OSI-906 (Linsitinib) 化学構造
分子量: 421.49

高品質保証

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Quality Control & 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 OSI-906(Linsitinib)は、IGF-IRとIrの選択的な阻害剤で、IC50 がそれぞれ 35 nM と 75 nMです。
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 NXzke4toT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfVXpdKSzVyPUCuNFI5ODZizszN MY\TRW5ITVJ?
KS-1 NG\1NVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTBwMEO4N|Uh|ryP M{Hp[3NCVkeHUh?=
TE-11 NHnjZoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrTVlNKSzVyPUCuNFc5OjJizszN NWPvdYxnW0GQR1XS
EW-1 NWq4SGtKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1zHWmlEPTB;MD6wPFU5PSEQvF2= MWXTRW5ITVJ?
HMV-II MlOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXwdFU{UUN3ME2wMlA5QDR4IN88US=> MmrhV2FPT0WU
COLO-205 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGT3c3FKSzVyPUCuNVA1PTRizszN M{TCTnNCVkeHUh?=
ES1 NEG0boNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXHe5BiUUN3ME2wMlExPjl4IN88US=> MVTTRW5ITVJ?
GDM-1 NWXHTWZQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVq1PG1CUUN3ME2wMlE{Pjd{IN88US=> NFzzToZUSU6JRWK=
ML-2 M2TKd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHXWpF6UUN3ME2wMlE2QDl4IN88US=> MVXTRW5ITVJ?
Saos-2 NXvPXYVsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHNTWM2OD1yLkG2OVI3KM7:TR?= MoHpV2FPT0WU
NCI-H1355 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTBwMUixN|Uh|ryP NUOwWoZtW0GQR1XS
G-401 NUTEXIozT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4\5XmlEPTB;MD6xPFI{KM7:TR?= MXTTRW5ITVJ?
EW-16 NVLzOo85T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTBwMUi3O|ch|ryP MY\TRW5ITVJ?
EW-7 NFnrfoJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7VbZlKSzVyPUCuNVg5QDFizszN MUXTRW5ITVJ?
NCI-H727 M2XsZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml[1TWM2OD1yLkG5O|k1KM7:TR?= MmjCV2FPT0WU
LCLC-97TM1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXG2Ulg4UUN3ME2wMlIxQTV3IN88US=> MU\TRW5ITVJ?
NCI-H650 NVrU[lZKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVjJR|UxRTBwMkGzPFQh|ryP NU\BRXp3W0GQR1XS
NCI-H2122 NWn1NI53T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUTnfWd1UUN3ME2wMlI{Ojl7IN88US=> NGL6UWdUSU6JRWK=
SK-N-DZ NFvONpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{nEdmlEPTB;MD6yN|Y6QCEQvF2= MkPRV2FPT0WU
HT-29 M{jRemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PxcGlEPTB;MD6yOFI1QCEQvF2= NInGfmRUSU6JRWK=
LB771-HNC NI\QNW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17pemlEPTB;MD6yOVkyPSEQvF2= NUT2ZXpzW0GQR1XS
HT-144 NXzPfpVuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvsbGVvUUN3ME2wMlI3OTlzIN88US=> NFn4PIVUSU6JRWK=
LAN-6 M4DiWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUPJR|UxRTBwMk[zOFgh|ryP MXzTRW5ITVJ?
EW-18 NX\5c3cxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoLGTWM2OD1yLkK3NFAyKM7:TR?= MXrTRW5ITVJ?
LS-1034 NEPTXINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHCOnhKSzVyPUCuNlcyOzJizszN MlLDV2FPT0WU
EW-11 NFnxfZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NW\WelF6UUN3ME2wMlI5PDN{IN88US=> MmT1V2FPT0WU
SNU-C1 NWjVVm1[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LBc2lEPTB;MD6yPVMyOyEQvF2= NGrENmZUSU6JRWK=
RS4-11 NWrjVHVtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX\JR|UxRTBwM{O3OVgh|ryP M1P1dnNCVkeHUh?=
ES4 NFLjfldIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTBwNEGwN|gh|ryP MY\TRW5ITVJ?
COLO-320-HSR M1f2S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXaTWM2OD1yLkSxN|Y5KM7:TR?= NXzZPGdMW0GQR1XS
NB10 NEfQSpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYfLeVRyUUN3ME2wMlQ2PDN5IN88US=> MWHTRW5ITVJ?
BFTC-905 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVvNc|JEUUN3ME2wMlQ3PzV6IN88US=> MmfJV2FPT0WU
A375 NE[4TJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwNEe2NVch|ryP NIHkNJhUSU6JRWK=
SJRH30 MlvMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvGPHZiUUN3ME2wMlUxQDJ{IN88US=> MX\TRW5ITVJ?
NOS-1 NVXX[HVST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTBwNUKyOlch|ryP MmDOV2FPT0WU
SIG-M5 NEDZXIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL2S2EzUUN3ME2wMlU{PTV5IN88US=> NV\FOZh1W0GQR1XS
DOK NW[wfnpqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF:1XItKSzVyPUCuOVU3KM7:TR?= NHLyOoJUSU6JRWK=
NB69 Mn72S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFjPUW9KSzVyPUCuOVgzPTdizszN MoLvV2FPT0WU
SK-NEP-1 M{O1Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjpbYVuUUN3ME2wMlYxOjN4IN88US=> MWPTRW5ITVJ?
SK-MM-2 MkHMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwNkW0PVEh|ryP MkO1V2FPT0WU
NCI-H358 NEXEb5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTYTWM2OD1yLk[3NFgzKM7:TR?= NVrWfYd4W0GQR1XS
RH-1 NVfve3JJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoPvTWM2OD1yLke0PFU6KM7:TR?= NEL5dZlUSU6JRWK=
NH-12 M1vjT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnXRnY3UUN3ME2wMlc3ODR4IN88US=> NGryW5ZUSU6JRWK=
TE-12 MmnNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoG5TWM2OD1yLke2OFg3KM7:TR?= MW\TRW5ITVJ?
COLO-668 M3uwNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{fJZWlEPTB;MD64OFY3PiEQvF2= NG\RS3pUSU6JRWK=
PANC-08-13 Moq0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHJVmxuUUN3ME2wMlg3Ozd5IN88US=> NUHiTHoxW0GQR1XS
HCC2998 MorKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUTOVmQ4UUN3ME2wMlg5OjZ|IN88US=> M33FPHNCVkeHUh?=
ABC-1 NY\Ze3ZtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DBNmlEPTB;MD65NFM2OiEQvF2= MkLMV2FPT0WU
ES6 M4\Mdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\qTWM2OD1yLkmxNFY3KM7:TR?= MnPCV2FPT0WU
SNU-387 NXjiW3FST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTBwOUmzPVMh|ryP M1PvSHNCVkeHUh?=
CMK MnTwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYfvb253UUN3ME2wMlk6QTJ7IN88US=> M4TOXnNCVkeHUh?=
SJSA-1 NXS0NphsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XPZmlEPTB;MT6wN|Y2OyEQvF2= M{j1fnNCVkeHUh?=
SIMA NWCwR4RUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWHKWmNOUUN3ME2xMlA3QDJ3IN88US=> NGS1ZZdUSU6JRWK=
ES3 NXTIdYpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3mwZWlEPTB;MT6xNlI6PyEQvF2= MWrTRW5ITVJ?
IGROV-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL1W3FSUUN3ME2xMlE2PDR2IN88US=> Ml3LV2FPT0WU
MEL-JUSO MmXvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTFwMUW3OVkh|ryP NXHPO2dtW0GQR1XS
T84 MkjNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XlZ2lEPTB;MT6yNFkyPCEQvF2= M3HDW3NCVkeHUh?=
CAL-85-1 NX\nfIxJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NISyclZKSzVyPUGuNlMyOzhizszN M364fXNCVkeHUh?=
RD M1LZTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYC2SZFIUUN3ME2xMlI3PDV3IN88US=> MoTBV2FPT0WU
TE-8 NEnBTHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTFwM{G0OlIh|ryP MnzhV2FPT0WU
L-363 Ml\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPKTWM2OD1zLkO0NlA5KM7:TR?= MVjTRW5ITVJ?
EKVX NEexNJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzKTWM2OD1zLkO0OVY5KM7:TR?= MkLHV2FPT0WU
SK-MEL-3 MlrrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDJR|UxRTFwNEi1OVYh|ryP M2G5R3NCVkeHUh?=
TGBC24TKB Mn\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4jDb2lEPTB;MT61NFE6OyEQvF2= NHrzPZpUSU6JRWK=
NCI-H1770 NInXPYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13yVGlEPTB;MT61NVEyOyEQvF2= MkPtV2FPT0WU
HuH-7 NF3pc|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXjpbYRCUUN3ME2xMlYxODl6IN88US=> MkHWV2FPT0WU
HL-60 M160[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki4TWM2OD1zLk[2PVI5KM7:TR?= M1T6O3NCVkeHUh?=
TE-1 NUHk[olJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjufoFkUUN3ME2xMlcxQTR3IN88US=> M4XJZXNCVkeHUh?=
LC-2-ad MmOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlXtTWM2OD1zLkezPFg4KM7:TR?= NIL4U5NUSU6JRWK=
LB647-SCLC NV[0ZZBpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml3TTWM2OD1zLke2OVg{KM7:TR?= NUDBNJROW0GQR1XS
NCI-H2171 NFrHNHFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPnTWM2OD1zLke3O|E3KM7:TR?= MYDTRW5ITVJ?
SK-PN-DW NF\lXVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfxTWM2OD1zLkmxNlk5KM7:TR?= NIfocWNUSU6JRWK=
MC-IXC NVzTS2RDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3vLOGlEPTB;MT65PFk5KM7:TR?= MVTTRW5ITVJ?
LS-513 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYrvfWh6UUN3ME2yMlA2OzB3IN88US=> M1XVU3NCVkeHUh?=
EW-3 M1z6dmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGrIcopKSzVyPUKuNFk5PDRizszN Mn3WV2FPT0WU
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LP-1 NGLTN5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1nG[GlEPTB;Mj6yOVgxPyEQvF2= NVHlVJA2W0GQR1XS
LU-134-A MnLCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrjTWM2OD1{LkK3O{DPxE1? NYjqfoZ7W0GQR1XS
CP66-MEL NHfme4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rodGlEPTB;Mj6yPVAyPCEQvF2= NIH5eYNUSU6JRWK=
HCC1143 M2Dmemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTJwNEWzOlgh|ryP NHX6ZXlUSU6JRWK=
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TE-10 MkCzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLQTWM2OD1{LkewPFM5KM7:TR?= M{W5SnNCVkeHUh?=
NCI-H1882 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmflTWM2OD1{Lke1NlI4KM7:TR?= MkTzV2FPT0WU
CHP-126 NITZO3lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PYUWlEPTB;Mj63OlMyPyEQvF2= MU\TRW5ITVJ?
NCI-H1623 NUe5[VNPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXXJR|UxRTJwOUKwNlQh|ryP Ml75V2FPT0WU
GB-1 NEP6dY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3nwZ2lEPTB;Mj65N|QxPCEQvF2= NXvQ[VM5W0GQR1XS
RCC10RGB MnzVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTJwOUWyPFEh|ryP MmfJV2FPT0WU
NCI-H2141 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXnJR|UxRTJwOU[4PVYh|ryP NGq5UI5USU6JRWK=
GI-ME-N MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrCTWM2OD1|LkCwOVY2KM7:TR?= NXTLfI4{W0GQR1XS
NCI-H526 NF3oVpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrDcmtKSzVyPUOuNFQxQDVizszN M3mzVnNCVkeHUh?=
NCI-H747 MlH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3fsfGlEPTB;Mz6wOFk6OiEQvF2= NEfGRmVUSU6JRWK=
SNU-423 NYTTWoR4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1XBXmlEPTB;Mz6yNFMyOyEQvF2= MVvTRW5ITVJ?
A427 M1O5W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTNwMkW2PVkh|ryP M2T0dHNCVkeHUh?=
CAL-12T NX3lU2M4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX2xeldWUUN3ME2zMlQxPzF|IN88US=> MUfTRW5ITVJ?
LU-99A MnLGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLBWpJKSzVyPUOuOFcyODVizszN MlLLV2FPT0WU
MS-1 NETDVYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmG5TWM2OD1|LkWzOFI6KM7:TR?= M2jXcnNCVkeHUh?=
SK-LU-1 NHvwN|hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVnORo95UUN3ME2zMlc3Ojl3IN88US=> NEjqU45USU6JRWK=
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LS-411N MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTRwNES4PFUh|ryP NH22UVVUSU6JRWK=
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PANC-10-05 M1WxSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvnTWM2OD12Lk[5PFQh|ryP NV\qWmVXW0GQR1XS
DK-MG MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWT4WnZMUUN3ME20MlgxQTN|IN88US=> MYHTRW5ITVJ?
OVCAR-5 MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3lN4dEUUN3ME20MlgyOjJ4IN88US=> NH\iT4FUSU6JRWK=
CAL-39 M3LLZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3x[m1KSzVyPUSuPFc3PyEQvF2= MnXjV2FPT0WU
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MOLT-16 NHrCdnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWDFcGlzUUN3ME20Mlk2OjV|IN88US=> M{S3RXNCVkeHUh?=
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CAPAN-1 M2j4eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r2emlEPTB;NT6yOVcxPyEQvF2= MWTTRW5ITVJ?
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NCI-H292 NXX5OYplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTVwM{CwOFQh|ryP MXHTRW5ITVJ?
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LB1047-RCC MmSzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2OwTWlEPTB;NT61OVk{OyEQvF2= MoDHV2FPT0WU
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YAPC M3ey[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\seYg3UUN3ME21Mlc3OjBzIN88US=> MWLTRW5ITVJ?
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TE-15 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4TkS2lEPTB;Nj6wOlYxPSEQvF2= M1XXT3NCVkeHUh?=
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NB6 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXqxV|N7UUN3ME22MlI6PjJ{IN88US=> MnG4V2FPT0WU
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NCI-H522 NFnJZ21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHhdIpUUUN3ME22MlM{OzB4IN88US=> MULTRW5ITVJ?
MV-4-11 M4Cwd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{m3[GlEPTB;Nj6zO|A4QSEQvF2= M{HDT3NCVkeHUh?=
LB2241-RCC MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHOxXZBKSzVyPU[uN|g3PjdizszN MWDTRW5ITVJ?
NCI-H1417 MlPGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV7JR|UxRTZwNEC4OFch|ryP NIPufphUSU6JRWK=
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ALL-PO MlXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVzZZZhZUUN3ME22MlcyQTF4IN88US=> M2X2WHNCVkeHUh?=
OVCAR-4 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2G1R2lEPTB;Nj63OVQxPSEQvF2= M{nLWHNCVkeHUh?=
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NCI-H838 NEnzUZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2Ho[2lEPTB;Nj65OlQ6KM7:TR?= NGXKUZBUSU6JRWK=
NCI-H1299 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVS3OHJmUUN3ME22Mlk4ODlizszN MmLIV2FPT0WU
SW954 NEfJWolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\6N5RKSzVyPUeuNlAxPjhizszN MnLOV2FPT0WU
NCI-H441 Moi2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFfmcXdKSzVyPUeuN|QxPjVizszN NUDvfZY1W0GQR1XS
SK-MEL-2 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnMPGFKSzVyPUeuOFg{PzNizszN NUjIZopWW0GQR1XS
KARPAS-45 NGPleG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVS5PYRMUUN3ME23MlY2QTJ7IN88US=> MoDjV2FPT0WU
CAL-54 NFrlOXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmT5TWM2OD15LkiyPVc4KM7:TR?= MV;TRW5ITVJ?
KYSE-180 NY\BdXNOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX\jWpYzUUN3ME23Mlg5QTRzIN88US=> MUfTRW5ITVJ?
NCI-H187 MnjOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe0fJlnUUN3ME23Mlk2QTR5IN88US=> NVHCdJZLW0GQR1XS
RT-112 MoDlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NW\OOHBRUUN3ME24MlA6Pjd5IN88US=> NFnuNlNUSU6JRWK=
NCI-H1437 NHToNWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHRTWM2OD16LkC5O|k2KM7:TR?= NVPUXZFiW0GQR1XS
SNU-449 Mo\FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\ZTWM2OD16LkK4NlczKM7:TR?= MkHVV2FPT0WU
HCC1187 NWW3PWZiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDXTWM2OD16LkK5N|kyKM7:TR?= NVrWNZE2W0GQR1XS
NCI-H2030 NX7FeoE4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfxTWM2OD16LkO3O|E1KM7:TR?= NHGxWIFUSU6JRWK=
HuO-3N1 M1Thfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2rYfWlEPTB;OD6zO|g1PCEQvF2= MVLTRW5ITVJ?
COLO-792 Ml24S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1i3WWlEPTB;OD60NVUzPyEQvF2= MV;TRW5ITVJ?
MIA-PaCa-2 MWHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmH0TWM2OD16Lki1OVA5KM7:TR?= M2r2TnNCVkeHUh?=
SK-N-FI NGPQd3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUX6VIZRUUN3ME25MlA1OjVizszN M{fnUXNCVkeHUh?=
MMAC-SF M2jHS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVyzN2poUUN3ME25MlA6PzVzIN88US=> MoDCV2FPT0WU
NCI-H28 M{PqcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjte|FKSzVyPUmuNVA1PjlizszN NFrpfXVUSU6JRWK=
ETK-1 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjBS45GUUN3ME25MlI6QTd2IN88US=> NVm3e3BoW0GQR1XS
NCI-H1993 NWLtUWJ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPlW3N2UUN3ME25MlQ1OjZzIN88US=> NV\CNnU4W0GQR1XS
no-11 MoH6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{X3Z2lEPTB;OT60O|EzKM7:TR?= NW\jW3huW0GQR1XS
ChaGo-K-1 NXzIcJlyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPTUG9KSzVyPUmuOVE2QDNizszN MV\TRW5ITVJ?
NCCIT MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{LIRmlEPTB;OT61N|E3QSEQvF2= NHHUPGVUSU6JRWK=
SAS NW\VWIs{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PhPWlEPTB;MUCuNlQ5KM7:TR?= NEXSb|NUSU6JRWK=
A673 M{fzN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFL0O4xKSzVyPUGwMlM4ODRizszN NGnUc2pUSU6JRWK=
NCI-H1522 Ml3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTafZVKUUN3ME2xNE4{PzB5IN88US=> NFfO[2pUSU6JRWK=
NCI-H810 M{X1dGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHnCe21KSzVyPUGwMlM6ODdizszN NHLGbolUSU6JRWK=
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GR-ST MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4XhemlEPTB;MUCuOVAzPCEQvF2= NV;3Z2ptW0GQR1XS
SUP-T1 MnLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1rQ[2lEPTB;MUCuO|MyPyEQvF2= MVrTRW5ITVJ?
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MZ1-PC NIrWOllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{TzVmlEPTB;MUCuPVU4OSEQvF2= M{jZVnNCVkeHUh?=
SK-CO-1 NIXNZoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTFyLkm5N|Eh|ryP MmjLV2FPT0WU
Capan-2 Moe1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV;JR|UxRTFzLkOxPVgh|ryP MoTpV2FPT0WU
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REH NFPkW5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn6zTWM2OD1zMT63OFUyKM7:TR?= NYjkWFRkW0GQR1XS
GI-1 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XTfmlEPTB;MUGuPFYyPSEQvF2= MoO4V2FPT0WU
BB65-RCC MmLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrMSlY{UUN3ME2xNk4xQTF4IN88US=> MVjTRW5ITVJ?
NCI-H1651 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{HV[GlEPTB;MUKuNlQ4QCEQvF2= MVHTRW5ITVJ?
NCI-H1618 Mn3VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGnpVldKSzVyPUGyMlM6PzZizszN M1fPU3NCVkeHUh?=
NCI-H2081 NXjTOoNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3e2e2lEPTB;MUKuOlE1OSEQvF2= MkHiV2FPT0WU
GCIY MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnKyTWM2OD1zMj63NlE{KM7:TR?= MU\TRW5ITVJ?
NY NYTWUG14T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYnJXIR{UUN3ME2xN{4xPjR|IN88US=> NFvMNodUSU6JRWK=
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SK-OV-3 NF7a[G1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVjJR|UxRTF|LkO3OlMh|ryP M1L5ZXNCVkeHUh?=
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LC-1F NUfLRm5oT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfEfFliUUN3ME2xOE4xOzV4IN88US=> Mlr6V2FPT0WU
SNB75 NEf5NYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDxTWM2OD1zND6wN|g{KM7:TR?= MXvTRW5ITVJ?
CHP-212 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGS0dGRKSzVyPUG0MlA1PjRizszN NXiz[mVJW0GQR1XS
HT-1376 M3n4UGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjWNWlCUUN3ME2xOE4yOTJ4IN88US=> Ml;VV2FPT0WU
MONO-MAC-6 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXjJR|UxRTF2LkG1NFIh|ryP Mnq0V2FPT0WU
CA46 NYfPNXp{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIXvXZpKSzVyPUG0MlE5OjdizszN NVz0[|dyW0GQR1XS
SCC-15 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEfjTFlKSzVyPUG0MlU2QDNizszN MVfTRW5ITVJ?
ATN-1 M2POTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXoTWM2OD1zND62OlI4KM7:TR?= M2DDbnNCVkeHUh?=
NCI-H2405 NInY[5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\TfGlEPTB;MUSuPFE2PyEQvF2= NEe1SJpUSU6JRWK=
NCI-H716 NFPjSnBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUDFRoZZUUN3ME2xOE45PDl|IN88US=> MkjnV2FPT0WU
SW620 NV65O49lT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYHJR|UxRTF2LkmwNVQh|ryP MX7TRW5ITVJ?
NCI-H226 M37jNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{T6[mlEPTB;MUSuPVA5PSEQvF2= MVfTRW5ITVJ?
SW962 Mk\kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3;1T2lEPTB;MUSuPVQ{OiEQvF2= NILM[ppUSU6JRWK=
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OCUB-M M{LUT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TlN2lEPTB;MUSuPVg5OyEQvF2= NF7hPXBUSU6JRWK=
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CAKI-1 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvoUnJKSzVyPUG1MlU{PDZizszN M172VXNCVkeHUh?=
MKN28 M2fzcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrXSoh1UUN3ME2xOU42PDd7IN88US=> MYXTRW5ITVJ?
SW13 NE\4VWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfwNplKSzVyPUG1MlYyQCEQvF2= Mny4V2FPT0WU
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LU-65 NU\ScJNTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[ySmlEPTB;MUWuPVc3QCEQvF2= MoLQV2FPT0WU
Calu-1 M{XURWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnQTWM2OD1zNj6wN|Y5KM7:TR?= NWHUcYxpW0GQR1XS
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MN-60 Ml;QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1jlZWlEPTB;MUeuNlI6PyEQvF2= MYnTRW5ITVJ?
MPP-89 NXfTfnExT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzB[G9EUUN3ME2xO{4zPDV7IN88US=> NX3ZUo5nW0GQR1XS
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NCI-H2126 MmTLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUXJR|UxRTF5LkS3O|Eh|ryP MUjTRW5ITVJ?
NCI-H1563 Ml;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXrTWM2OD1zNz60PVE4KM7:TR?= NXPYcXFrW0GQR1XS
8-MG-BA M{jqdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPofFAzUUN3ME2xO{43PjR6IN88US=> MnHGV2FPT0WU
786-0 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTF5LkizOVMh|ryP NXvLVFlvW0GQR1XS
AM-38 MkfDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF5LkmzNFYh|ryP MYDTRW5ITVJ?
COLO-824 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2P2fWlEPTB;MUiuOFQ{PiEQvF2= NWXuSGlNW0GQR1XS
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CESS MkfiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoLSTWM2OD1zOD63OlA6KM7:TR?= MV3TRW5ITVJ?
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NCI-H2170 NF7oWodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXVTWM2OD1zOD65NVc6KM7:TR?= MWLTRW5ITVJ?
HT-3 Mn\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1P6WmlEPTB;MUiuPVg{KM7:TR?= NI\DdYhUSU6JRWK=
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... 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 OSI-906 (Linsitinib) SDF
分子量 421.49
化学式

C26H23N5O

CAS No. 867160-71-2
保管 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 84 mg/mL (199.29 mM)
<1 mg/mL (<1 mM)
エタノール <1 mg/mL (<1 mM)
In vivo 30% PEG400/0.5% Tween80/5% propylene glycol 30 mg/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

カスタマーフィードバック (3)


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Source Cancer Res, 2013, 73, 834-843. OSI-906 (Linsitinib) purchased from Selleck
Method Cell proliferation and growth assays
Cell Lines PFR3 cells
Concentrations 1 μM
Incubation Time
Results The IC50 of PFR3 cells for PF299804 was more than 100 fold lower with the combination of OSI-90 than with PF00299804 alone.

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Source Cancer Res, 2011, 71, 6773-84. OSI-906 (Linsitinib) purchased from Selleck
Method [18 F]FDG –PET/ Western blot
Cell Lines MCF-7 cells/athymic mice
Concentrations 50 mg/kg/day
Incubation Time 6 weeks
Results mice without palpable tumors were randomized to treatment with vehicle or OSI-906. Six of 20 control mice (30%) developed tumors, whereas none of the 20 OSI-906–treated mice did (Fig. A). OSI-906 inhibited tumor growth compared with vehicle (Fig. B; P < 0.05). OSI-906–treated tumors exhibited markedly lower levels of phosphorylated IGF-IR, InsR, IRS-1, AKT, and S6 compared with vehicle controls (Fig. C). FDG uptake was significantly decreased 4 hours after a single dose of OSI-906 com-pared with baseline (Fig. D)

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Source OSI-906 (Linsitinib) purchased from Selleck
Method Flow cytometry/ Western Blotting
Cell Lines CLL B cells
Concentrations 1 µM
Incubation Time 24 h
Results three structurally unrelated IGF1R inhibi tors AG1024, Picropodophyllin (PPP) and linsitinib significantly reduced the cellular viability of primary CLL cells ( Figure A) and reduced levels of phosphorylated IGF1R and IRS-1 (Figure B,C). AG1024, which showed the strongest effect on viability, caused a dose-dependent decrease in the levels of phosphorylated Src, PI3K, Akt, MEK and ERK (Figure D).

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Tags: OSI-906 (Linsitinib)を買う | OSI-906 (Linsitinib)供給者 | OSI-906 (Linsitinib)を購入する | OSI-906 (Linsitinib)費用 | OSI-906 (Linsitinib)生産者 | オーダーOSI-906 (Linsitinib) | OSI-906 (Linsitinib)代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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