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 MkLZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHOTWM2OD1yLkCwOVczKM7:TR?= NH2wOY5USU6JRWK=
KASUMI-1 NXjjZZE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF23WJlKSzVyPUCuNFA6OTFizszN M3r4W3NCVkeHUh?=
HCC2218 MkPrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTBwMEC5PFch|ryP NU\Pbo5[W0GQR1XS
KARPAS-45 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{\icmlEPTB;MD6wNVY4OSEQvF2= NXPGdI5SW0GQR1XS
HSC-4 Mn\2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfMTWM2OD1yLkCxO|Q5KM7:TR?= MX3TRW5ITVJ?
CHL-1 M4TkOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUXYU4VKUUN3ME2wMlAyQDN7IN88US=> NFvhfppUSU6JRWK=
KY821 NYnJbHRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MW\JR|UxRTBwMEKwOkDPxE1? NVW2eIx4W0GQR1XS
NCI-N87 M3LrUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVHPdWVvUUN3ME2wMlAzPzd|IN88US=> M4jWV3NCVkeHUh?=
DOK M320OWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUHKb4kxUUN3ME2wMlA{OTl2IN88US=> NHjGVHFUSU6JRWK=
DSH1 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3vU[GlEPTB;MD6wN|MyPCEQvF2= Mm\YV2FPT0WU
MDA-MB-175-VII NVTzS4Z[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnP1TWM2OD1yLkCzOFE3KM7:TR?= NWnQU5F6W0GQR1XS
NCI-H2170 NVTOVJplT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvEWolKSzVyPUCuNFM4OjhizszN NE[ySFFUSU6JRWK=
BT-474 M1PFXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4TvbGlEPTB;MD6wOFk5PiEQvF2= M4LPVHNCVkeHUh?=
EFO-27 NYPISnFOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGLDdlRKSzVyPUCuNFUyQDJizszN M2LMfHNCVkeHUh?=
NCI-H720 M3zGNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TQfWlEPTB;MD6wOVMzPSEQvF2= M3W0OnNCVkeHUh?=
PC-14 Mnn1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVPMS5hlUUN3ME2wMlA2PjZ6IN88US=> NFntdm5USU6JRWK=
EC-GI-10 MlOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUHJR|UxRTBwMEW5NVIh|ryP M3nXZnNCVkeHUh?=
KYSE-450 NF\DNWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIXwSHRKSzVyPUCuNFU6PzhizszN M3\aXnNCVkeHUh?=
BPH-1 NEDoXVlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVHJR|UxRTBwMEW5PFgh|ryP NYXBZZF6W0GQR1XS
NCI-H292 NF3p[mFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2r2TGlEPTB;MD6wOlA6KM7:TR?= MW\TRW5ITVJ?
H9 NVnmZ2FGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXnJR|UxRTBwMEexN|Ih|ryP MkSzV2FPT0WU
NCI-H526 NInRO3BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV7rS4VVUUN3ME2wMlA4QDJ|IN88US=> NIjjS4ZUSU6JRWK=
NCI-H1623 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NITNRnNKSzVyPUCuNFgxOjVizszN M2jrUnNCVkeHUh?=
KYSE-140 Mn7jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;5UnhmUUN3ME2wMlA5OzNizszN MYDTRW5ITVJ?
Ca9-22 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3iWXdKSzVyPUCuNFg{PTNizszN MmHUV2FPT0WU
AU565 MnKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTBwMEi1NFQh|ryP NVrSelJzW0GQR1XS
ZR-75-30 NXfm[2k4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvyTWM2OD1yLkC5OVQ2KM7:TR?= Ml7GV2FPT0WU
NCI-H1770 M2fRVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWnISnZVUUN3ME2wMlExOjhizszN NWDIZZo1W0GQR1XS
LB2241-RCC Mo\PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfJR|UxRTBwMUC4PFQh|ryP MW\TRW5ITVJ?
CAL-39 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX3JR|UxRTBwMUG3PVIh|ryP NF\tZ3pUSU6JRWK=
UACC-893 M2PXOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwMUG4PFUh|ryP MYDTRW5ITVJ?
LU-65 NUPGe3ZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTXTWM2OD1yLkGyOlM{KM7:TR?= MnjjV2FPT0WU
HN NH7jXG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTBwMUOwO|ch|ryP NYW3XGJwW0GQR1XS
TI-73 MlWzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFu4eohKSzVyPUCuNVQ4OTVizszN NU\U[lU3W0GQR1XS
KU812 M{Twc2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MorvTWM2OD1yLkG1OFU3KM7:TR?= MWHTRW5ITVJ?
SW13 M3LpVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\CTWM2OD1yLkG2NlE3KM7:TR?= NVnxRZk6W0GQR1XS
BB30-HNC M1nMcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{SyPWlEPTB;MD6xOlU4PiEQvF2= MYPTRW5ITVJ?
HSC-2 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXvTHZKSzVyPUCuNVY5OzdizszN MWPTRW5ITVJ?
BV-173 NW\2fGk6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYrudFRMUUN3ME2wMlE4PTl4IN88US=> NG\te2FUSU6JRWK=
CAL-27 NYfZSnlHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTBwMUe2N|Yh|ryP MVfTRW5ITVJ?
SBC-1 NHO5W49Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXTJR|UxRTBwMUi5OVkh|ryP MXzTRW5ITVJ?
CAL-33 M1Xobmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEP0PIhKSzVyPUCuNlAyQDRizszN NHHTOJhUSU6JRWK=
NCI-H209 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVL0Wmw4UUN3ME2wMlIxPDZizszN M164WHNCVkeHUh?=
COR-L105 NFf2PVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3K4T2lEPTB;MD6yNVA5PCEQvF2= M3nlenNCVkeHUh?=
HSC-3 NX;4dHU4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\HUHpKSzVyPUCuNlEyQThizszN MXjTRW5ITVJ?
NCI-H69 NEPHWm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzITWM2OD1yLkKxOFUyKM7:TR?= MV3TRW5ITVJ?
MOLT-13 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYq5bHBmUUN3ME2wMlI{QTd3IN88US=> M2KxfXNCVkeHUh?=
ML-2 Mn;2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1Xxe2lEPTB;MD6yOFgxOiEQvF2= NGrGWINUSU6JRWK=
IGROV-1 M{fSXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPJR|UxRTBwMkW5OVIh|ryP NIrB[Y5USU6JRWK=
TK10 NET5V2ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH7RUW9KSzVyPUCuNlY4OzhizszN M3\2WnNCVkeHUh?=
EoL-1-cell NGLV[GtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn[zTWM2OD1yLkK2PFkzKM7:TR?= MUXTRW5ITVJ?
HO-1-N-1 MkXIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE\UW2hKSzVyPUCuNlc5PTNizszN NEP0WFFUSU6JRWK=
BHY MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1XpemlEPTB;MD6yPFY2PSEQvF2= MoLWV2FPT0WU
LU-139 NXrsXZNJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{TpXGlEPTB;MD6zNFUyKM7:TR?= Mm\pV2FPT0WU
23132-87 M{Pwemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnOzTWM2OD1yLkOxPVI{KM7:TR?= M{nXN3NCVkeHUh?=
ACHN NUT0dFBOT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4i0fmlEPTB;MD6zNVk6PCEQvF2= M1j3TXNCVkeHUh?=
DoTc2-4510 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWTJR|UxRTBwM{KyNVkh|ryP NGrsfm1USU6JRWK=
BB65-RCC MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkDSTWM2OD1yLkO0OVk{KM7:TR?= Mn7RV2FPT0WU
HLE NFLiVI5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY[zdGdMUUN3ME2wMlM2ODR4IN88US=> M2W1c3NCVkeHUh?=
HCC1419 NWfoZ5IxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHG5XXpKSzVyPUCuN|Y1ODhizszN NHLzSoRUSU6JRWK=
A388 M3r6PGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwM{[4OVch|ryP MUPTRW5ITVJ?
NUGC-3 M2TxVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWrBcmxIUUN3ME2wMlM5Ozd|IN88US=> Mn;RV2FPT0WU
KYSE-180 M2T4Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFPBZYVKSzVyPUCuN|kxQDlizszN M1PZZ3NCVkeHUh?=
TE-6 NUX2XI9YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWjTfplnUUN3ME2wMlQxOjR4IN88US=> M1exZnNCVkeHUh?=
A498 Mn\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYfJR|UxRTBwNEC2O|Qh|ryP MnriV2FPT0WU
NCI-H1648 NF7xW4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3XbI03UUN3ME2wMlQ1OTh{IN88US=> NIHhSotUSU6JRWK=
DU-145 NEWyNGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXnVYx4UUN3ME2wMlQ1QDN|IN88US=> MWrTRW5ITVJ?
CW-2 MnfYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFLJN3RKSzVyPUCuOFY6OTRizszN NFLXOo1USU6JRWK=
A431 M4LGTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnWTWM2OD1yLkS4NlM{KM7:TR?= Mof1V2FPT0WU
SAS MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlrJTWM2OD1yLkS4N|k5KM7:TR?= MkTyV2FPT0WU
NCI-H2126 NWSxVmtmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHLtNJhKSzVyPUCuOVE6OjZizszN NInmNlBUSU6JRWK=
NCI-H358 MnPqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1W0O2lEPTB;MD61N|IyKM7:TR?= MoDKV2FPT0WU
FADU Mnz1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYLJR|UxRTBwNUS0NFQh|ryP MlnlV2FPT0WU
ACN NWroe4RpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvuTWM2OD1yLkW1NFk1KM7:TR?= NUTTTpV5W0GQR1XS
HCC70 MkDPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1vNRWlEPTB;MD61O|Y3OSEQvF2= M3yweXNCVkeHUh?=
NCI-H1838 NH\Bc|RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnTKTWM2OD1yLk[wNlk6KM7:TR?= M2HsWnNCVkeHUh?=
CAL-54 MkDKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHnnSWVKSzVyPUCuOlE3OjFizszN M1zReXNCVkeHUh?=
NCI-H1975 NFvMUmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwNkG3Nlgh|ryP MWXTRW5ITVJ?
COR-L88 NYDsfYxNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYXocGs5UUN3ME2wMlY1OTF|IN88US=> NY\5XZg1W0GQR1XS
CTV-1 NHH3UJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXPJR|UxRTBwNkSzPVIh|ryP MnrsV2FPT0WU
EW-18 M4HKbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnTPTWM2OD1yLk[4Olk5KM7:TR?= MWfTRW5ITVJ?
HCC1806 NHXPcFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2i1[GlEPTB;MD62PVY3PiEQvF2= NXHLTIY4W0GQR1XS
HuP-T4 NIfVWYxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUH3NmRHUUN3ME2wMlY6PzZizszN MlrtV2FPT0WU
MDA-MB-361 M37sPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUWzSnFnUUN3ME2wMlczPjZ{IN88US=> MXvTRW5ITVJ?
NCI-H1573 Mni4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYntbWpyUUN3ME2wMlc{PjNizszN NEPHdIlUSU6JRWK=
KU-19-19 MlrtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnjhTWM2OD1yLke3OFY1KM7:TR?= MmHCV2FPT0WU
COLO-678 NVXSVXhTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3WzW2lEPTB;MD64NFg{PCEQvF2= NUT1[lViW0GQR1XS
C-33-A M4DXe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkfuTWM2OD1yLkixNlk4KM7:TR?= NYPLe3BEW0GQR1XS
Calu-3 M{TYZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVvpV2dMUUN3ME2wMlgyPDN2IN88US=> NXz4TII5W0GQR1XS
AGS MljHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTBwOEO2OFgh|ryP Ml\MV2FPT0WU
SCC-25 MmTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M122[2lEPTB;MD64OFE4OSEQvF2= MlHXV2FPT0WU
JVM-2 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2jOW2lEPTB;MD64PFI6QSEQvF2= M1fSbHNCVkeHUh?=
HCE-T M1rvfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFSwUm9KSzVyPUCuPFg1OjhizszN M2fCTnNCVkeHUh?=
ES4 M13FS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwOUe4N|Yh|ryP MXfTRW5ITVJ?
EKVX MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjQXZRKSzVyPUGuNFExPjRizszN MVfTRW5ITVJ?
D-542MG NF76SmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2fIbGlEPTB;MT6wNVA3PCEQvF2= NHfzN|FUSU6JRWK=
SW1116 NHrMN4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH:0epFKSzVyPUGuNFEzQDdizszN NIjGd49USU6JRWK=
5637 NUjlWYQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M37BU2lEPTB;MT6wNVUyKM7:TR?= M1fiXnNCVkeHUh?=
HT-1376 NX30OnlKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmDaTWM2OD1zLkCxOVE{KM7:TR?= NYrOZ|VJW0GQR1XS
NB69 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETrU5lKSzVyPUGuNFI6PDVizszN NFj2TIVUSU6JRWK=
YKG-1 M3vDemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\zb3RwUUN3ME2xMlA2PDF7IN88US=> M{C2XXNCVkeHUh?=
EW-3 NF7Y[4VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3i2S2lEPTB;MT6wO|g5OyEQvF2= NFXNR2lUSU6JRWK=
GCIY MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV7JR|UxRTFwMEixNFQh|ryP M2q3e3NCVkeHUh?=
SK-MES-1 NFv2cpFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUS4SFNIUUN3ME2xMlEyPDh5IN88US=> NFXpdnlUSU6JRWK=
PANC-08-13 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DwXmlEPTB;MT6xOlQyPiEQvF2= MlnLV2FPT0WU
SK-NEP-1 NFTndoxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlLKTWM2OD1zLkG3OVE{KM7:TR?= M1n1RnNCVkeHUh?=
SW954 M4nhTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXn2O2hZUUN3ME2xMlIxOjF2IN88US=> NFv3UIxUSU6JRWK=
NCI-SNU-5 M{DkOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jxcWlEPTB;MT6yN|kh|ryP Mnn1V2FPT0WU
SW48 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\aVlN3UUN3ME2xMlI2PDN{IN88US=> NIj6bXFUSU6JRWK=
HT-3 NUD1[GZkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3rlWWlEPTB;MT6yPFc2OyEQvF2= NED1cnlUSU6JRWK=
ETK-1 NWf4c40xT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEno[ZVKSzVyPUGuN|c1PTZizszN MWrTRW5ITVJ?
SCC-15 Mme5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXfzSodqUUN3ME2xMlM6PDVzIN88US=> MoTwV2FPT0WU
DU-4475 NY\DeYxjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXXoRWc{UUN3ME2xMlQxOTJzIN88US=> MnnhV2FPT0WU
NB5 M4DLdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlnjTWM2OD1zLkSxN|E4KM7:TR?= NGfUcndUSU6JRWK=
CFPAC-1 M{[2U2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX[yeVRDUUN3ME2xMlQzPDl|IN88US=> NFXDSodUSU6JRWK=
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SW1710 NWLQNmxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYDJR|UxRThwMUi1NVUh|ryP MV\TRW5ITVJ?
D-502MG NVXSTYVLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGnHfm5KSzVyPUiuNlkzQDJizszN NH61c3BUSU6JRWK=
NCI-H1993 NGjHemNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXKx[oZjUUN3ME24MlM{PjNzIN88US=> MV7TRW5ITVJ?
SCC-4 MoDwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1H6T2lEPTB;OD60OFA2QSEQvF2= MYTTRW5ITVJ?
HAL-01 Mn;kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRThwNUG5NUDPxE1? MV3TRW5ITVJ?
GT3TKB MoLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXL6XZJ7UUN3ME24MlY4QTZ2IN88US=> NGnKTHVUSU6JRWK=
SK-OV-3 NH7LVoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRThwN{GzNlkh|ryP NYfwRoRNW0GQR1XS
COLO-829 MkTRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{XYdGlEPTB;OD64NFk4PiEQvF2= NXzWWZVFW0GQR1XS
OCI-AML2 NWKxXlRpT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{DEUGlEPTB;OD65OVQ5OSEQvF2= NI\udWFUSU6JRWK=
OS-RC-2 M2ftbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH76SZNKSzVyPUmuNFIyQSEQvF2= NUjnS|NbW0GQR1XS
BFTC-909 NFTjeZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mnu4TWM2OD17LkC2O|k6KM7:TR?= MWXTRW5ITVJ?
EW-11 NH\3[|JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{PYeWlEPTB;OT6xO|Y2OyEQvF2= NEDJXnVUSU6JRWK=
HCE-4 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\DU5VXUUN3ME25MlIyPTV6IN88US=> NXT1cFRtW0GQR1XS
BALL-1 MkD0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVHJR|UxRTlwMkG5NFch|ryP NVzlfGROW0GQR1XS
SF539 M3rHcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\6c5JRUUN3ME25MlI{PTZ{IN88US=> MX7TRW5ITVJ?
CAMA-1 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmS2TWM2OD17LkK4NVI5KM7:TR?= MXHTRW5ITVJ?
C32 Mn7TS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTYNYRKSzVyPUmuN|MxPjRizszN M{nUUHNCVkeHUh?=
NCI-H1703 MoDOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\HTWM2OD17LkO0N|c2KM7:TR?= MV\TRW5ITVJ?
NCI-H1650 MkPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEDZOXZKSzVyPUmuOlA6PDZizszN MUjTRW5ITVJ?
NCI-H1563 M3rp[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkDSTWM2OD17Lke2NFMyKM7:TR?= NVvGZmtxW0GQR1XS
CAL-85-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH7PVJJKSzVyPUmuPFc{QDNizszN MnnpV2FPT0WU
UM-UC-3 NHHQW5hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DuTGlEPTB;OT65OVA{KM7:TR?= Mn33V2FPT0WU
BxPC-3 M17uSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDQfWJKSzVyPUGwMlA6PzJizszN NUPpUGNSW0GQR1XS
MHH-PREB-1 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnKTWM2OD1zMD6xPVk6KM7:TR?= NGCwfGNUSU6JRWK=
DEL M13WWmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVzJR|UxRTFyLkO5OFYh|ryP MkfEV2FPT0WU
HuCCT1 MmLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF7HS4lKSzVyPUGwMlYxOzNizszN M1XaVXNCVkeHUh?=
OVCAR-4 M{DHb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1r0fmlEPTB;MUCuPFg{PSEQvF2= NVX1PGp4W0GQR1XS
CAL-72 MmXHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{PrcGlEPTB;MUCuPVM6OSEQvF2= MX3TRW5ITVJ?
HCC1954 NIP6S2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M13zVWlEPTB;MUGuNFc2PCEQvF2= NEHJflVUSU6JRWK=
EFO-21 NXnOWFYxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHBVHdKSzVyPUGxMlExPDVizszN NHrFdJBUSU6JRWK=
FTC-133 M3zvRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Ml7sTWM2OD1zMT6xOFA4KM7:TR?= NUTrXGQ2W0GQR1XS
SK-MEL-24 M3;6Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTzUYZKSzVyPUGxMlI{PjZizszN NHTGU5JUSU6JRWK=
UACC-62 M1PqdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTFzLkKzOlgh|ryP NFTKPWVUSU6JRWK=
NCI-H650 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnqzTWM2OD1zMT6yOFE5KM7:TR?= NF;1SohUSU6JRWK=
ALL-PO MYnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUW1fXQ4UUN3ME2xNU4zPTF{IN88US=> NYXDfoh4W0GQR1XS
T84 MmrFS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHTUbmtKSzVyPUGxMlM6ODdizszN NVywUIg2W0GQR1XS
IST-MEL1 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mnr4TWM2OD1zMT60OVU6KM7:TR?= NYfBT2xCW0GQR1XS
SW626 NH3GPG1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnfJTWM2OD1zMT61O|U2KM7:TR?= MU\TRW5ITVJ?
RPMI-2650 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfJR|UxRTFzLkW4PFUh|ryP MV;TRW5ITVJ?
MC-IXC Mm\3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHEcWlKSzVyPUGxMlY4OjhizszN Mn3IV2FPT0WU
HOP-62 NH6zSFNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnrETWM2OD1zMT62O|Y1KM7:TR?= MXzTRW5ITVJ?
NOS-1 M1;BeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{DjOWlEPTB;MUGuO|ExQSEQvF2= NWCyPZI4W0GQR1XS
SW1573 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIXkeItKSzVyPUGxMlczQTVizszN M17aUXNCVkeHUh?=
WM-115 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTFzLke1PFgh|ryP NVnWeXR[W0GQR1XS
HuO9 NEjy[3VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{jx[WlEPTB;MUGuPFc4PCEQvF2= NFrGcFdUSU6JRWK=
YAPC MkWxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnO3TWM2OD1zMT65NlU6KM7:TR?= MoDpV2FPT0WU
MDA-MB-453 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnLWTWM2OD1zMT65OVE2KM7:TR?= NWDRfpM5W0GQR1XS
NCI-H596 M1PtZmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1m2Z2lEPTB;MUKuNFM3QSEQvF2= MVvTRW5ITVJ?
A172 Ml3kS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4K5XmlEPTB;MUKuNFc6QCEQvF2= MknoV2FPT0WU
RS4-11 NGr2VWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV22XYh[UUN3ME2xNk4yPzJ3IN88US=> Mo\BV2FPT0WU
HCC1937 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M322TGlEPTB;MUKuO|U3PCEQvF2= M1rUXnNCVkeHUh?=
SW837 Mn\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml32TWM2OD1zMj65NFI5KM7:TR?= Mn3OV2FPT0WU
NMC-G1 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTF{LkmyN|Qh|ryP MlnnV2FPT0WU
PFSK-1 MlraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NETiNoJKSzVyPUGzMlA3KM7:TR?= M3XvNnNCVkeHUh?=
DBTRG-05MG M1PFNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVjo[llHUUN3ME2xN{4xPjN{IN88US=> MVLTRW5ITVJ?
SK-UT-1 NYnNR2RPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWTCZ25bUUN3ME2xN{4yODh|IN88US=> MkTzV2FPT0WU
OVCAR-5 M{PWdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MULJR|UxRTF|LkG1PVMh|ryP NF\zd4FUSU6JRWK=
8505C MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1fLT2lEPTB;MUOuNlA3PyEQvF2= NYfTfJl4W0GQR1XS
SK-MEL-1 MnrMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml;6TWM2OD1zMz63NVM2KM7:TR?= M3;qNXNCVkeHUh?=
LK-2 NIHQd5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXZTWM2OD1zMz63OlM6KM7:TR?= Mk\GV2FPT0WU
OE33 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1;KU2lEPTB;MUOuO|g3KM7:TR?= NXLBPJdyW0GQR1XS
Ramos-2G6-4C10 NWf0V5pWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGflc2ZKSzVyPUG0MlAzODJizszN NUDETYJ1W0GQR1XS
EW-13 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4HN[GlEPTB;MUSuNFM2OiEQvF2= MmTqV2FPT0WU
NCI-H1793 NWnRS3VPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\ZU2lEPTB;MUSuNlA5PyEQvF2= MW\TRW5ITVJ?
BHT-101 M1qxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NU\sbJBxUUN3ME2xOE4zPDFizszN NVTacIkxW0GQR1XS
RKO MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYHMPFJOUUN3ME2xOE42ODd3IN88US=> MWTTRW5ITVJ?
NEC8 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWrJcHRSUUN3ME2xOE42PDd{IN88US=> NWqxfYNCW0GQR1XS
PANC-10-05 M1vHVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1K2UGlEPTB;MUSuOlI1PyEQvF2= NXvXXFBQW0GQR1XS
NCI-H2030 NXXEXZoxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HmfmlEPTB;MUSuOlQ1QCEQvF2= M2n1dnNCVkeHUh?=
C2BBe1 NFXRXmhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVLJR|UxRTF2Lke2OEDPxE1? MoTSV2FPT0WU
EM-2 NV\Fb5BqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWPJR|UxRTF2Lki1O|Yh|ryP NWGzTIo5W0GQR1XS
HCC1395 MlXkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn3hTWM2OD1zND65N|M5KM7:TR?= MXvTRW5ITVJ?
A2058 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTF3LkC0NFkh|ryP MUfTRW5ITVJ?
SW1463 NUfGNnBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUf4UGVEUUN3ME2xOU4xPDh3IN88US=> MmL0V2FPT0WU
J82 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{nPV2lEPTB;MUWuNFU4KM7:TR?= MmTQV2FPT0WU
CAL-120 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFrrcGhKSzVyPUG1MlE1PDdizszN MUXTRW5ITVJ?
COLO-824 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUjjTpJOUUN3ME2xOU4yPTd7IN88US=> MYrTRW5ITVJ?
LNCaP-Clone-FGC MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL3VZVvUUN3ME2xOU41OjR6IN88US=> MlHpV2FPT0WU
CP66-MEL MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYHJR|UxRTF3LkS2PFgh|ryP M1;yVHNCVkeHUh?=
OC-314 Mk[1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX7JR|UxRTF3LkS3NVQh|ryP MkDhV2FPT0WU
OVCAR-8 M3nTZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEH2VHhKSzVyPUG1Mlg5PjFizszN NWTHfZVSW0GQR1XS
MFE-280 NUnzPWhwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo\PTWM2OD1zNj6wOFg5KM7:TR?= MWTTRW5ITVJ?
MHH-NB-11 M3X3TGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn:4TWM2OD1zNj6wPFM6KM7:TR?= MUPTRW5ITVJ?
SW1990 NGWxXFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlSyTWM2OD1zNj6xO|U2KM7:TR?= MVLTRW5ITVJ?
U-266 MnniS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWTJR|UxRTF4LkKyPVkh|ryP MVfTRW5ITVJ?
MFM-223 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfvTWM2OD1zNj6zPVY2KM7:TR?= NF3wdZRUSU6JRWK=
L-363 NVqzboZ3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWKwOpBtUUN3ME2xOk41PTd5IN88US=> M3P2XnNCVkeHUh?=
MCF7 NHK3UnlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUf5UGVsUUN3ME2xOk41PzJ|IN88US=> NIfYPJdUSU6JRWK=
SK-MEL-3 MmfoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlK0TWM2OD1zNj60O|g4KM7:TR?= MkXOV2FPT0WU
HH NYftNGNsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUj3UIk6UUN3ME2xOk42OTZ{IN88US=> NHXoS2RUSU6JRWK=
no-10 NFfk[ZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ThZmlEPTB;MU[uOlM1OyEQvF2= MYrTRW5ITVJ?
HuP-T3 M3\h[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF;CUppKSzVyPUG2MlY2PzZizszN NWC2fndnW0GQR1XS
QIMR-WIL M1;IV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\RTWM2OD1zNj63NVA2KM7:TR?= Ml3jV2FPT0WU
NCI-H1092 MkfGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTF4LkizNVYh|ryP MVjTRW5ITVJ?
MZ2-MEL NVrNbZg2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M13UdGlEPTB;MU[uPFQxOyEQvF2= MkDkV2FPT0WU
ES3 NYO5[m4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzIcopRUUN3ME2xOk46OTN2IN88US=> MYTTRW5ITVJ?
COLO-684 NWnnd21YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVi4[VM5UUN3ME2xOk46PDd5IN88US=> NUPNfIxSW0GQR1XS
NCI-H661 NHTNdIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF4Lkm2PVQh|ryP NYXaR25QW0GQR1XS
CP50-MEL-B NYK0T4duT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4jUTmlEPTB;MUeuNFM1OyEQvF2= MYDTRW5ITVJ?
NCI-H2405 NWXPU4t[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnFTWM2OD1zNz6xPVc1KM7:TR?= NHLQVoJUSU6JRWK=
U-2-OS M{PYcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGPlfWFKSzVyPUG3MlU{ODdizszN NISzNnNUSU6JRWK=
RERF-LC-MS M{DXNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTF5LkW1NFgh|ryP M2j6b3NCVkeHUh?=
NCI-H2342 NX7Vcm5LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzoZ5M5UUN3ME2xO{42PTdizszN NV;6OI91W0GQR1XS
ES8 M2XiXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rMO2lEPTB;MUeuOlA5PyEQvF2= NUOySFdYW0GQR1XS
MOLT-16 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTF5Lki5N|Qh|ryP MlrIV2FPT0WU
RH-18 NULFWHRDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3np[2lEPTB;MUiuNFA{PSEQvF2= MVHTRW5ITVJ?
D-283MED NWDk[4RsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3fW[WlEPTB;MUiuNFA5QCEQvF2= MnjNV2FPT0WU
RCC10RGB M4GxWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUHJR|UxRTF6LkC1OVkh|ryP MnS2V2FPT0WU
NCI-H1437 Mk\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlSzTWM2OD1zOD6xOlQyKM7:TR?= M4nGSnNCVkeHUh?=
SW982 NHrNdIhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkTxTWM2OD1zOD6yOlcyKM7:TR?= M3G5[3NCVkeHUh?=
IST-MES1 MoXTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2j3dWlEPTB;MUiuOFQzQCEQvF2= MVPTRW5ITVJ?
A704 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGj4eG1KSzVyPUG4MlQ4PTNizszN NIfWSZNUSU6JRWK=
ESS-1 MmG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHle45KSzVyPUG4MlUzODVizszN MmLUV2FPT0WU
SCH M{T1eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MonsTWM2OD1zOD62OFU3KM7:TR?= NGLE[opUSU6JRWK=
COLO-320-HSR MkjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEnq[lNKSzVyPUG4Mlc1PiEQvF2= NF\qbGVUSU6JRWK=
Mo-T M1LlXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPKTWM2OD1zOD64NlA1KM7:TR?= NX;zRYRNW0GQR1XS
Saos-2 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUXJR|UxRTF7LkGxOlIh|ryP MVTTRW5ITVJ?
SW684 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2r6XGlEPTB;MUmuNVMzPiEQvF2= NVzTVGo3W0GQR1XS
KMOE-2 Mo\mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\HeIl[UUN3ME2xPU4zOjR{IN88US=> Mn\HV2FPT0WU
MMAC-SF MnXBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHm3ToJKSzVyPUG5MlI3ODdizszN NXHLTnM2W0GQR1XS
JAR MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTF7LkK5PUDPxE1? MlfGV2FPT0WU
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U-118-MG NIfmVY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rJPGlEPTB;M{[uPFg1PyEQvF2= NEPmOo9USU6JRWK=
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A427 MXPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGi5SVNKSzVyPUO3MlkyODdizszN Ml;GV2FPT0WU
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U251 NFG0dGxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUHJR|UxRTRyLkSwOVQh|ryP M33Xe3NCVkeHUh?=
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HT NV7hZnlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3KOYdKSzVyPUSwMlY3OzlizszN M{HUbHNCVkeHUh?=
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A673 NX;5dppKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4LOPGlEPTB;NEGuOVE2PyEQvF2= M3\CRnNCVkeHUh?=
HPAF-II MlHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkLETWM2OD12MT62O|A6KM7:TR?= M3uxeHNCVkeHUh?=
UACC-257 NXfSfnBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{LTSGlEPTB;NEGuO|M3QSEQvF2= MmDYV2FPT0WU
EW-22 NGPzfGhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDFU41KSzVyPUSxMlg3QTdizszN NETXPJlUSU6JRWK=
NCI-H1755 MnzTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2LxXWlEPTB;NEGuPFczPSEQvF2= M1HmfXNCVkeHUh?=
KYSE-150 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYLJR|UxRTR{LkG3PFIh|ryP M1\2PHNCVkeHUh?=
CGTH-W-1 NILCUHVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M33lPGlEPTB;NEKuOFk2PSEQvF2= MkGzV2FPT0WU
NB13 MnXpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYny[FBEUUN3ME20Nk43OjF5IN88US=> NHnBSmFUSU6JRWK=
SW872 M{XUSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH\BendKSzVyPUSyMlY{OzFizszN MVPTRW5ITVJ?
KP-4 NXrqOoVxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MknXTWM2OD12Mj64PFMzKM7:TR?= M2PqcnNCVkeHUh?=
HCC38 M13PXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDqTHJ5UUN3ME20Nk46PjF6IN88US=> MX7TRW5ITVJ?
BB49-HNC NF\LdWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnLd3V4UUN3ME20N{4zOzV4IN88US=> M1\MfnNCVkeHUh?=
CAL-62 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFjiO|lKSzVyPUSzMlQxOjhizszN NWPnRZppW0GQR1XS
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M14 NYPwVIZoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HafGlEPTB;NESuNVM{OiEQvF2= NETsWnlUSU6JRWK=
COLO-680N NXzXUpVoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH:xTZVKSzVyPUS0MlM{QSEQvF2= NETSeGhUSU6JRWK=
Hs-578-T Mn[zS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXnJR|UxRTR3LkCyPVQh|ryP MUPTRW5ITVJ?
MSTO-211H MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWn6fHFNUUN3ME20OU46PDh{IN88US=> NH7yT2dUSU6JRWK=
EW-1 NX7PdWNET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4rsfGlEPTB;NEWuPVY5QSEQvF2= Mn[5V2FPT0WU
SW948 NFLsZ|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3:3U2lEPTB;NE[uOFQ3OiEQvF2= NGnqUXpUSU6JRWK=
NCI-H460 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEeyTJJKSzVyPUS2MlUzOyEQvF2= NYLSXVFEW0GQR1XS
CAS-1 NYTJfVM1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHHhTVlKSzVyPUS2Mlc4ODFizszN MmP2V2FPT0WU
TGBC11TKB MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIrWVZlKSzVyPUS3MlE4PzdizszN NIfqUpRUSU6JRWK=
HD-MY-Z NVrUNHVRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2[3VGlEPTB;NEiuO|g3KM7:TR?= Mnv0V2FPT0WU
NCI-H226 NGDEO4FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHL3[nlKSzVyPUS5Mlc4QDVizszN MWjTRW5ITVJ?
PA-1 M1fNe2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmXDTWM2OD12OT64N|M2KM7:TR?= NFPmcoZUSU6JRWK=
LB2518-MEL NXz0SWNnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mk[4TWM2OD12OT64O|I{KM7:TR?= MkfwV2FPT0WU
A101D M1TPNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIXLSYlKSzVyPUS5Mlk1OjVizszN MkLXV2FPT0WU
NCI-H2087 MmjTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWjJR|UxRTR7Lkm2PFIh|ryP MUXTRW5ITVJ?

... 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

カスタマーフィードバック (3)


Click to enlarge
Rating
Source Int J Proteomics, 2011, 2011, 215496. Afatinib (BIBW2992) purchased from Selleck
Method CEER assay
Cell Lines H460/A549/RFU cell lines
Concentrations 0-10 μM
Incubation Time 4 h
Results This data showed that a potent dose-dependent inhibition of the HER1 and HER2 pathways in the HCC827 cells was observed by treatment with BIBW-2992. Other HER1 and/or HER2 pathway-activated cell lines, H1975 and H1650, were likewise had these pathway activations blocked by the treatment with BIBW-2992.

Click to enlarge
Rating
Source Int J Proteomics, 2011, 2011, 215496. Afatinib (BIBW2992) purchased from Selleck
Method Nikon inverted-phase microscope
Cell Lines lung tumor cell lines
Concentrations 0.1/1 µM
Incubation Time two weeks
Results Reduction of cell colony size formation was observed by the treatment with the irreversible HER1/2 inhibitor BIBW-2992 in H1975 and H1650 cells as seen when these cells were grown in an anchorage-dependent manner.

Click to enlarge
Rating
Source Dr. Zhang of Tianjin Medical University. Afatinib (BIBW2992) purchased from Selleck
Method Western blot
Cell Lines Breast cancer cells
Concentrations 0-1 nM
Incubation Time 3 h
Results BIBW2992 treatment resulted in a reduction of EGFR phosphorylation in Breast cancer cells.

文献中の引用 (34)

技術サポート&よくある質問(FAQ)

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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