Afatinib (BIBW2992)

Afatinib (BIBW2992)は不可逆的にEGF受容体/ HER2含むEGF受容体を抑制、 EGFR L858R , EGFR L858R/T790M と HER2を作用すると、 IC50がそれぞれ0.5 nM, 0.4 nM, 10 nM, 14 nMとなる。

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Afatinib (BIBW2992) 化学構造
分子量: 485.94

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Quality Control & 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)は不可逆的にEGF受容体/ HER2含むEGF受容体を抑制、 EGFR L858R , EGFR L858R/T790M と HER2を作用すると、 IC50がそれぞれ0.5 nM, 0.4 nM, 10 nM, 14 nMとなる。
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 NUnRWmJ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUXsUJlsUUN3ME2wMlAxPTd{IN88US=> MlO5V2FPT0WU
KASUMI-1 NGK2bGpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYDxZ5Y1UUN3ME2wMlAxQTFzIN88US=> NYjvVWs3W0GQR1XS
HCC2218 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1L2[WlEPTB;MD6wNFk5PyEQvF2= MXXTRW5ITVJ?
KARPAS-45 M{jXTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NULLWlVYUUN3ME2wMlAyPjdzIN88US=> M4nxNnNCVkeHUh?=
HSC-4 MlH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFz0VYxKSzVyPUCuNFE4PDhizszN NUDQblh[W0GQR1XS
CHL-1 M321d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYnJR|UxRTBwMEG4N|kh|ryP NYqybYptW0GQR1XS
KY821 NX3VTpZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTBwMEKwOkDPxE1? NEHBVXFUSU6JRWK=
NCI-N87 MnHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXO4fnViUUN3ME2wMlAzPzd|IN88US=> NYeyVo9FW0GQR1XS
DOK NYD2eoNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIjVd3BKSzVyPUCuNFMyQTRizszN NVTjUFhEW0GQR1XS
DSH1 MlnpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYTRN2xJUUN3ME2wMlA{OzF2IN88US=> M{jLfXNCVkeHUh?=
MDA-MB-175-VII MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIP2THBKSzVyPUCuNFM1OTZizszN MYHTRW5ITVJ?
NCI-H2170 NEfocYRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX3JR|UxRTBwMEO3Nlgh|ryP MUTTRW5ITVJ?
BT-474 NF;3eolIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEP2VZlKSzVyPUCuNFQ6QDZizszN NGfGOmVUSU6JRWK=
EFO-27 M1TFd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnjrTWM2OD1yLkC1NVgzKM7:TR?= MV7TRW5ITVJ?
NCI-H720 NWLqNGE{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYPrdol7UUN3ME2wMlA2OzJ3IN88US=> MVvTRW5ITVJ?
PC-14 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwMEW2Olgh|ryP MWDTRW5ITVJ?
EC-GI-10 MnriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MknITWM2OD1yLkC1PVEzKM7:TR?= NX3qSZZTW0GQR1XS
KYSE-450 NYTZTmM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDjN|RKSzVyPUCuNFU6PzhizszN MX\TRW5ITVJ?
BPH-1 NVnh[I1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn0TWM2OD1yLkC1PVg5KM7:TR?= MVfTRW5ITVJ?
NCI-H292 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2XBZ2lEPTB;MD6wOlA6KM7:TR?= MV3TRW5ITVJ?
H9 MlOwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnCTWM2OD1yLkC3NVMzKM7:TR?= MnLRV2FPT0WU
NCI-H526 NUPKRphYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYG4XWx[UUN3ME2wMlA4QDJ|IN88US=> NXnXOpZCW0GQR1XS
NCI-H1623 NYrueYh7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\qXHlKSzVyPUCuNFgxOjVizszN NV6wSYdiW0GQR1XS
KYSE-140 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33YdmlEPTB;MD6wPFM{KM7:TR?= MknhV2FPT0WU
Ca9-22 NWfYb5htT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfqSVl[UUN3ME2wMlA5OzV|IN88US=> NXHEU3N3W0GQR1XS
AU565 M1\VSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zkNWlEPTB;MD6wPFUxPCEQvF2= MkL2V2FPT0WU
ZR-75-30 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrtXm1KSzVyPUCuNFk2PDVizszN NIjiUIpUSU6JRWK=
NCI-H1770 MkLtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTBwMUCyPEDPxE1? NIDaOHBUSU6JRWK=
LB2241-RCC NVPB[XpiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1nQSmlEPTB;MD6xNFg5PCEQvF2= NYTPPGF7W0GQR1XS
CAL-39 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NW\2c|k2UUN3ME2wMlEyPzl{IN88US=> M{HYZnNCVkeHUh?=
UACC-893 MlzmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnueGVzUUN3ME2wMlEyQDh3IN88US=> MnTJV2FPT0WU
LU-65 M4nDZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPvTWM2OD1yLkGyOlM{KM7:TR?= MVfTRW5ITVJ?
HN MljIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGfzXW1KSzVyPUCuNVMxPzdizszN NWqxUXg{W0GQR1XS
TI-73 MnHWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnXYTWM2OD1yLkG0O|E2KM7:TR?= NEfiXWdUSU6JRWK=
KU812 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1r2R2lEPTB;MD6xOVQ2PiEQvF2= MlWxV2FPT0WU
SW13 M2HFTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPMN41rUUN3ME2wMlE3OjF4IN88US=> NWnXOFI5W0GQR1XS
BB30-HNC MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnPUTWM2OD1yLkG2OVc3KM7:TR?= NWGwdmQ5W0GQR1XS
HSC-2 NUnvTllmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwMU[4N|ch|ryP MmeyV2FPT0WU
BV-173 Mom5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTBwMUe1PVYh|ryP NXz3ToYxW0GQR1XS
CAL-27 NXPlUlZxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\STWM2OD1yLkG3OlM3KM7:TR?= NGTUNYFUSU6JRWK=
SBC-1 M{X1XGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlLjTWM2OD1yLkG4PVU6KM7:TR?= NX3sOW1CW0GQR1XS
CAL-33 NEfqSJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMkCxPFQh|ryP MY\TRW5ITVJ?
NCI-H209 MlPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLETWM2OD1yLkKwOFYh|ryP MYnTRW5ITVJ?
COR-L105 MmTYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX;3TnhNUUN3ME2wMlIyODh2IN88US=> MkjhV2FPT0WU
HSC-3 NF7Cco5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXLJR|UxRTBwMkGxPVgh|ryP NVfrNZF7W0GQR1XS
NCI-H69 M172V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYDxUFAxUUN3ME2wMlIyPDVzIN88US=> MlLkV2FPT0WU
MOLT-13 MknZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NI\GNWRKSzVyPUCuNlM6PzVizszN M3nl[3NCVkeHUh?=
ML-2 M2OxTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\yUIRPUUN3ME2wMlI1QDB{IN88US=> M{fFRXNCVkeHUh?=
IGROV-1 M4HqWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3jfGlKSzVyPUCuNlU6PTJizszN M1S5O3NCVkeHUh?=
TK10 MoXKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXvJR|UxRTBwMk[3N|gh|ryP NIfDc41USU6JRWK=
EoL-1-cell M1vZSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkHQTWM2OD1yLkK2PFkzKM7:TR?= M3PvS3NCVkeHUh?=
HO-1-N-1 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrYcVFKSzVyPUCuNlc5PTNizszN NYrSZllYW0GQR1XS
BHY M4iwdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF7ZSolKSzVyPUCuNlg3PTVizszN MVXTRW5ITVJ?
LU-139 NVi5OVNbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYTJR|UxRTBwM{C1NUDPxE1? MUfTRW5ITVJ?
23132-87 M4LZV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{noeGlEPTB;MD6zNVkzOyEQvF2= MWXTRW5ITVJ?
ACHN M2mySmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mo\ETWM2OD1yLkOxPVk1KM7:TR?= MkHVV2FPT0WU
DoTc2-4510 NEnZPHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTBwM{KyNVkh|ryP MVnTRW5ITVJ?
BB65-RCC MkT4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3TTWM2OD1yLkO0OVk{KM7:TR?= M{nkVHNCVkeHUh?=
HLE MnrBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTBwM{WwOFYh|ryP NEO5PIlUSU6JRWK=
HCC1419 MnTBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwM{[0NFgh|ryP NUm0dIhnW0GQR1XS
A388 MkLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HrXWlEPTB;MD6zOlg2PyEQvF2= MX7TRW5ITVJ?
NUGC-3 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUeyeHYxUUN3ME2wMlM5Ozd|IN88US=> M13yPXNCVkeHUh?=
KYSE-180 M2rTdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\PRYRKUUN3ME2wMlM6ODh7IN88US=> MmPGV2FPT0WU
TE-6 Mn\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYnJR|UxRTBwNECyOFYh|ryP NUn6RmQzW0GQR1XS
A498 NUPYfohPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2DqSGlEPTB;MD60NFY4PCEQvF2= MXHTRW5ITVJ?
NCI-H1648 MoHiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUfJR|UxRTBwNESxPFIh|ryP MYPTRW5ITVJ?
DU-145 NXHmTVJbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfpWItzUUN3ME2wMlQ1QDN|IN88US=> NULkfZREW0GQR1XS
CW-2 M3;HcGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4\6RWlEPTB;MD60OlkyPCEQvF2= NEPWbZJUSU6JRWK=
A431 M{L5Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjpTWM2OD1yLkS4NlM{KM7:TR?= MlPLV2FPT0WU
SAS NHn1eoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXfJR|UxRTBwNEizPVgh|ryP NF34RplUSU6JRWK=
NCI-H2126 NYjFSY52T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTFTWM2OD1yLkWxPVI3KM7:TR?= NUnrO|B[W0GQR1XS
NCI-H358 NHnwUlBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf1OWJTUUN3ME2wMlU{OjFizszN M3jJcXNCVkeHUh?=
FADU Ml3iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXXz[nIzUUN3ME2wMlU1PDB2IN88US=> MVLTRW5ITVJ?
ACN MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYC3Z3ExUUN3ME2wMlU2ODl2IN88US=> MWfTRW5ITVJ?
HCC70 NHfCR4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXK1SGRDUUN3ME2wMlU4PjZzIN88US=> M4jWNHNCVkeHUh?=
NCI-H1838 NWf6dGdVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIryUnlKSzVyPUCuOlAzQTlizszN MmLjV2FPT0WU
CAL-54 NEPiTnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwNkG2NlEh|ryP M{jrNXNCVkeHUh?=
NCI-H1975 NYHWVIZ7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mly2TWM2OD1yLk[xO|I5KM7:TR?= MkTUV2FPT0WU
COR-L88 NEL4WYdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWLMO216UUN3ME2wMlY1OTF|IN88US=> NV;kWGd[W0GQR1XS
CTV-1 NEjGdFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPHTWM2OD1yLk[0N|kzKM7:TR?= MXLTRW5ITVJ?
EW-18 NYDzS2J3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTBwNki2PVgh|ryP MmiwV2FPT0WU
HCC1806 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFP6TIRKSzVyPUCuOlk3PjZizszN NHv1[oFUSU6JRWK=
HuP-T4 M1npdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTwTWM2OD1yLk[5O|Yh|ryP MUPTRW5ITVJ?
MDA-MB-361 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M322[2lEPTB;MD63NlY3OiEQvF2= NXHPeI11W0GQR1XS
NCI-H1573 Ml\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPKXIZPUUN3ME2wMlc{PjNizszN NHTPZ4VUSU6JRWK=
KU-19-19 M2HMNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWL5e5k3UUN3ME2wMlc4PDZ2IN88US=> MnXEV2FPT0WU
COLO-678 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk[wTWM2OD1yLkiwPFM1KM7:TR?= M4f3cHNCVkeHUh?=
C-33-A MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfCNFRKSzVyPUCuPFEzQTdizszN M4PGfXNCVkeHUh?=
Calu-3 NGGyeoNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUW4[2FmUUN3ME2wMlgyPDN2IN88US=> NGPjcVdUSU6JRWK=
AGS NWO4[WtlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXO5OlI2UUN3ME2wMlg{PjR6IN88US=> NIKwUWRUSU6JRWK=
SCC-25 NViyR|JzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVf5e3FXUUN3ME2wMlg1OTdzIN88US=> MWfTRW5ITVJ?
JVM-2 NVHjb5pnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnO4TWM2OD1yLki4Nlk6KM7:TR?= MVXTRW5ITVJ?
HCE-T NInySlhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1fR[mlEPTB;MD64PFQzQCEQvF2= NIDWXJFUSU6JRWK=
ES4 MX3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVLX[GR2UUN3ME2wMlk4QDN4IN88US=> MmLkV2FPT0WU
EKVX MnHVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTkRnJKSzVyPUGuNFExPjRizszN MXTTRW5ITVJ?
D-542MG M3HKVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki1TWM2OD1zLkCxNFY1KM7:TR?= MoTLV2FPT0WU
SW1116 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYLIR4llUUN3ME2xMlAyOjh5IN88US=> MYDTRW5ITVJ?
5637 NVT5TZhQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[wdZdKSzVyPUGuNFE2OSEQvF2= Ml2xV2FPT0WU
HT-1376 NF\3U4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWOxWphCUUN3ME2xMlAyPTF|IN88US=> NX\sTphFW0GQR1XS
NB69 M2\xVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jKNGlEPTB;MT6wNlk1PSEQvF2= M4Tre3NCVkeHUh?=
YKG-1 NVWyU5NTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVfNNpFjUUN3ME2xMlA2PDF7IN88US=> MXPTRW5ITVJ?
EW-3 NIPFOFhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorRTWM2OD1zLkC3PFg{KM7:TR?= M2rUXnNCVkeHUh?=
GCIY NEPjN|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnqTWM2OD1zLkC4NVA1KM7:TR?= NEX4UHJUSU6JRWK=
SK-MES-1 Mn;yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGD5T4dKSzVyPUGuNVE1QDdizszN NY\2N5NnW0GQR1XS
PANC-08-13 M37pbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoK3TWM2OD1zLkG2OFE3KM7:TR?= M1XQUXNCVkeHUh?=
SK-NEP-1 NEXub5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXXTWM2OD1zLkG3OVE{KM7:TR?= MnLGV2FPT0WU
SW954 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPqbIVGUUN3ME2xMlIxOjF2IN88US=> NHzlNXZUSU6JRWK=
NCI-SNU-5 M2\QNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjnZZVHUUN3ME2xMlI{QSEQvF2= MlrpV2FPT0WU
SW48 Ml7aS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTFwMkW0N|Ih|ryP NX65enRUW0GQR1XS
HT-3 NF;BOGVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF\6ZY5KSzVyPUGuNlg4PTNizszN M2[4d3NCVkeHUh?=
ETK-1 Ml32S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXO5OWFyUUN3ME2xMlM4PDV4IN88US=> NYnPVJNmW0GQR1XS
SCC-15 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTFwM{m0OVEh|ryP NH;XSYFUSU6JRWK=
DU-4475 NFm0cI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTaeFE{UUN3ME2xMlQxOTJzIN88US=> MX7TRW5ITVJ?
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NCI-H727 M3TaT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NInBToVKSzVyPUiuNVA1OiEQvF2= M3e0b3NCVkeHUh?=
SW1710 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRThwMUi1NVUh|ryP MnXSV2FPT0WU
D-502MG MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mo\aTWM2OD16LkK5NlgzKM7:TR?= Ml[zV2FPT0WU
NCI-H1993 M3H5OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRThwM{O2N|Eh|ryP NWXnWFFRW0GQR1XS
SCC-4 NInNcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRThwNESwOVkh|ryP NYfYVGpuW0GQR1XS
HAL-01 NUjROJZmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvzVYhVUUN3ME24MlUyQTFizszN MkjjV2FPT0WU
GT3TKB MkX6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEjZNnZKSzVyPUiuOlc6PjRizszN M4HVWHNCVkeHUh?=
SK-OV-3 NETHVWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRThwN{GzNlkh|ryP Mn;JV2FPT0WU
COLO-829 Mm\xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;Yd4pyUUN3ME24MlgxQTd4IN88US=> M1G2PXNCVkeHUh?=
OCI-AML2 NGXyUGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjwPXFmUUN3ME24Mlk2PDhzIN88US=> MWjTRW5ITVJ?
OS-RC-2 NX\5NW12T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\6cnJOUUN3ME25MlAzOTlizszN NWfLdlR{W0GQR1XS
BFTC-909 NWe3[mVYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\4TWM2OD17LkC2O|k6KM7:TR?= MWrTRW5ITVJ?
EW-11 Ml3tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTlwMUe2OVMh|ryP M3jnNXNCVkeHUh?=
HCE-4 NFmzbZZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3zpdmlEPTB;OT6yNVU2QCEQvF2= NVzRU2FNW0GQR1XS
BALL-1 NF\aO29Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHjvVm1KSzVyPUmuNlE6ODdizszN MUHTRW5ITVJ?
SF539 M2HpTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HQdmlEPTB;OT6yN|U3OiEQvF2= NYroTGNHW0GQR1XS
CAMA-1 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3riZWlEPTB;OT6yPFEzQCEQvF2= NVfEV4hzW0GQR1XS
C32 NFWzeFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIr0UG9KSzVyPUmuN|MxPjRizszN M1vJU3NCVkeHUh?=
NCI-H1703 M2joRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTlwM{SzO|Uh|ryP NF7rTFdUSU6JRWK=
NCI-H1650 NIni[3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPtVYhKSzVyPUmuOlA6PDZizszN Mn7qV2FPT0WU
NCI-H1563 M4fD[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1za[2lEPTB;OT63OlA{OSEQvF2= M3;xTXNCVkeHUh?=
CAL-85-1 Mk[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TJdmlEPTB;OT64O|M5OyEQvF2= MVLTRW5ITVJ?
UM-UC-3 MoDRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPv[plnUUN3ME25Mlk2ODNizszN M1riR3NCVkeHUh?=
BxPC-3 MknOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYr3cnQ4UUN3ME2xNE4xQTd{IN88US=> NFuxd3VUSU6JRWK=
MHH-PREB-1 NXjxN3N7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4nhO2lEPTB;MUCuNVk6QSEQvF2= MV7TRW5ITVJ?
DEL NIHFZZpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnkeVROUUN3ME2xNE4{QTR4IN88US=> NXuyUWtwW0GQR1XS
HuCCT1 M{\OPWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH;0cIxKSzVyPUGwMlYxOzNizszN MlT1V2FPT0WU
OVCAR-4 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYfKbWJPUUN3ME2xNE45QDN3IN88US=> NIi5WHVUSU6JRWK=
CAL-72 NEjZToZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFvtcYJKSzVyPUGwMlk{QTFizszN M2PIdHNCVkeHUh?=
HCC1954 NHLhN5ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXufnkzUUN3ME2xNU4xPzV2IN88US=> MXvTRW5ITVJ?
EFO-21 MofxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTFzLkGwOFUh|ryP M37s[3NCVkeHUh?=
FTC-133 NVKyNGJuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnfDTWM2OD1zMT6xOFA4KM7:TR?= M{K2OHNCVkeHUh?=
SK-MEL-24 NGnLNZBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPJR|UxRTFzLkKzOlYh|ryP MmT0V2FPT0WU
UACC-62 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGfnVVBKSzVyPUGxMlI{PjhizszN NVTsUldvW0GQR1XS
NCI-H650 NILFcnJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYnBV5NHUUN3ME2xNU4zPDF6IN88US=> Mm\sV2FPT0WU
ALL-PO MnvyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XBU2lEPTB;MUGuNlUyOiEQvF2= M1nzeHNCVkeHUh?=
T84 NWqzZ4JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:4bHlKSzVyPUGxMlM6ODdizszN MVnTRW5ITVJ?
IST-MEL1 MVPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWLJR|UxRTFzLkS1OVkh|ryP NVjh[Fl[W0GQR1XS
SW626 MnLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWDtZlZNUUN3ME2xNU42PzV3IN88US=> M3;t[HNCVkeHUh?=
RPMI-2650 Ml\0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XjNmlEPTB;MUGuOVg5PSEQvF2= NI\iXJVUSU6JRWK=
MC-IXC NHLaO|dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEXESHdKSzVyPUGxMlY4OjhizszN NX7KbWFCW0GQR1XS
HOP-62 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTFzLk[3OlQh|ryP NGLj[VVUSU6JRWK=
NOS-1 NGrwZnFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3vMOGlEPTB;MUGuO|ExQSEQvF2= Mnv6V2FPT0WU
SW1573 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX60Z2dxUUN3ME2xNU44Ojl3IN88US=> Ml\KV2FPT0WU
WM-115 M3nFdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYeyUnNWUUN3ME2xNU44PTh6IN88US=> M4jJVHNCVkeHUh?=
HuO9 NWrPeWh4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1vjXmlEPTB;MUGuPFc4PCEQvF2= NXvaXlRxW0GQR1XS
YAPC M1;D[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1nwfmlEPTB;MUGuPVI2QSEQvF2= MW\TRW5ITVJ?
MDA-MB-453 NFr4WIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTFzLkm1NVUh|ryP MnLYV2FPT0WU
NCI-H596 M{Wx[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHy4VZlKSzVyPUGyMlA{PjlizszN NUO4e2tPW0GQR1XS
A172 M4SxRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYrJR|UxRTF{LkC3PVgh|ryP M2q2SHNCVkeHUh?=
RS4-11 Mk\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXf2U2xZUUN3ME2xNk4yPzJ3IN88US=> M4X3VHNCVkeHUh?=
HCC1937 NXXJPFNoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX7JR|UxRTF{Lke1OlQh|ryP M17qd3NCVkeHUh?=
SW837 MoPES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Moj6TWM2OD1zMj65NFI5KM7:TR?= M3LwbnNCVkeHUh?=
NMC-G1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYDJR|UxRTF{LkmyN|Qh|ryP Mn7EV2FPT0WU
PFSK-1 M2Cw[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPxVmxKSzVyPUGzMlA3KM7:TR?= MlzuV2FPT0WU
DBTRG-05MG NWnzT3I6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2Tm[mlEPTB;MUOuNFY{OiEQvF2= NEfDNmtUSU6JRWK=
SK-UT-1 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmXVTWM2OD1zMz6xNFg{KM7:TR?= MlXwV2FPT0WU
OVCAR-5 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4DMdmlEPTB;MUOuNVU6OyEQvF2= MoXMV2FPT0WU
8505C MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTF|LkKwOlch|ryP NI\wOYhUSU6JRWK=
SK-MEL-1 NVe0[4ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4X6TmlEPTB;MUOuO|E{PSEQvF2= NVXzcWF6W0GQR1XS
LK-2 MmiwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3r0[mlEPTB;MUOuO|Y{QSEQvF2= NFrMSZFUSU6JRWK=
OE33 NYD6R3FlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjMdJhMUUN3ME2xN{44QDZizszN MnfnV2FPT0WU
Ramos-2G6-4C10 MkPWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7H[WJKSzVyPUG0MlAzODJizszN M3fRWXNCVkeHUh?=
EW-13 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIKwSndKSzVyPUG0MlA{PTJizszN MVjTRW5ITVJ?
NCI-H1793 M2XBW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUTJR|UxRTF2LkKwPFch|ryP NYiwSGQ5W0GQR1XS
BHT-101 Mnm0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV60S4FtUUN3ME2xOE4zPDFizszN MlPiV2FPT0WU
RKO NY\pRlFjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\CV|VHUUN3ME2xOE42ODd3IN88US=> NFThXZVUSU6JRWK=
NEC8 NHzBPVJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2PkNGlEPTB;MUSuOVQ4OiEQvF2= M13iPXNCVkeHUh?=
PANC-10-05 NWPOb|BTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk\QTWM2OD1zND62NlQ4KM7:TR?= MW\TRW5ITVJ?
NCI-H2030 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnoTWM2OD1zND62OFQ5KM7:TR?= MkjaV2FPT0WU
C2BBe1 M3K5Nmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTF2Lke2OEDPxE1? NXLnVmF{W0GQR1XS
EM-2 M2PL[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2HMcmlEPTB;MUSuPFU4PiEQvF2= M13YZnNCVkeHUh?=
HCC1395 NV\KTGVFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{XrSWlEPTB;MUSuPVM{QCEQvF2= MU\TRW5ITVJ?
A2058 NIX2[FhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVvJR|UxRTF3LkC0NFkh|ryP NIfXe4tUSU6JRWK=
SW1463 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn6xTWM2OD1zNT6wOFg2KM7:TR?= M3TlWHNCVkeHUh?=
J82 NWSyNo1kT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFniNotKSzVyPUG1MlA2PyEQvF2= M4\xVXNCVkeHUh?=
CAL-120 NFTTT49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV\jVHNyUUN3ME2xOU4yPDR5IN88US=> NFTsSHNUSU6JRWK=
COLO-824 Ml2yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXzJR|UxRTF3LkG1O|kh|ryP NWrUcpJ6W0GQR1XS
LNCaP-Clone-FGC M3fWN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTF3LkSyOFgh|ryP Mm[wV2FPT0WU
CP66-MEL NGexUI1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NInvN3dKSzVyPUG1MlQ3QDhizszN NHz3[HlUSU6JRWK=
OC-314 M3LYfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVf5U3NDUUN3ME2xOU41PzF2IN88US=> NYPubZlOW0GQR1XS
OVCAR-8 MmO4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWfJR|UxRTF3Lki4OlEh|ryP NIDIem1USU6JRWK=
MFE-280 NIm5RmxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWjJR|UxRTF4LkC0PFgh|ryP MYDTRW5ITVJ?
MHH-NB-11 M2T1PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVLJR|UxRTF4LkC4N|kh|ryP NInUXmVUSU6JRWK=
SW1990 M2LUXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTF4LkG3OVUh|ryP NIHIfmpUSU6JRWK=
U-266 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3GxWmlEPTB;MU[uNlI6QSEQvF2= M1L3fnNCVkeHUh?=
MFM-223 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlnDTWM2OD1zNj6zPVY2KM7:TR?= M1faPXNCVkeHUh?=
L-363 MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVvJR|UxRTF4LkS1O|ch|ryP NGDHenBUSU6JRWK=
MCF7 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUfJR|UxRTF4LkS3NlMh|ryP MX7TRW5ITVJ?
SK-MEL-3 NFfOZnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVTQdFd5UUN3ME2xOk41Pzh5IN88US=> MoP1V2FPT0WU
HH NUfVUlNxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NX;GN41TUUN3ME2xOk42OTZ{IN88US=> MV;TRW5ITVJ?
no-10 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fhOGlEPTB;MU[uOlM1OyEQvF2= M{HqUnNCVkeHUh?=
HuP-T3 NFXQWHJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHTvN3dKSzVyPUG2MlY2PzZizszN MYPTRW5ITVJ?
QIMR-WIL MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3xcmhKSzVyPUG2MlcyODVizszN MXrTRW5ITVJ?
NCI-H1092 M2nFUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrHbmRJUUN3ME2xOk45OzF4IN88US=> NUSybpFyW0GQR1XS
MZ2-MEL NXi2O4Y{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzYbYtKSzVyPUG2Mlg1ODNizszN NIrnPYFUSU6JRWK=
ES3 MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrvPWVbUUN3ME2xOk46OTN2IN88US=> Mn3kV2FPT0WU
COLO-684 M1TSZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XnNGlEPTB;MU[uPVQ4PyEQvF2= M4PWW3NCVkeHUh?=
NCI-H661 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml72TWM2OD1zNj65Olk1KM7:TR?= MV3TRW5ITVJ?
CP50-MEL-B M2jPN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPMfJZmUUN3ME2xO{4xOzR|IN88US=> Ml;3V2FPT0WU
NCI-H2405 M4H2Umdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTF5LkG5O|Qh|ryP Mn;qV2FPT0WU
U-2-OS NUD5e21jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MofaTWM2OD1zNz61N|A4KM7:TR?= MkDaV2FPT0WU
RERF-LC-MS M4jtSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHjiPZhKSzVyPUG3MlU2ODhizszN Mle4V2FPT0WU
NCI-H2342 M4XacGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4LvSGlEPTB;MUeuOVU4KM7:TR?= NYP5dFV7W0GQR1XS
ES8 NXnF[lh3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHToSI9KSzVyPUG3MlYxQDdizszN MnrIV2FPT0WU
MOLT-16 NVPHN4NmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTF5Lki5N|Qh|ryP MYLTRW5ITVJ?
RH-18 M4nB[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXnse5VjUUN3ME2xPE4xODN3IN88US=> NHqzTlFUSU6JRWK=
D-283MED NUHKcpprT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkTrTWM2OD1zOD6wNFg5KM7:TR?= NH\CNmxUSU6JRWK=
RCC10RGB NESwTo9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX;aW|FCUUN3ME2xPE4xPTV7IN88US=> NHLkOZhUSU6JRWK=
NCI-H1437 NX\VNmIxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rMcWlEPTB;MUiuNVY1OSEQvF2= Mo\wV2FPT0WU
SW982 NGLFWJNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLiVnJKSzVyPUG4MlI3PzFizszN MYnTRW5ITVJ?
IST-MES1 NH3tRW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2\sXmlEPTB;MUiuOFQzQCEQvF2= M3LaUHNCVkeHUh?=
A704 NIKxO4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDsTWM2OD1zOD60O|U{KM7:TR?= Mn7wV2FPT0WU
ESS-1 NWXQT5pkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXrJR|UxRTF6LkWyNFUh|ryP MnrlV2FPT0WU
SCH M4DXUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NY\GbI42UUN3ME2xPE43PDV4IN88US=> M1PWN3NCVkeHUh?=
COLO-320-HSR MoHvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PSdmlEPTB;MUiuO|Q3KM7:TR?= NV75ZpVZW0GQR1XS
Mo-T MlLHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PoO2lEPTB;MUiuPFIxPCEQvF2= MVzTRW5ITVJ?
Saos-2 MkXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XLOGlEPTB;MUmuNVE3OiEQvF2= MVXTRW5ITVJ?
SW684 M2XSeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUfJR|UxRTF7LkGzNlYh|ryP M2fYWnNCVkeHUh?=
KMOE-2 MkjCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDqRYtKSzVyPUG5MlIzPDJizszN MkXWV2FPT0WU
MMAC-SF NIj1dG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXHJR|UxRTF7LkK2NFch|ryP NXH3RnZxW0GQR1XS
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... 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 2年-20℃
6月-80℃in solvent
別名 N/A
溶解度 (25°C) * In vitro DMSO 97 mg/mL (199.61 mM)
エタノール 15 mg/mL (30.86 mM)
<1 mg/mL (<1 mM)
In vivo 0.5% methylcellulose+0.2% Tween 80 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 (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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* 必須

Related EGFR 阻害剤

  • Erlotinib

    Erlotinib is an EGFR inhibitor with IC50 of 2 nM, >1000-fold more sensitive for EGFR than human c-Src or v-Abl.

  • Afatinib (BIBW2992) Dimaleate

    Afatinib (BIBW2992) Dimaleate irreversibly inhibits EGFR/HER2 including EGFR(wt), EGFR(L858R), EGFR(L858R/T790M) and HER2 with IC50 of 0.5 nM, 0.4 nM, 10 nM and 14 nM, respectively; 100-fold more active against Gefitinib-resistant L858R-T790M EGFR mutant.

  • Poziotinib (HM781-36B)

    Poziotinib (HM781-36B) is an irreversible pan-HER inhibitor with IC50 of 3.2 nM, 5.3 nM and 23.5 nM for HER1, HER2, and HER4, respectively. Phase 2.

  • AZ5104

    AZ5104, the demethylated metabolite of AZD-9291, is a potent EGFR inhibitor. Phase 1.

  • Gefitinib (ZD1839)

    Gefitinib (ZD1839) は、NR6wtEGFRとNR6W細胞のTyr1173、Tyr992、Tyr1173とTyr992のためのEGFR阻害剤で、IC50 がそれぞれ 37 nM、 37nM、 26 nM 、57 nMです。

    Features:A potent EGFR tyrosine kinase inhibitor.

  • Erlotinib HCl (OSI-744)

    Erlotinib HCl (OSI-744)は、2nMのIC50によるHER1/EGFR阻害剤です。

  • Osimertinib (AZD9291)

    AZD9291 is an oral, irreversible, and mutant-selective EGFR inhibitor with IC50 of 12.92, 11.44 and 493.8 nM for Exon 19 deletion EGFR, L858R/T790M EGFR, and WT EGFR, respectively. Phase 3.

  • Lapatinib

    ラパチニブ(Lapatinib Ditosylateの形で使われる)は、有力なEGFRErbB2 阻害剤で、IC50 がそれぞれ 10.8 と 9.2 nMです。

  • AG-490 (Tyrphostin B42)

    AG-490 (Tyrphostin B42)は、EGFRの選択的な阻害剤、ErbB2とJAK2で、IC50 がそれぞれ 0.1 μM、 13.5 μM、 and ~10 μMです。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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