5WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\ETWM2OD1{LkmzOFA1KM7:TR?= MYjTRW5ITVJ?
RCC10RGB MoLrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHyRZM6UUN3ME2yMlk2OjhzIN88US=> M1XuNXNCVkeHUh?=
NCI-H2141 NV3iUnZRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV22c2NvUUN3ME2yMlk3QDl4IN88US=> MlfKV2FPT0WU
GI-ME-N MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHWxNHhKSzVyPUOuNFA2PjVizszN Ml\iV2FPT0WU
NCI-H526 Mn\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXFTWM2OD1|LkC0NFg2KM7:TR?= MVjTRW5ITVJ?
NCI-H747 M4rsWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4jSdmlEPTB;Mz6wOFk6OiEQvF2= M2q5N3NCVkeHUh?=
SNU-423 M33MSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NILVbWxKSzVyPUOuNlA{OTNizszN MoDtV2FPT0WU
A427 NHO3UVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H2TGlEPTB;Mz6yOVY6QSEQvF2= NV\iZ4NNW0GQR1XS
CAL-12T NVfSNo15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\GPG9KSzVyPUOuOFA4OTNizszN MlSzV2FPT0WU
LU-99A M{[4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHtW|JKSzVyPUOuOFcyODVizszN NXy1TWo4W0GQR1XS
MS-1 NFv1eItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmrXTWM2OD1|LkWzOFI6KM7:TR?= MX;TRW5ITVJ?
SK-LU-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkXZTWM2OD1|Lke2Nlk2KM7:TR?= M32wPHNCVkeHUh?=
SW837 M{T1T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTNwN{[zN|Mh|ryP NEK0UG1USU6JRWK=
ES8 NV3INYkyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTNwOEO4O|ch|ryP M{iwfHNCVkeHUh?=
MZ2-MEL Mmj2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NESw[mhKSzVyPUOuPVIxQDZizszN MmS3V2FPT0WU
TGW MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;TSXpmUUN3ME20MlAyOzFzIN88US=> M2[1WHNCVkeHUh?=
GP5d M1;JU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHT[YtKSzVyPUSuNFU{PjJizszN M1fWbXNCVkeHUh?=
BB49-HNC MoXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUPkVYpMUUN3ME20MlE2OjF|IN88US=> MnvJV2FPT0WU
NB13 NHzMb2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLWTWM2OD12LkK2PFg4KM7:TR?= NHq2VYRUSU6JRWK=
NTERA-S-cl-D1 Mn62S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEfrXnNKSzVyPUSuNlg3OTVizszN NVSxS405W0GQR1XS
NCI-H1648 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTRwMkm4NVkh|ryP MVzTRW5ITVJ?
LCLC-103H MnToS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGPqZ2ZKSzVyPUSuN|IyQTVizszN MX\TRW5ITVJ?
LS-411N NUT6UHU{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LSZmlEPTB;ND60OFg5PSEQvF2= MlLLV2FPT0WU
NCI-H1092 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHz2OHBKSzVyPUSuOFU3QDdizszN MYrTRW5ITVJ?
PANC-10-05 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\6PWwyUUN3ME20MlY6QDRizszN M2\icXNCVkeHUh?=
DK-MG MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1Tzd2lEPTB;ND64NFk{OyEQvF2= MlnZV2FPT0WU
OVCAR-5 M4O2SWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYK5foRFUUN3ME20MlgyOjJ4IN88US=> MW\TRW5ITVJ?
CAL-39 NX\RO2JTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVPJR|UxRTRwOEe2O{DPxE1? M4LOVnNCVkeHUh?=
TE-441-T MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjaTWM2OD12LkmwOVM4KM7:TR?= NHWycYRUSU6JRWK=
MOLT-16 M2qwPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;nVJJKSzVyPUSuPVUzPTNizszN MYHTRW5ITVJ?
MCF7 M3rnNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXnW5FKSzVyPUWuNVQ2OTdizszN NUPFOYtjW0GQR1XS
CAPAN-1 M{PmcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3HBfGlEPTB;NT6yOVcxPyEQvF2= NVfpTJRjW0GQR1XS
PSN1 NEn3UphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzZVnkxUUN3ME21MlI4OjN3IN88US=> MW\TRW5ITVJ?
NCI-H292 M2rRPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTVwM{CwOFQh|ryP M3exbHNCVkeHUh?=
CPC-N NVPlS49rT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXWfWhlUUN3ME21MlM6PDF7IN88US=> NH3OUmhUSU6JRWK=
DoTc2-4510 M4K4Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvETWM2OD13LkS1N|cyKM7:TR?= NEn4O3dUSU6JRWK=
LB1047-RCC NEnUWVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTVwNUW5N|Mh|ryP NYX2TG5pW0GQR1XS
MHH-ES-1 M4Xre2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTVwNUm5NFch|ryP NXLsflc2W0GQR1XS
NMC-G1 NH;mfoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYrJR|UxRTVwN{CyNlch|ryP MWjTRW5ITVJ?
SW1710 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXq4ZYg{UUN3ME21Mlc1PzVzIN88US=> MVnTRW5ITVJ?
YAPC M3\v[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlT3TWM2OD13Lke2NlAyKM7:TR?= NIjRRYFUSU6JRWK=
22RV1 M4qzWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmS4TWM2OD13LkiwNFE6KM7:TR?= MXvTRW5ITVJ?
COLO-679 NF;XXo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\ibWlEPTB;NT64PFk1QCEQvF2= MlTvV2FPT0WU
TCCSUP MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDJU2k5UUN3ME21Mlk{OjV7IN88US=> MYDTRW5ITVJ?
C2BBe1 NF:zS5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vwRWlEPTB;NT65N|k4KM7:TR?= MWHTRW5ITVJ?
TE-15 NHnKXmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDVT44xUUN3ME22MlA3PjB3IN88US=> MoLZV2FPT0WU
SCLC-21H MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVnqU2ttUUN3ME22MlExQDR|IN88US=> M4C2XHNCVkeHUh?=
EoL-1-cell NVLOU4NTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NV3hTYk4UUN3ME22MlE3PTZ|IN88US=> MnfOV2FPT0WU
NKM-1 M2OzcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYTJR|UxRTZwMU[3NUDPxE1? NEX6N3FUSU6JRWK=
NCI-H1304 NH35[mpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTZwMke0Nlgh|ryP M{m2eXNCVkeHUh?=
NB6 NYrvWmltT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4ezPWlEPTB;Nj6yPVYzOiEQvF2= MkjqV2FPT0WU
NALM-6 NYXkcnV5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTZwM{OyN{DPxE1? M3roO3NCVkeHUh?=
NCI-H522 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHSwS|FKSzVyPU[uN|M{ODZizszN NXnYcWk6W0GQR1XS
MV-4-11 M37RfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3O4T2lEPTB;Nj6zO|A4QSEQvF2= MVXTRW5ITVJ?
LB2241-RCC NW\xdJRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUXJR|UxRTZwM{i2Olch|ryP MljCV2FPT0WU
NCI-H1417 M3rMOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7XNpZKSzVyPU[uOFA5PDdizszN MXrTRW5ITVJ?
HT-1197 MnT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVHJbGx1UUN3ME22MlU4OTJ{IN88US=> NVnqPIFKW0GQR1XS
P30-OHK MlLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF;DU2xKSzVyPU[uOlI4PyEQvF2= MoTRV2FPT0WU
ALL-PO M1XRSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoGxTWM2OD14LkexPVE3KM7:TR?= NV;wc5A1W0GQR1XS
OVCAR-4 NFfPSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\DOFVKSzVyPU[uO|U1ODVizszN NHXufHlUSU6JRWK=
HCC2157 MmDJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIG0O|RKSzVyPU[uO|c1PzVizszN Mmf0V2FPT0WU
NCI-H838 NU[3eFZ5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTZwOU[0PUDPxE1? M{XQXHNCVkeHUh?=
NCI-H1299 MoH0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{nVR2lEPTB;Nj65O|A6KM7:TR?= NULNbGFyW0GQR1XS
SW954 Ml30S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3rUHhCUUN3ME23MlIxODZ6IN88US=> NY\GdG9mW0GQR1XS
NCI-H441 M3TxTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEfwPXFKSzVyPUeuN|QxPjVizszN NE\2O4ZUSU6JRWK=
SK-MEL-2 M{W4RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1G2UWlEPTB;Nz60PFM4OyEQvF2= M3H2RnNCVkeHUh?=
KARPAS-45 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnSyTWM2OD15Lk[1PVI6KM7:TR?= NIrFPHlUSU6JRWK=
CAL-54 M1HPXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFX6RpdKSzVyPUeuPFI6PzdizszN NHL4[FFUSU6JRWK=
KYSE-180 MlL3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF3sUXFKSzVyPUeuPFg6PDFizszN NWH5[HlPW0GQR1XS
NCI-H187 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\2TWM2OD15Lkm1PVQ4KM7:TR?= NILPTYJUSU6JRWK=
RT-112 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoGwTWM2OD16LkC5Olc4KM7:TR?= M{\5Z3NCVkeHUh?=
NCI-H1437 NXTKbXNNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRThwMEm3PVUh|ryP Mkn0V2FPT0WU
SNU-449 M{DVTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3T[5piUUN3ME24MlI5Ojd{IN88US=> MWTTRW5ITVJ?
HCC1187 NGDVXYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFO0fldKSzVyPUiuNlk{QTFizszN MYrTRW5ITVJ?
NCI-H2030 Mom3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnnRTWM2OD16LkO3O|E1KM7:TR?= NFXi[|NUSU6JRWK=
HuO-3N1 M4nFdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkCwTWM2OD16LkO3PFQ1KM7:TR?= MWPTRW5ITVJ?
COLO-792 M{jIO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nlWmlEPTB;OD60NVUzPyEQvF2= NUnYUo1iW0GQR1XS
MIA-PaCa-2 NE\yR4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXNZ5RKSzVyPUiuPFU2ODhizszN NHrzVYlUSU6JRWK=
SK-N-FI MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFfvdIRKSzVyPUmuNFQzPSEQvF2= MlnsV2FPT0WU
MMAC-SF NWH1SmE5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXlTWM2OD17LkC5O|UyKM7:TR?= M{L2UHNCVkeHUh?=
NCI-H28 NGPxcHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTlwMUC0Olkh|ryP M2fs[HNCVkeHUh?=
ETK-1 Mn3JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7VTItuUUN3ME25MlI6QTd2IN88US=> M13rTXNCVkeHUh?=
NCI-H1993 M1\nemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGW5b41KSzVyPUmuOFQzPjFizszN MlywV2FPT0WU
no-11 NHq0[2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzXTnJKSzVyPUmuOFcyOiEQvF2= MnT4V2FPT0WU
ChaGo-K-1 NVnDcFhqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfTNVlKSzVyPUmuOVE2QDNizszN NFzxdWZUSU6JRWK=
NCCIT MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XiVWlEPTB;OT61N|E3QSEQvF2= NEXL[nVUSU6JRWK=
SAS NH\SNY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7MW4FbUUN3ME2xNE4zPDhizszN MlKwV2FPT0WU
A673 NIizXI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYXNbWxqUUN3ME2xNE4{PzB2IN88US=> MUTTRW5ITVJ?
NCI-H1522 M1u4dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\Bc|NIUUN3ME2xNE4{PzB5IN88US=> NYnWdm5tW0GQR1XS
NCI-H810 NXqwT2dVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2XXbmlEPTB;MUCuN|kxPyEQvF2= NVf5OmNGW0GQR1XS
IST-MES1 NInPO41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEDwSlNKSzVyPUGwMlQ2PjRizszN NYPtUJVsW0GQR1XS
GR-ST M4rSTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M33rfWlEPTB;MUCuOVAzPCEQvF2= NIL4eJhUSU6JRWK=
SUP-T1 NUXwb4xWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIq4RpJKSzVyPUGwMlc{OTdizszN M3zlRnNCVkeHUh?=
NB5 NF\hT49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYLJR|UxRTFyLkmwNlIh|ryP NGnDNXdUSU6JRWK=
MZ1-PC NIXMSVdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWL5WZh5UUN3ME2xNE46PTdzIN88US=> MYnTRW5ITVJ?
SK-CO-1 NUPvfoplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYr1XmtMUUN3ME2xNE46QTNzIN88US=> M3raVXNCVkeHUh?=
Capan-2 NEXJfppIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX2y[nFLUUN3ME2xNU4{OTl6IN88US=> NHXjbWhUSU6JRWK=
697 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTFzLk[3OVch|ryP M{nQWXNCVkeHUh?=
REH NV\wSGViT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHDTWM2OD1zMT63OFUyKM7:TR?= MWLTRW5ITVJ?
GI-1 NGDQS29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXH3SJZRUUN3ME2xNU45PjF3IN88US=> M1nBeXNCVkeHUh?=
BB65-RCC NGj2Vo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MULJR|UxRTF{LkC5NVYh|ryP NVm1dFRZW0GQR1XS
NCI-H1651 NWC2VVBTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYXJR|UxRTF{LkK0O|gh|ryP M{f4ZnNCVkeHUh?=
NCI-H1618 NGnZVlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF{LkO5O|Yh|ryP Mne3V2FPT0WU
NCI-H2081 NF\Jc4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33oRWlEPTB;MUKuOlE1OSEQvF2= NWjXRmpUW0GQR1XS
GCIY NEnPTWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MojkTWM2OD1zMj63NlE{KM7:TR?= NILCUopUSU6JRWK=
NY NULNW3AzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrUeINYUUN3ME2xN{4xPjR|IN88US=> M4CxUnNCVkeHUh?=
PANC-03-27 NUXBUWZ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVrJR|UxRTF|LkC4NFch|ryP MVTTRW5ITVJ?
BHY MoXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH2wZmxKSzVyPUGzMlIyOjFizszN NIrt[pFUSU6JRWK=
SK-OV-3 NWDWdIRHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILNd2lKSzVyPUGzMlM4PjNizszN MlHNV2FPT0WU
5637 NE\h[GlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3e4eWlEPTB;MUOuO|c2QSEQvF2= Mme1V2FPT0WU
LC-1F M2nPNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDoXJdKSzVyPUG0MlA{PTZizszN NV\lOHFWW0GQR1XS
SNB75 NVfqbIZpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEO5VIhKSzVyPUG0MlA{QDNizszN MlryV2FPT0WU
CHP-212 M{O4[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWDJR|UxRTF2LkC0OlQh|ryP Mn3nV2FPT0WU
HT-1376 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\wb2lEPTB;MUSuNVEzPiEQvF2= NX\CeWRzW0GQR1XS
MONO-MAC-6 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4rCfGlEPTB;MUSuNVUxOiEQvF2= NVvDd4lkW0GQR1XS
CA46 M3;peGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlj6TWM2OD1zND6xPFI4KM7:TR?= NFHIfXZUSU6JRWK=
SCC-15 NEPrUIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVu0[ZEzUUN3ME2xOE42PTh|IN88US=> MVvTRW5ITVJ?
ATN-1 NUjoV5N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnGTWM2OD1zND62OlI4KM7:TR?= NVr5N2hyW0GQR1XS
NCI-H2405 NG\oSpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nOZ2lEPTB;MUSuPFE2PyEQvF2= NXvWclRWW0GQR1XS
NCI-H716 M1j4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzKfINKSzVyPUG0Mlg1QTNizszN MmP6V2FPT0WU
SW620 NFTCWo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MofGTWM2OD1zND65NFE1KM7:TR?= M3G3cXNCVkeHUh?=
NCI-H226 NFnrbZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlzMTWM2OD1zND65NFg2KM7:TR?= MWHTRW5ITVJ?
SW962 NIPUXXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1XSSGlEPTB;MUSuPVQ{OiEQvF2= MXrTRW5ITVJ?
KYSE-150 M2jxU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPiTWM2OD1zND65OVUh|ryP NEToSJVUSU6JRWK=
OCUB-M Mk\1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P5VWlEPTB;MUSuPVg5OyEQvF2= MVPTRW5ITVJ?
ES7 MnvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXrJR|UxRTF3LkC5PFQh|ryP M4jRbHNCVkeHUh?=
SW1463 MlXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrQXlVKSzVyPUG1MlQzOjNizszN MVTTRW5ITVJ?
CAKI-1 M{PkSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIqxdYdKSzVyPUG1MlU{PDZizszN NGLONZlUSU6JRWK=
MKN28 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVyzPWZ5UUN3ME2xOU42PDd7IN88US=> NEG2bFJUSU6JRWK=
SW13 NV7nPXZVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWnmTot2UUN3ME2xOU43OThizszN NVfZVpdUW0GQR1XS
A3-KAW M4jiV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHGzUoNKSzVyPUG1Mlk3QTdizszN NXf1S|ZvW0GQR1XS
LU-65 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjYWYN4UUN3ME2xOU46PzZ6IN88US=> MWnTRW5ITVJ?
Calu-1 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYjJR|UxRTF4LkCzOlgh|ryP NXHPUlZNW0GQR1XS
ST486 NED3WWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjYTWM2OD1zNj6wOFMyKM7:TR?= NHzhSm9USU6JRWK=
BB30-HNC NEHPZnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHLiUWRKSzVyPUG2MlEzPDZizszN NVW1VWp2W0GQR1XS
EGI-1 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPGTWM2OD1zNj60OFYh|ryP MUnTRW5ITVJ?
SH-4 Mk\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUnJR|UxRTF4LkS3N|Eh|ryP Mnm4V2FPT0WU
MN-60 Ml;nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHJ[JBKSzVyPUG3MlIzQTdizszN NVzSUpRZW0GQR1XS
MPP-89 M2HUZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWm5TGJ5UUN3ME2xO{4zPDV7IN88US=> MnnFV2FPT0WU
A2780 NXLnd2Y4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHFPItKSzVyPUG3MlQyOzlizszN M4HGR3NCVkeHUh?=
Daoy M{HRdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\nOmVxUUN3ME2xO{41Pjl3IN88US=> NGT5eFJUSU6JRWK=
NCI-H2126 NXn5c4VbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\JdJVKSzVyPUG3MlQ4PzFizszN M4fDbnNCVkeHUh?=
NCI-H1563 NYq1R2VsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPWdpBSUUN3ME2xO{41QTF5IN88US=> MX3TRW5ITVJ?
8-MG-BA MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTF5Lk[2OFgh|ryP M{ny[3NCVkeHUh?=
786-0 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\OcmlEPTB;MUeuPFM2OyEQvF2= NWf4ZmNTW0GQR1XS
AM-38 M{LoW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVG3XGlMUUN3ME2xO{46OzB4IN88US=> Mor2V2FPT0WU
COLO-824 NUfwOVh5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PxfmlEPTB;MUiuOFQ{PiEQvF2= NYH5PVRsW0GQR1XS
SK-MEL-30 M{DQemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTF6LkWwPFIh|ryP NXHTNXJQW0GQR1XS
CESS NITESJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\6blRKSzVyPUG4Mlc3ODlizszN NWLlTohSW0GQR1XS
BL-70 NWHMUJJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjSfGpKSzVyPUG4MlgyPTZizszN Mk\IV2FPT0WU
NCI-H2170 NGnKdG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTF6LkmxO|kh|ryP NVnETo1[W0GQR1XS
HT-3 MnrVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTF6Lkm4N{DPxE1? MnrkV2FPT0WU
BOKU MnLKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYm2eVFlUUN3ME2xPU4xOzhzIN88US=> NHrXdW9USU6JRWK=
HPAF-II M2OxNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTF7LkOwNVUh|ryP MoS0V2FPT0WU
KGN M2jDZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTTfIhKSzVyPUG5MlQ4PjVizszN MWXTRW5ITVJ?
MC-CAR M2TDR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX;DNYpLUUN3ME2xPU43OzF|IN88US=> MmnqV2FPT0WU
BHT-101 NFLhXVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MU\JR|UxRTF7Lke3O{DPxE1? NWXXNFdsW0GQR1XS
SW1783 NF7QV3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzjbZZoUUN3ME2xPU44QDB4IN88US=> MXnTRW5ITVJ?
KP-N-YN MkXZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkHFTWM2OD1{MD6wNlYzKM7:TR?= M{D6RnNCVkeHUh?=
LU-165 NXXuSmtCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTJyLkW1O|Eh|ryP M1PzSXNCVkeHUh?=
GOTO MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTJyLk[0OVEh|ryP NF\HOmhUSU6JRWK=
EFM-19 NF;Cd4JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXuwUWRzUUN3ME2yNU4xPzF4IN88US=> Mnz2V2FPT0WU
CTV-1 NV7kdGN[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HKeWlEPTB;MkGuNVA2PCEQvF2= NYTjfmtxW0GQR1XS
HEL M1rwW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\jcGlEPTB;MkGuOFIyPiEQvF2= NUn5UWZYW0GQR1XS
SNU-C2B M3;6Omdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2fQdmlEPTB;MkGuOFI3KM7:TR?= MWrTRW5ITVJ?
ECC4 NHPQenpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTJzLkewO{DPxE1? MmrVV2FPT0WU
NEC8 NEHMVWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHryRmlKSzVyPUKxMlg{PjhizszN MmjBV2FPT0WU
KMOE-2 NE[2XVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUSzSW06UUN3ME2yNU45QTJzIN88US=> Mm\mV2FPT0WU
NCI-H524 M{XubWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTJ{LkC4NFgh|ryP NVHhdVNXW0GQR1XS
WSU-NHL NIXa[WpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DOZmlEPTB;MkKuNVU4PyEQvF2= NF\RUIJUSU6JRWK=
SF126 M2K4UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{nQVmlEPTB;MkKuNlQ3QSEQvF2= NEXtV2FUSU6JRWK=
HOP-92 M3[4Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUjJR|UxRTJ{LkOxOlch|ryP MoW1V2FPT0WU
CTB-1 NGLJcIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTJ{LkS2O|ch|ryP MUPTRW5ITVJ?
KYSE-270 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonJTWM2OD1{Mj65N|U4KM7:TR?= Mn3lV2FPT0WU
SK-MEL-24 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnncYJVUUN3ME2yN{4yQDdizszN MoHZV2FPT0WU
Calu-3 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfQU4pKSzVyPUKzMlIyOjhizszN MYTTRW5ITVJ?
GAMG NHvzUHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULBZYZEUUN3ME2yN{4zOzZ5IN88US=> NWW1SlVjW0GQR1XS
SW1573 Mnv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XjeWlEPTB;MkOuO|QyPSEQvF2= MoPIV2FPT0WU
MHH-NB-11 M4e1Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXnJR|UxRTJ2LkCxPVQh|ryP NWOxNGIyW0GQR1XS
TK10 MmTaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjYTWM2OD1{ND61NFE{KM7:TR?= MXrTRW5ITVJ?
LB373-MEL-D NED1VZNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVrJR|UxRTJ2Lk[wOlQh|ryP MWnTRW5ITVJ?
KALS-1 MoD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWLTWlNyUUN3ME2yOE44OzJ5IN88US=> MVfTRW5ITVJ?
HUTU-80 NWm2RlNKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoDlTWM2OD1{NT64NFMzKM7:TR?= Mmf2V2FPT0WU
HuP-T3 NWXUOHlQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUjJR|UxRTJ4LkG2O|Qh|ryP MniwV2FPT0WU
OE19 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTaNW9zUUN3ME2yOk4zOTV|IN88US=> M{fEc3NCVkeHUh?=
J82 NIHVWJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MljJTWM2OD1{Nj6yOFcyKM7:TR?= NXywVmNqW0GQR1XS
DU-4475 M1\LVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGS4UFFKSzVyPUK2MlM5OTlizszN MV3TRW5ITVJ?
DMS-53 MlfwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTJ4LkWxN|gh|ryP Ml:4V2FPT0WU
COLO-741 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrpNIRKSzVyPUK2Mlg{PDRizszN NFroOGhUSU6JRWK=
SW48 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHBfW5KSzVyPUK2Mlg5OiEQvF2= M{LUVHNCVkeHUh?=
IGR-1 MkTvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUTJR|UxRTJ4LkmzN|Qh|ryP MXLTRW5ITVJ?
639-V MoPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTJ5LkCyOFUh|ryP MoHjV2FPT0WU
LK-2 NXTUT4lDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfaVZFKSzVyPUK3MlQyPDFizszN MoDlV2FPT0WU
NCI-H2347 Mom4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnfTTWM2OD1{Nz65Olk6KM7:TR?= MUTTRW5ITVJ?
NCI-H2228 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTJ6LkC5NFUh|ryP MVvTRW5ITVJ?
LS-123 NIDCTlFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrmbHhKSzVyPUK4MlEzPjJizszN NH21bXhUSU6JRWK=
U031 NV7ZUHI5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTJ6LkK1NkDPxE1? M1XxbnNCVkeHUh?=
NCI-H1792 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXvRS4NvUUN3ME2yPE41PzJzIN88US=> MUTTRW5ITVJ?
NCI-H2087 NVfTNok5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\RTWM2OD1{OD63OVUzKM7:TR?= MnPjV2FPT0WU
NCI-H2342 MnnQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfrNGNKSzVyPUK5MlUzODhizszN M3vUOHNCVkeHUh?=
SW626 MorzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmfKTWM2OD1{OT63OVYh|ryP NGCzXVRUSU6JRWK=
LB2518-MEL NXLWZYpVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjNTWM2OD1{OT64NVUh|ryP MVzTRW5ITVJ?
RXF393 NUH3folyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2eyd2lEPTB;M{CuNFk2OiEQvF2= M1PqV3NCVkeHUh?=
LC4-1 NVTGWHI1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3\FNGlEPTB;M{CuN|A6OiEQvF2= MVrTRW5ITVJ?
NCI-H1694 MmK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LXcmlEPTB;M{CuOlYzPCEQvF2= MXfTRW5ITVJ?
K5 NUnIbW0xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mom3TWM2OD1|MD65O|AzKM7:TR?= MVrTRW5ITVJ?
HDLM-2 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXu0W|VkUUN3ME2zNE46PzJ3IN88US=> NVToT213W0GQR1XS
BCPAP M2DKN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVfhcYdTUUN3ME2zNU45Ozd7IN88US=> NFjwXI9USU6JRWK=
BC-3 MlPzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mnn1TWM2OD1|Mj6xOFA{KM7:TR?= NUnvSo43W0GQR1XS
LB996-RCC NV\5U2FVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnoPGRzUUN3ME2zNk4zOzV6IN88US=> M2WwT3NCVkeHUh?=
NCI-H2009 Mn\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIH3NnZKSzVyPUOyMlQ6QDFizszN NILkTJFUSU6JRWK=
HTC-C3 NFnWUo5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHG0fGtKSzVyPUOzMlc2OTlizszN NFHBfnVUSU6JRWK=
LAMA-84 NUe3UFJkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4DDdGlEPTB;M{SuOFQxPyEQvF2= NYS5VI46W0GQR1XS
CCRF-CEM NH\l[FhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHXVV2RKSzVyPUO0MlU4OTVizszN NVizR5U2W0GQR1XS
AN3-CA MnrOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTN3LkC1Olgh|ryP NIjvfGhUSU6JRWK=
NCI-H1734 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\KdmlKSzVyPUO1MlI2PjFizszN NX\uRnFvW0GQR1XS
Ca-Ski M3;vUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXS2PY9PUUN3ME2zOU41OTBzIN88US=> NVT4W5dsW0GQR1XS
U-266 Ml7qS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4LnbWlEPTB;M{WuOlEyPCEQvF2= MkHHV2FPT0WU
SBC-5 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPJR|UxRTN3Lke3PFEh|ryP MYjTRW5ITVJ?
GT3TKB M4jx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTN5LkGxOUDPxE1? NWT6eYpQW0GQR1XS
MDA-MB-175-VII MomyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXETWM2OD1|Nz6yNlQ5KM7:TR?= M4PGNHNCVkeHUh?=
PFSK-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MojnTWM2OD1|Nz6yOFM2KM7:TR?= NEfOSHZUSU6JRWK=
IMR-5 M1\YPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TZeGlEPTB;M{euNlQ5PyEQvF2= NIPJcINUSU6JRWK=
Daudi NECyb5BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPCTWM2OD1|Nz6zOVk4KM7:TR?= NH:xOY1USU6JRWK=
A498 MmT5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjTOZNKSzVyPUO3MlczOThizszN MWDTRW5ITVJ?
SCC-4 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TrOGlEPTB;M{euO|g1OyEQvF2= NY\xe5JkW0GQR1XS
COLO-680N MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2nNRmlEPTB;M{iuNlg5PSEQvF2= M4flSnNCVkeHUh?=
SK-MES-1 MkDmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonOTWM2OD1|OD6zNlE2KM7:TR?= NXPPZ|JWW0GQR1XS
SR MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1nKW2lEPTB;M{iuOVQ6PSEQvF2= M17YdXNCVkeHUh?=
LNCaP-Clone-FGC NXjmcpB[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NU\2RpB5UUN3ME2zPE42PjN5IN88US=> NVvHNGFCW0GQR1XS
SK-HEP-1 M{jIVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4X4OmlEPTB;M{iuO|gzOiEQvF2= M2\afHNCVkeHUh?=
BPH-1 NIjxUFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTN6LkizNlkh|ryP M3jJZ3NCVkeHUh?=
NCI-H1755 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYDETXZkUUN3ME2zPU42QDF5IN88US=> NWj5W|RLW0GQR1XS
LXF-289 NGfQ[XdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TnSmlEPTB;M{muPFA5PCEQvF2= M2\lWHNCVkeHUh?=
SW1088 M3;5eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\LOmlEPTB;NECuNlExPyEQvF2= MWjTRW5ITVJ?
MOLT-4 M4WzZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWHJR|UxRTRyLkK5NFEh|ryP MXXTRW5ITVJ?
AsPC-1 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXrUHJKSzVyPUSwMlQ2QDNizszN M1HxO3NCVkeHUh?=
HOP-62 NIDXZYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIrj[WFKSzVyPUSwMlY2PjhizszN M{njZXNCVkeHUh?=
A172 M37Xbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVnJR|UxRTRyLki1NVEh|ryP MWHTRW5ITVJ?
SN12C M1\Y[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3vtSWlEPTB;NECuPVM5PSEQvF2= NYS0Tms4W0GQR1XS
MDA-MB-231 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWXZ[2N6UUN3ME20NE46QDl6IN88US=> MmW2V2FPT0WU
RPMI-2650 NHKwOnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIjPZ3pKSzVyPUSxMlE2QTNizszN NXfibYJiW0GQR1XS
KYSE-140 M4jHTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\LTWM2OD12MT64NVI{KM7:TR?= NEX2[XlUSU6JRWK=
KINGS-1 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnS2TWM2OD12Mj60Olk4KM7:TR?= MUnTRW5ITVJ?
HSC-3 MkH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTR{Lk[2OlEh|ryP Mnj3V2FPT0WU
PC-14 NF3ENHpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{HtTmlEPTB;NEOuNVg5OiEQvF2= M1z4bnNCVkeHUh?=
COR-L105 MmjKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlH2TWM2OD12Mz62OVAzKM7:TR?= NXnQ[4lDW0GQR1XS
BE-13 M37o[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1LY[GlEPTB;NESuNlM4OSEQvF2= MV7TRW5ITVJ?
NCI-H661 NIn1N2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\YfXdKSzVyPUS0MlI6PThizszN NHXrSWtUSU6JRWK=
IST-MEL1 M1\mUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLETWM2OD12ND6zOVk6KM7:TR?= MnzPV2FPT0WU
HCC1806 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2X2dGlEPTB;NESuOVg4OyEQvF2= NGm4cHJUSU6JRWK=
COLO-800 NIHBOnhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[xWG1KSzVyPUS0Mlg1PTNizszN NGjEbFBUSU6JRWK=
IST-SL2 NWnVSVdST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nrTWlEPTB;NEWuNVI1PyEQvF2= MnnuV2FPT0WU
8305C NIrlSnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\6bItKSzVyPUS1MlMxQSEQvF2= MmHxV2FPT0WU
UACC-62 NHX2[m9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf5UY5RUUN3ME20Ok4zQDd3IN88US=> MlywV2FPT0WU
COR-L23 MkfRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HoSGlEPTB;NEeuNVk6KM7:TR?= M{j0eXNCVkeHUh?=
EFE-184 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jIXWlEPTB;NEeuN|g5KM7:TR?= NYjmXmtFW0GQR1XS
DMS-114 NV[xdm9uT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\BcGFsUUN3ME20O{41OTR7IN88US=> MWfTRW5ITVJ?
KYSE-520 M3nXO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYjJR|UxRTR6LkWzNVUh|ryP MYjTRW5ITVJ?
SNG-M NGPSNWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXf0bJR{UUN3ME20PU41OzRizszN MYjTRW5ITVJ?
A2058 MnX4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki3TWM2OD12OT60PFg2KM7:TR?= MmKwV2FPT0WU

... Click to View More Cell Line Experimental Data

In vivo試験 OSI-906 inhibits tumor growth in an IGF-1R-driven xenograft mouse model, with 100% TGI and 55% regression at a dose of 75 mg/kg and 60% TGI and no regression at a dose of 25 mg/kg. OSI-906 administration induces different elimination half-lives of itself in dog, rat and mice, the elimination half-lives are 1.18 hours, 2.64 hours and 2.14 hours, respectively. OSI-906 administration at different single dose once-daily in femal Sprague-Dawley rat and femal CD-1 mouse reveal that the Vmax is not dose-proportional to OSI-906 dose. OSI-906 elevates the blood glucose levels at a dose of 25 mg/kg after 12 days administration. OSI-906 administration at a single dose of 75 mg/kg in IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model achieve maximal inhibition of IGF-1R phosphorylation (80%) between 4 and 24 hours with plasma drug concentrations of 26.6-4.77 μM. [1] OSI-906 administered as a single dose of at 60 mg/kg in NCI-H292 xenografts mice inhibits uptake of glucose at 2, 4, and 24 hours post-treatment in vivo. OSI-906 inhibits the growth of tumors in NCI-H292 xenograft mouse model. [2]
臨床試験 OSI-906 is currently under a Phase III clinical trial in adrenocortical carcinoma (ACC).
特集

プロトコル (参考用のみ)

キナーゼアッセイ: [1]

Protein kinase biochemical assays Protein kinase assays are either performed in-house by ELISA-based assay methods (IGF-1R, IR, EGFR and KDR) or at Upstate Inc. by a radiometric method with ATP at 100 µM concentration. In-house ELISA assays use poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates and phosphorylation is detected using an antiphosphotyrosine antibody conjugated to horseradish peroxidase. The bound antibody is quantified using ABTS as the peroxidase substrate by measuring absorbance at 405 / 490 nm. All assays use purified recombinant kinase catalytic domains. Recombinant enzymes of human IGF-1R or EGFR are expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and are purified in house. IC50 values are determined from the sigmoidal dose–response plot of percent inhibition versus log10 compound concentration. A minimum of three measurements, performed in duplicate, are carried out with in-house assays unless otherwise indicated. OSI-906 at a concentration of 1 µM is profiled versus a panel of kinases using the ProfilerProTM Kinase Selectivity Assay Kit.

細胞アッセイ: [1]

細胞株 MCF7, NCI-H292, Colo-205, HT29, H358, H1703, BxPC3, A673, SW620, DU4475, HepG2 and Hepa-1, RKO 3T3/hulGF-IR and H292 cells
濃度 0.02-0.8 μM
反応時間 3 days
実験の流れ For assays of cell proliferation, cells are seeded into 96-well plates in appropriate media containing FCS 10% and incubated for 3 days in the presence of OSI-906 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of intracellular ATP content using CellTiterGlo. Data is presented as a fraction of maximal proliferation, calculated by dividing the cellular density in the presence of varying concentrations of OSI-906 by the cellular density of control cells treated with vehicle (DMSO) only.

動物実験: [1]

動物モデル IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model
製剤 25 mM tartaric acid
投薬量 25 mg / kg and 75 mg / kg
投与方法 Orally administrated at once-daily oral dose for 14 days

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

参考

化学情報

Download Linsitinib (OSI-906) SDF
分子量 421.49
化学式

C26H23N5O

CAS No. 867160-71-2
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 84 mg/mL (199.29 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 30% PEG 400+0.5% Tween 80+5% Propylene glycol 30mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
化学名 (1s,3s)-3-(8-amino-1-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol

文献中の引用 (15)

Frequently Asked Questions

  • Question 1
    Does the inhibitor dissolve in the vehicle (30% PEG400/0.5%Tween 80/5% propylene glycol) or is it a suspension?

    Answer: OSI-906 in 30% PEG400/0.5%Tween 80/5% propylene glycol is a suspension.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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