Afatinib (BIBW2992)

Afatinib (BIBW2992)はEGFR/HER2( EGFR(wt)、EGFR(L858R)、EGFR(L858R/T790M) とHER2を含める)を不可逆に抑制して、無細胞試験でIC50値が0.5 nM,0.4 nM,10 nM 和 14 nMにそれえぞれ分かれることです。

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Afatinib (BIBW2992) 化学構造
分子量: 485.94

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MSDS

製品説明

  • Compare EGFR Inhibitors
    EGFR製品生物活性の比較
  • 研究分野
  • Combination Therapy
    併用療法
  • Afatinib (BIBW2992)のメカニズム

製品の説明

生物活性

製品説明 Afatinib (BIBW2992)はEGFR/HER2( EGFR(wt)、EGFR(L858R)、EGFR(L858R/T790M) とHER2を含める)を不可逆に抑制して、無細胞試験でIC50値が0.5 nM,0.4 nM,10 nM 和 14 nMにそれえぞれ分かれることです。
ターゲット

EGFRwt

EGFRL858R

EGFR L858R/T790M

HER2

IC50

0.5 nM

0.4 nM

10 nM

14 nM [1]

In vitro試験 BIBW2992 shows potent activity against both wild-type and mutant forms of EGFR and HER2. It is similar to Gefitinib in potency against L858R EGFR, but about 100-fold more active against the Gefitinib resistant L858R-T790M EGFR double mutant. BIBW2992 exhibits potent effects on both EGFR and HER2 phosphorylation in vivo. It compares favorably to reference compounds (such as Lapatinib et al.) in all cell types tested, such as human epidermoid carcinoma cell line A431 expressing wt EGFR, murine NIH-3T3 cells transfected with wt HER2, as well as breast cancer cell line BT-474 and gastric cancer cell line NCI-N87, which express endogenous HER2. [1]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
HDLM-2 NUS1WpNHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LBdmlEPTB;MD6wNFU4OiEQvF2= NF\Gb|dUSU6JRWK=
KASUMI-1 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{fu[WlEPTB;MD6wNFkyOSEQvF2= MV7TRW5ITVJ?
HCC2218 NWn6dXBmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\yVXpKSzVyPUCuNFA6QDdizszN MWXTRW5ITVJ?
KARPAS-45 NGntSnNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvUWWpvUUN3ME2wMlAyPjdzIN88US=> MluwV2FPT0WU
HSC-4 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\OWnFKSzVyPUCuNFE4PDhizszN M2\3WXNCVkeHUh?=
CHL-1 MoO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTBwMEG4N|kh|ryP M3;MbnNCVkeHUh?=
KY821 M3TrR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4nldGlEPTB;MD6wNlA3KM7:TR?= M13HO3NCVkeHUh?=
NCI-N87 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7jTWM2OD1yLkCyO|c{KM7:TR?= NIj6WJZUSU6JRWK=
DOK NWPxfJVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwMEOxPVQh|ryP NF3hVFVUSU6JRWK=
DSH1 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1TLRWlEPTB;MD6wN|MyPCEQvF2= MmniV2FPT0WU
MDA-MB-175-VII M1[5eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPTTWM2OD1yLkCzOFE3KM7:TR?= MYHTRW5ITVJ?
NCI-H2170 MnOxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWTic5luUUN3ME2wMlA{PzJ6IN88US=> NUPqfWFbW0GQR1XS
BT-474 NV3rdJo5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3XNTWlEPTB;MD6wOFk5PiEQvF2= MnjJV2FPT0WU
EFO-27 NWrKb2pXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jtWWlEPTB;MD6wOVE5OiEQvF2= M{O1TnNCVkeHUh?=
NCI-H720 M{e1UWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml\sTWM2OD1yLkC1N|I2KM7:TR?= Mmi5V2FPT0WU
PC-14 NGP5ZZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1f2R2lEPTB;MD6wOVY3QCEQvF2= NUPJWGViW0GQR1XS
EC-GI-10 M2rqS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml:4TWM2OD1yLkC1PVEzKM7:TR?= Mn[4V2FPT0WU
KYSE-450 NIWxUJpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M17HfGlEPTB;MD6wOVk4QCEQvF2= NFruPJRUSU6JRWK=
BPH-1 NFLHO4RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\aTWM2OD1yLkC1PVg5KM7:TR?= MnTIV2FPT0WU
NCI-H292 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PpU2lEPTB;MD6wOlA6KM7:TR?= M322[HNCVkeHUh?=
H9 M2LOSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnH2TWM2OD1yLkC3NVMzKM7:TR?= NEXLTGpUSU6JRWK=
NCI-H526 NHnlOHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknnTWM2OD1yLkC3PFI{KM7:TR?= MkWzV2FPT0WU
NCI-H1623 M1T4SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\HfW1KSzVyPUCuNFgxOjVizszN MlvhV2FPT0WU
KYSE-140 M1LmPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUS0cZhYUUN3ME2wMlA5OzNizszN MnWyV2FPT0WU
Ca9-22 M1rIO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnPUVBGUUN3ME2wMlA5OzV|IN88US=> NVXhUopuW0GQR1XS
AU565 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{XOe2lEPTB;MD6wPFUxPCEQvF2= M2[yXHNCVkeHUh?=
ZR-75-30 NXfDUFVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF3TNVFKSzVyPUCuNFk2PDVizszN MmD4V2FPT0WU
NCI-H1770 M3PJdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFvtS|VKSzVyPUCuNVAzQCEQvF2= NWjBRVBvW0GQR1XS
LB2241-RCC M2jP[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4r1dWlEPTB;MD6xNFg5PCEQvF2= MnP0V2FPT0WU
CAL-39 NUj1bGlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXjNXVJoUUN3ME2wMlEyPzl{IN88US=> NH;3XmtUSU6JRWK=
UACC-893 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrlTWM2OD1yLkGxPFg2KM7:TR?= Mnq4V2FPT0WU
LU-65 NHHUdZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzBTW04UUN3ME2wMlEzPjN|IN88US=> NWPPXYhKW0GQR1XS
HN NFjyO2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\jTpBNUUN3ME2wMlE{ODd5IN88US=> M3O5VXNCVkeHUh?=
TI-73 NES3PVZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnqwTWM2OD1yLkG0O|E2KM7:TR?= Ml7sV2FPT0WU
KU812 MoDTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWHJR|UxRTBwMUW0OVYh|ryP NHnve4VUSU6JRWK=
SW13 M3Gx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTNTWM2OD1yLkG2NlE3KM7:TR?= NUC4[GJqW0GQR1XS
BB30-HNC MnvGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4S0VGlEPTB;MD6xOlU4PiEQvF2= MV7TRW5ITVJ?
HSC-2 NWruZohjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIP0V2ZKSzVyPUCuNVY5OzdizszN M3v3THNCVkeHUh?=
BV-173 NVLuW2JGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTBwMUe1PVYh|ryP MXjTRW5ITVJ?
CAL-27 NHnGbJBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWX2V|NjUUN3ME2wMlE4PjN4IN88US=> M4\BRXNCVkeHUh?=
SBC-1 Mkn6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwMUi5OVkh|ryP Mn7yV2FPT0WU
CAL-33 NE\CeZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{fScmlEPTB;MD6yNFE5PCEQvF2= MnS4V2FPT0WU
NCI-H209 Mn3vS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUnJbJNFUUN3ME2wMlIxPDZizszN MUDTRW5ITVJ?
COR-L105 NInPVpVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;3[3I1UUN3ME2wMlIyODh2IN88US=> M3W3VXNCVkeHUh?=
HSC-3 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIDse49KSzVyPUCuNlEyQThizszN MUjTRW5ITVJ?
NCI-H69 NYL3dVNQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYG1[ld1UUN3ME2wMlIyPDVzIN88US=> MonOV2FPT0WU
MOLT-13 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV3pRXY2UUN3ME2wMlI{QTd3IN88US=> M2LGeHNCVkeHUh?=
ML-2 MnvIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn\JTWM2OD1yLkK0PFAzKM7:TR?= M1q2NnNCVkeHUh?=
IGROV-1 NXTvVZNGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;BTWM2OD1yLkK1PVUzKM7:TR?= M{XkdHNCVkeHUh?=
TK10 NXLETWNwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwMk[3N|gh|ryP M4DPRXNCVkeHUh?=
EoL-1-cell M37Ddmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrDR2RnUUN3ME2wMlI3QDl{IN88US=> Mly1V2FPT0WU
HO-1-N-1 M3[3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1HieWlEPTB;MD6yO|g2OyEQvF2= MoT5V2FPT0WU
BHY M3\SVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlf4TWM2OD1yLkK4OlU2KM7:TR?= NIP1VFFUSU6JRWK=
LU-139 NH7hVo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGHpeIJKSzVyPUCuN|A2OSEQvF2= MYfTRW5ITVJ?
23132-87 NFvyWWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwM{G5NlMh|ryP NFHSblBUSU6JRWK=
ACHN NYrmT5pCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mki2TWM2OD1yLkOxPVk1KM7:TR?= M2fSe3NCVkeHUh?=
DoTc2-4510 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHWOY9XUUN3ME2wMlMzOjF7IN88US=> MmHHV2FPT0WU
BB65-RCC M4jaemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHyZ2NKSzVyPUCuN|Q2QTNizszN Mn\BV2FPT0WU
HLE MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnrsTWM2OD1yLkO1NFQ3KM7:TR?= NUT6UHlkW0GQR1XS
HCC1419 NX3uNWF{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWXRVJV{UUN3ME2wMlM3PDB6IN88US=> NVW3bFUzW0GQR1XS
A388 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2f6UmlEPTB;MD6zOlg2PyEQvF2= MmrZV2FPT0WU
NUGC-3 NXniVppCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn71TWM2OD1yLkO4N|c{KM7:TR?= M3zpfXNCVkeHUh?=
KYSE-180 NGHwS2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoP2TWM2OD1yLkO5NFg6KM7:TR?= M2C5cnNCVkeHUh?=
TE-6 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfwTWM2OD1yLkSwNlQ3KM7:TR?= NIHibW9USU6JRWK=
A498 MlPVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvoTWM2OD1yLkSwOlc1KM7:TR?= NIDq[mhUSU6JRWK=
NCI-H1648 NYK1eoJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlrJTWM2OD1yLkS0NVgzKM7:TR?= NWfESJRDW0GQR1XS
DU-145 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPzTWM2OD1yLkS0PFM{KM7:TR?= MULTRW5ITVJ?
CW-2 M4e1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVfJR|UxRTBwNE[5NVQh|ryP NXfzNZNoW0GQR1XS
A431 MorvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXCTWM2OD1yLkS4NlM{KM7:TR?= NFH2RlNUSU6JRWK=
SAS M2C5ZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXPJNXlIUUN3ME2wMlQ5Ozl6IN88US=> MXfTRW5ITVJ?
NCI-H2126 NVfCS2NHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF\FT2lKSzVyPUCuOVE6OjZizszN NEjrS4lUSU6JRWK=
NCI-H358 MkDWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HpSGlEPTB;MD61N|IyKM7:TR?= NITWdYVUSU6JRWK=
FADU Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrVPHFKSzVyPUCuOVQ1ODRizszN MX3TRW5ITVJ?
ACN NFTvOXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjITWM2OD1yLkW1NFk1KM7:TR?= MkTMV2FPT0WU
HCC70 M{jPOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{P0cmlEPTB;MD61O|Y3OSEQvF2= NXznWpQ4W0GQR1XS
NCI-H1838 NXyz[o1UT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NI\m[IVKSzVyPUCuOlAzQTlizszN NULt[VNGW0GQR1XS
CAL-54 MlXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLxTWM2OD1yLk[xOlIyKM7:TR?= NXfsZ5NQW0GQR1XS
NCI-H1975 NEntcHRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2TSRWlEPTB;MD62NVczQCEQvF2= NUPxTYUyW0GQR1XS
COR-L88 NF3HWphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWLJR|UxRTBwNkSxNVMh|ryP NV;LNXZoW0GQR1XS
CTV-1 NXSzOHJDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvsfINnUUN3ME2wMlY1Ozl{IN88US=> Mn\BV2FPT0WU
EW-18 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVTYZXFEUUN3ME2wMlY5Pjl6IN88US=> MnP0V2FPT0WU
HCC1806 NV3vXmwxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUHJR|UxRTBwNkm2OlYh|ryP NFXUZ3JUSU6JRWK=
HuP-T4 NGjoU|ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXmxeHA3UUN3ME2wMlY6PzZizszN MVHTRW5ITVJ?
MDA-MB-361 MoTXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXGTWM2OD1yLkeyOlYzKM7:TR?= NIT3dnFUSU6JRWK=
NCI-H1573 M4Locmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;3eoJKSzVyPUCuO|M3OyEQvF2= NWfKNYt6W0GQR1XS
KU-19-19 NH\XdnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTBwN{e0OlQh|ryP MYTTRW5ITVJ?
COLO-678 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\q[I1KSzVyPUCuPFA5OzRizszN NGPxdVBUSU6JRWK=
C-33-A NXXYb4pMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPWSoxKSzVyPUCuPFEzQTdizszN M4TxRXNCVkeHUh?=
Calu-3 NIDt[WxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXyTWM2OD1yLkixOFM1KM7:TR?= Mo\yV2FPT0WU
AGS MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MY\JR|UxRTBwOEO2OFgh|ryP M1HUUHNCVkeHUh?=
SCC-25 MlvtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHleJpKSzVyPUCuPFQyPzFizszN MmDMV2FPT0WU
JVM-2 NUDpUHdxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3nISWlEPTB;MD64PFI6QSEQvF2= MUPTRW5ITVJ?
HCE-T NXP5Z|E2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVfJR|UxRTBwOEi0Nlgh|ryP NX3YPFJWW0GQR1XS
ES4 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUi0dVRuUUN3ME2wMlk4QDN4IN88US=> MU\TRW5ITVJ?
EKVX NFL1VHlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF:3[IJKSzVyPUGuNFExPjRizszN MWHTRW5ITVJ?
D-542MG NFrJ[JNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX3hSFNQUUN3ME2xMlAyODZ2IN88US=> MX;TRW5ITVJ?
SW1116 NVH6eo9tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUHtZWpVUUN3ME2xMlAyOjh5IN88US=> NXL0flNlW0GQR1XS
5637 NH3xbZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml;oTWM2OD1zLkCxOVEh|ryP M2XmdHNCVkeHUh?=
HT-1376 MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEHGSW5KSzVyPUGuNFE2OTNizszN MXHTRW5ITVJ?
NB69 NWW4[m4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmHETWM2OD1zLkCyPVQ2KM7:TR?= MV;TRW5ITVJ?
YKG-1 MnX2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY[3SXd7UUN3ME2xMlA2PDF7IN88US=> NFXXSZhUSU6JRWK=
EW-3 M2fzdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEHRbIpKSzVyPUGuNFc5QDNizszN MYLTRW5ITVJ?
GCIY MmnCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjhdHVKSzVyPUGuNFgyODRizszN NFjEZ4FUSU6JRWK=
SK-MES-1 M2LLVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3fnTWlEPTB;MT6xNVQ5PyEQvF2= M3n2dnNCVkeHUh?=
PANC-08-13 M{LOPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrzUmE4UUN3ME2xMlE3PDF4IN88US=> NFv5dldUSU6JRWK=
SK-NEP-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTFwMUe1NVMh|ryP NYP4[3F2W0GQR1XS
SW954 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVKzTYI2UUN3ME2xMlIxOjF2IN88US=> NUTGPHM4W0GQR1XS
NCI-SNU-5 NGS4RlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTFwMkO5JO69VQ>? MmDUV2FPT0WU
SW48 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mm[5TWM2OD1zLkK1OFMzKM7:TR?= NYr2RpRzW0GQR1XS
HT-3 Mn;1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MonXTWM2OD1zLkK4O|U{KM7:TR?= M3rn[HNCVkeHUh?=
ETK-1 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NU\iPJVPUUN3ME2xMlM4PDV4IN88US=> M3rq[HNCVkeHUh?=
SCC-15 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nNZWlEPTB;MT6zPVQ2OSEQvF2= NV3TcnhwW0GQR1XS
DU-4475 NYnzU5ZZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWLJR|UxRTFwNECxNlEh|ryP NHLUdWhUSU6JRWK=
NB5 MoDuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTFwNEGzNVch|ryP MUPTRW5ITVJ?
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BE-13 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfSTWM2OD15Lkm4NVEzKM7:TR?= Mn\IV2FPT0WU
VMRC-RCZ M3H0WGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRThwMEG2PVch|ryP NEXsfmlUSU6JRWK=
NCI-H727 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\GZWlEPTB;OD6xNFQzKM7:TR?= M1X2eHNCVkeHUh?=
SW1710 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2CyRWlEPTB;OD6xPFUyPSEQvF2= M3Xo[HNCVkeHUh?=
D-502MG MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXfJR|UxRThwMkmyPFIh|ryP MlzoV2FPT0WU
NCI-H1993 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV;JR|UxRThwM{O2N|Eh|ryP M2\LbXNCVkeHUh?=
SCC-4 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXHJR|UxRThwNESwOVkh|ryP NH;wPYVUSU6JRWK=
HAL-01 MnnRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrBb|FtUUN3ME24MlUyQTFizszN MWTTRW5ITVJ?
GT3TKB Mn7CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NY\pW5l5UUN3ME24MlY4QTZ2IN88US=> MlP2V2FPT0WU
SK-OV-3 NV;TOFhZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHINZRbUUN3ME24MlcyOzJ7IN88US=> NWH1[2VoW0GQR1XS
COLO-829 M2LDNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWDK[nRpUUN3ME24MlgxQTd4IN88US=> NHS4SXpUSU6JRWK=
OCI-AML2 M2LoVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRThwOUW0PFEh|ryP NVy1e25oW0GQR1XS
OS-RC-2 NEjTUWlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUPJR|UxRTlwMEKxPUDPxE1? MYTTRW5ITVJ?
BFTC-909 NVK5O5NqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHjxR4NKSzVyPUmuNFY4QTlizszN MWrTRW5ITVJ?
EW-11 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2\B[WlEPTB;OT6xO|Y2OyEQvF2= MojGV2FPT0WU
HCE-4 M1;EOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTlwMkG1OVgh|ryP NH;TWZdUSU6JRWK=
BALL-1 NIj5NllIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTlwMkG5NFch|ryP NUO1b3kxW0GQR1XS
SF539 NH7XeGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXrnZm5WUUN3ME25MlI{PTZ{IN88US=> NWrpSGZ3W0GQR1XS
CAMA-1 M2jlS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HFZmlEPTB;OT6yPFEzQCEQvF2= NYLDc492W0GQR1XS
C32 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1PJeGlEPTB;OT6zN|A3PCEQvF2= M3SxeHNCVkeHUh?=
NCI-H1703 NGjDdoRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Ml7rTWM2OD17LkO0N|c2KM7:TR?= M4jBNHNCVkeHUh?=
NCI-H1650 MmDBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGrNfZZKSzVyPUmuOlA6PDZizszN NWjZPIVZW0GQR1XS
NCI-H1563 M1ywdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnrFTWM2OD17Lke2NFMyKM7:TR?= NYnQd|hiW0GQR1XS
CAL-85-1 NWrsS|RjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUDJR|UxRTlwOEezPFMh|ryP M4rRN3NCVkeHUh?=
UM-UC-3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XWcWlEPTB;OT65OVA{KM7:TR?= M4nOTHNCVkeHUh?=
BxPC-3 NWi2ZYN3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLRPVVKSzVyPUGwMlA6PzJizszN NH\CWWlUSU6JRWK=
MHH-PREB-1 MnLOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4fMdmlEPTB;MUCuNVk6QSEQvF2= M{nhZ3NCVkeHUh?=
DEL NYjTS3N4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXjJR|UxRTFyLkO5OFYh|ryP M1XON3NCVkeHUh?=
HuCCT1 MnLVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4P4W2lEPTB;MUCuOlA{OyEQvF2= NVzGVYc5W0GQR1XS
OVCAR-4 NIK2SZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXkSZZKSzVyPUGwMlg5OzVizszN MmXiV2FPT0WU
CAL-72 MoTUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTFyLkmzPVEh|ryP NYDySVN2W0GQR1XS
HCC1954 Ml\oS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGXlWm5KSzVyPUGxMlA4PTRizszN MUDTRW5ITVJ?
EFO-21 M3uy[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NW\aVXR5UUN3ME2xNU4yODR3IN88US=> NIrYRpZUSU6JRWK=
FTC-133 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MljFTWM2OD1zMT6xOFA4KM7:TR?= MkDJV2FPT0WU
SK-MEL-24 M4rNT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTFzLkKzOlYh|ryP MkXOV2FPT0WU
UACC-62 M13UTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnXpTWM2OD1zMT6yN|Y5KM7:TR?= MUTTRW5ITVJ?
NCI-H650 NYn4Sot{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmnVTWM2OD1zMT6yOFE5KM7:TR?= NVS0O2R7W0GQR1XS
ALL-PO NXPoN|Y2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGizWIZKSzVyPUGxMlI2OTJizszN NVLhfHF{W0GQR1XS
T84 MkfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PGOWlEPTB;MUGuN|kxPyEQvF2= MVPTRW5ITVJ?
IST-MEL1 NF3iT2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHfFfpBKSzVyPUGxMlQ2PTlizszN M1HIbXNCVkeHUh?=
SW626 NIjPZ4hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWXJR|UxRTFzLkW3OVUh|ryP NISxZXZUSU6JRWK=
RPMI-2650 M1jpWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mm\vTWM2OD1zMT61PFg2KM7:TR?= M1;YVXNCVkeHUh?=
MC-IXC NEX5[pFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjOWY1yUUN3ME2xNU43PzJ6IN88US=> M1K5dHNCVkeHUh?=
HOP-62 MnW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoftTWM2OD1zMT62O|Y1KM7:TR?= M2HvZ3NCVkeHUh?=
NOS-1 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmjITWM2OD1zMT63NVA6KM7:TR?= NHTVeJVUSU6JRWK=
SW1573 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX7UZZNQUUN3ME2xNU44Ojl3IN88US=> NXLRe5RFW0GQR1XS
WM-115 MmrYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vnPWlEPTB;MUGuO|U5QCEQvF2= MnnXV2FPT0WU
HuO9 NULhPY5TT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV7JR|UxRTFzLki3O|Qh|ryP MWjTRW5ITVJ?
YAPC M3rJZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFzLkmyOVkh|ryP MlXTV2FPT0WU
MDA-MB-453 M13xZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml;jTWM2OD1zMT65OVE2KM7:TR?= MWTTRW5ITVJ?
NCI-H596 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlrwTWM2OD1zMj6wN|Y6KM7:TR?= NXjEOVRkW0GQR1XS
A172 NGPyWo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1LuOWlEPTB;MUKuNFc6QCEQvF2= M1zqU3NCVkeHUh?=
RS4-11 NVzS[oFqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnmTWM2OD1zMj6xO|I2KM7:TR?= MV\TRW5ITVJ?
HCC1937 NGSzc3ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXfPcplNUUN3ME2xNk44PTZ2IN88US=> MX7TRW5ITVJ?
SW837 M17nUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7xbJpKSzVyPUGyMlkxOjhizszN MYnTRW5ITVJ?
NMC-G1 MnHGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmDPTWM2OD1zMj65NlM1KM7:TR?= MoW4V2FPT0WU
PFSK-1 NFTqT4xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3OPIJ4UUN3ME2xN{4xPiEQvF2= M13CbHNCVkeHUh?=
DBTRG-05MG MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVK2elhFUUN3ME2xN{4xPjN{IN88US=> MljEV2FPT0WU
SK-UT-1 NF3TPGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXT1bFFDUUN3ME2xN{4yODh|IN88US=> M37DOnNCVkeHUh?=
OVCAR-5 Mo\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjWfplwUUN3ME2xN{4yPTl|IN88US=> MVLTRW5ITVJ?
8505C MmXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rrNWlEPTB;MUOuNlA3PyEQvF2= M4\mcXNCVkeHUh?=
SK-MEL-1 NYPkVIlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX7yUYdMUUN3ME2xN{44OTN3IN88US=> MkLPV2FPT0WU
LK-2 MnizS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWPJR|UxRTF|Lke2N|kh|ryP M4nZcnNCVkeHUh?=
OE33 M{nEeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXjVb5lRUUN3ME2xN{44QDZizszN MV;TRW5ITVJ?
Ramos-2G6-4C10 Mk\US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXXJR|UxRTF2LkCyNFIh|ryP MoDiV2FPT0WU
EW-13 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfpTWM2OD1zND6wN|UzKM7:TR?= MWfTRW5ITVJ?
NCI-H1793 Mnm5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoSyTWM2OD1zND6yNFg4KM7:TR?= M1\iXHNCVkeHUh?=
BHT-101 M2jZTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPlTWM2OD1zND6yOFEh|ryP NUG1PXloW0GQR1XS
RKO M1e2RWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV;JR|UxRTF2LkWwO|Uh|ryP NIjVPVBUSU6JRWK=
NEC8 MmG2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2XFZWlEPTB;MUSuOVQ4OiEQvF2= Mk\jV2FPT0WU
PANC-10-05 NH3CXXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUS3W20{UUN3ME2xOE43OjR5IN88US=> M1fudnNCVkeHUh?=
NCI-H2030 NYW5c21wT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVTJR|UxRTF2Lk[0OFgh|ryP MmH4V2FPT0WU
C2BBe1 NI\E[YxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnHuTWM2OD1zND63OlQh|ryP M3r5RXNCVkeHUh?=
EM-2 NHPo[|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTF2Lki1O|Yh|ryP M2HYdnNCVkeHUh?=
HCC1395 NIrMNFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzHeZFKSzVyPUG0Mlk{OzhizszN MofIV2FPT0WU
A2058 NInHdYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTF3LkC0NFkh|ryP MkHRV2FPT0WU
SW1463 M3vvcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTF3LkC0PFUh|ryP MoPXV2FPT0WU
J82 NX\SfJJvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfu[Hd[UUN3ME2xOU4xPTdizszN M3vzWnNCVkeHUh?=
CAL-120 M4\qSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGjnbnNKSzVyPUG1MlE1PDdizszN NYrGfpNQW0GQR1XS
COLO-824 NVXUR4w5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3v5eWlEPTB;MUWuNVU4QSEQvF2= MojKV2FPT0WU
LNCaP-Clone-FGC MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DMemlEPTB;MUWuOFI1QCEQvF2= Mn;UV2FPT0WU
CP66-MEL MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTF3LkS2PFgh|ryP M3;WeHNCVkeHUh?=
OC-314 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYOzW2dlUUN3ME2xOU41PzF2IN88US=> NVPDdWd4W0GQR1XS
OVCAR-8 M4TUXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTF3Lki4OlEh|ryP NV;QdlM4W0GQR1XS
MFE-280 NULHSYNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HlTWlEPTB;MU[uNFQ5QCEQvF2= MknXV2FPT0WU
MHH-NB-11 NYnhTndNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHIemJjUUN3ME2xOk4xQDN7IN88US=> MUHTRW5ITVJ?
SW1990 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkC2TWM2OD1zNj6xO|U2KM7:TR?= MmHmV2FPT0WU
U-266 NHzIcodIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NETKdnZKSzVyPUG2MlIzQTlizszN NFHGcVBUSU6JRWK=
MFM-223 NFHFe41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHIbohKSzVyPUG2MlM6PjVizszN NWrnZottW0GQR1XS
L-363 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PLV2lEPTB;MU[uOFU4PyEQvF2= M2S4V3NCVkeHUh?=
MCF7 M1\ScWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTF4LkS3NlMh|ryP NGny[JNUSU6JRWK=
SK-MEL-3 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1LvcWlEPTB;MU[uOFc5PyEQvF2= MXjTRW5ITVJ?
HH M3LJTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnLYTWM2OD1zNj61NVYzKM7:TR?= NWPTS|VEW0GQR1XS
no-10 NVXwWm11T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGO2T3dKSzVyPUG2MlY{PDNizszN M3mwTHNCVkeHUh?=
HuP-T3 NYTo[IhJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVHpbXQ3UUN3ME2xOk43PTd4IN88US=> NX[3VmJ1W0GQR1XS
QIMR-WIL M1z0XWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYD6b4E3UUN3ME2xOk44OTB3IN88US=> M4LpVnNCVkeHUh?=
NCI-H1092 M3TUfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVHJR|UxRTF4LkizNVYh|ryP NYT4PJlwW0GQR1XS
MZ2-MEL M4myOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NI\ue4NKSzVyPUG2Mlg1ODNizszN M3LTT3NCVkeHUh?=
ES3 M4jnS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF4LkmxN|Qh|ryP MkXjV2FPT0WU
COLO-684 NHTUTFdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIroO5hKSzVyPUG2Mlk1PzdizszN M4HTPXNCVkeHUh?=
NCI-H661 M1G3bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWXkT|hOUUN3ME2xOk46Pjl2IN88US=> Ml3mV2FPT0WU
CP50-MEL-B MknGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmruTWM2OD1zNz6wN|Q{KM7:TR?= NYTFWZRCW0GQR1XS
NCI-H2405 NYfMVZlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\6SGlEPTB;MUeuNVk4PCEQvF2= M3PK[3NCVkeHUh?=
U-2-OS NXy1N4RwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTF5LkWzNFch|ryP M4\Q[nNCVkeHUh?=
RERF-LC-MS NHnveGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFn0bZlKSzVyPUG3MlU2ODhizszN NIrkVnpUSU6JRWK=
NCI-H2342 NVjQUpFwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HVWmlEPTB;MUeuOVU4KM7:TR?= NY\jT3NCW0GQR1XS
ES8 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIe0O3NKSzVyPUG3MlYxQDdizszN Mn;0V2FPT0WU
MOLT-16 MkT6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1f5emlEPTB;MUeuPFk{PCEQvF2= MVnTRW5ITVJ?
RH-18 NX3EVVFnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4PGRWlEPTB;MUiuNFA{PSEQvF2= MoX1V2FPT0WU
D-283MED MmnGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVyweFM5UUN3ME2xPE4xODh6IN88US=> MoftV2FPT0WU
RCC10RGB NVfGfnNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXv1b|hSUUN3ME2xPE4xPTV7IN88US=> NV:0PWtKW0GQR1XS
NCI-H1437 NV3BcVBMT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGHhV2JKSzVyPUG4MlE3PDFizszN NXLPV5Z7W0GQR1XS
SW982 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWjDbGxMUUN3ME2xPE4zPjdzIN88US=> M{DBVnNCVkeHUh?=
IST-MES1 MljmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHrTWM2OD1zOD60OFI5KM7:TR?= MmTKV2FPT0WU
A704 NGn1Z2dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHKUpNKSzVyPUG4MlQ4PTNizszN M1e2VHNCVkeHUh?=
ESS-1 MoftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml\UTWM2OD1zOD61NlA2KM7:TR?= MXjTRW5ITVJ?
SCH MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1G4PGlEPTB;MUiuOlQ2PiEQvF2= MlW3V2FPT0WU
COLO-320-HSR M3vjOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHPTS|BKSzVyPUG4Mlc1PiEQvF2= NWjqeVNVW0GQR1XS
Mo-T M4jvbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLCdo9pUUN3ME2xPE45OjB2IN88US=> M2jJdHNCVkeHUh?=
Saos-2 NGWyc4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTXTWM2OD1zOT6xNVYzKM7:TR?= M4HRXHNCVkeHUh?=
SW684 NV;FZWh1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVTuV5Q4UUN3ME2xPU4yOzJ4IN88US=> M1:2RXNCVkeHUh?=
KMOE-2 M3H2fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELSbW5KSzVyPUG5MlIzPDJizszN NFm4dXVUSU6JRWK=
MMAC-SF MkDpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7CTWM2OD1zOT6yOlA4KM7:TR?= MY\TRW5ITVJ?
JAR NGP6dYNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILx[WZKSzVyPUG5MlI6QSEQvF2= NUTtWFBoW0GQR1XS
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CAL-62 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX7JR|UxRTR|LkSwNlgh|ryP M1uzbHNCVkeHUh?=
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NCI-H460 Ml20S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYjJR|UxRTR4LkWyN{DPxE1? M3fKUnNCVkeHUh?=
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HD-MY-Z M{jGT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnfMTWM2OD12OD63PFYh|ryP NFW4[2RUSU6JRWK=
NCI-H226 NHjLTY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYjGdlVSUUN3ME20PU44Pzh3IN88US=> MXXTRW5ITVJ?
PA-1 M13tVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTR7LkizN|Uh|ryP MUHTRW5ITVJ?
LB2518-MEL NHLuWXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzlTFlwUUN3ME20PU45PzJ|IN88US=> MnLvV2FPT0WU
A101D NGnDUI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWPJR|UxRTR7Lkm0NlUh|ryP MkLBV2FPT0WU
NCI-H2087 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUPJR|UxRTR7Lkm2PFIh|ryP MWfTRW5ITVJ?

... Click to View More Cell Line Experimental Data

In vivo試験 Daily oral administration of BIBW2992 at 20 mg/kg for 25 days results in dramatic tumor regression with a cumulative treated/control tumor volume ratio (T/C ratio) of 2%. Reduced phosphorylation of EGFR and AKT is confirmed by immunohistochemical staining of tissue sections. Therefore, like lapatinib and neratinib, BIBW2992 is a next generation tyrosine kinase inhibitor (TKI) that inhibits human epidermal growth factor receptor 2 (Her2) and epidermal growth factor receptor (EGFR) kinases irreversibly. BIBW2992 is not only active against EGFR mutations targeted by first generation TKIs like Erlotinib or Gefitinib, but also against those insensitive to these standard therapies. [1]
臨床試験 A Phase II clinical trial of BIBW2992 for the treatment of cancer has been terminated.
特集

プロトコル (参考用のみ)

キナーゼアッセイ:

[1]

In vitro kinase activity assays The wild type tyrosine kinase domain of the human EGFR as well as that of the EGFR L858R/T790M double mutant are fused to Glutathione-S-transferase (GST), and extracted. Enzyme activity is then assayed in the presence of the inhibitor BIBW2992, serially diluted in 50% DMSO. A random polymer pEY (4:1) is used as substrate and biotinylated pEY (bio-pEY) is added as a tracer substrate. The kinase domain of HER2 is cloned using the baculovirus system and extracted similarly to that of EGFR kinase. Details of assays for EGFR, HER2, SRC, BIRK and VEGFR2 kinase activity are available in Supplementary information.

細胞アッセイ:

[1]

細胞株 NSCLC cells
濃度 0-10 μM
反応時間 1 hour
実験の流れ

1 × 104 NSCLC cells are transferred into each well of a 96-well plate and cultured overnight in serum-free media for the EGFR phosphorylation assay. After addition of BIBW2992 on the next day, the plates are incubated at 37 °C for 1 hour. EGF-stimulation is done using 100 ng/mL for 10 min at room temperature. Cells are washed with ice cold PBS, extracted with 120 μL HEPEX buffer per well and shaken at room temperature for 1 hour. In all 2 × 104 cells per well is used for the HER2 phosphorylation assay. Streptavidin precoated plates are coated with anti-EGFR-biotin at 1:100 dilution in blocking buffer and c-erb2/HER2 oncoprotein Ab-5(Clone N24)-Biotin. Cell extracts is then transferred to the antibody-coated wells and incubated at room temperature for 1 hour. Extinction is measured at 450 nm.

動物実験:

[1]

動物モデル Athymic NMRI-nu/nu female mice
製剤 In 0.5% methocellulose-0.4% polysorbate-80 (Tween 80)
投薬量 20 mg/kg
投与方法 Oral administration

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 Afatinib (BIBW2992) SDF
分子量 485.94
化学式

C24H25ClFN5O3

CAS No. 439081-18-2
保管 3年-20℃
2年-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 97 mg/mL (199.61 mM)
Ethanol 15 mg/mL (30.86 mM)
Water <1 mg/mL
In vivo 2% DMSO+30% PEG 300+5% Tween 80+ddH2O 10mg/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 (S,E)-N-(4-(3-chloro-4-fluorophenylamino)-7-(tetrahydrofuran-3-yloxy)quinazolin-6-yl)-4-(dimethylamino)but-2-enamide

文献中の引用 (35)

Frequently Asked Questions

  • Question 1
    What’s the recommendation about reconstitution of the compound for in vivo animal study?

    Answer: For in vivo experiment of afatinib, we recommend 0.5% methylcellulose/0.2% Tween 80 as vehicle.

技術サポート&よくある質問(FAQ)

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Tags: Afatinib (BIBW2992)を買う | Afatinib (BIBW2992)供給者 | Afatinib (BIBW2992)を購入する | Afatinib (BIBW2992)費用 | Afatinib (BIBW2992)生産者 | オーダーAfatinib (BIBW2992) | Afatinib (BIBW2992)代理店
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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