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

高品質保証

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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 MlO1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MljDTWM2OD1yLkCwOVczKM7:TR?= NV74XlVoW0GQR1XS
KASUMI-1 M{fNO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYLJR|UxRTBwMEC5NVEh|ryP MlLXV2FPT0WU
HCC2218 NUTPXWJqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGrBc|hKSzVyPUCuNFA6QDdizszN MUTTRW5ITVJ?
KARPAS-45 M4G0bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTrTWM2OD1yLkCxOlcyKM7:TR?= MWjTRW5ITVJ?
HSC-4 M{fSfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NX\BS5doUUN3ME2wMlAyPzR6IN88US=> MlHqV2FPT0WU
CHL-1 NX\nfpR{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rLc2lEPTB;MD6wNVg{QSEQvF2= NED3fYdUSU6JRWK=
KY821 NFTnUYZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYnJR|UxRTBwMEKwOkDPxE1? MnzRV2FPT0WU
NCI-N87 NF3JSW5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYTJR|UxRTBwMEK3O|Mh|ryP MXTTRW5ITVJ?
DOK MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3;KOGlEPTB;MD6wN|E6PCEQvF2= NUTNc2VpW0GQR1XS
DSH1 NWPtWm4zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mm\sTWM2OD1yLkCzN|E1KM7:TR?= NYDUWXVNW0GQR1XS
MDA-MB-175-VII M2H6cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkjyTWM2OD1yLkCzOFE3KM7:TR?= MWTTRW5ITVJ?
NCI-H2170 MorOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPaTWM2OD1yLkCzO|I5KM7:TR?= MlvOV2FPT0WU
BT-474 NXXCdm5jT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTBwMES5PFYh|ryP M1rPcnNCVkeHUh?=
EFO-27 MnvPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVrJR|UxRTBwMEWxPFIh|ryP MmLDV2FPT0WU
NCI-H720 NWT2cIhFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYHscHl[UUN3ME2wMlA2OzJ3IN88US=> MW\TRW5ITVJ?
PC-14 M1W5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TvcGlEPTB;MD6wOVY3QCEQvF2= MmLKV2FPT0WU
EC-GI-10 M{\nT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLhbIdJUUN3ME2wMlA2QTF{IN88US=> MnvOV2FPT0WU
KYSE-450 M1e2Xmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGT3bmVKSzVyPUCuNFU6PzhizszN NH\JbFdUSU6JRWK=
BPH-1 NHezZVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVjGUXBtUUN3ME2wMlA2QTh6IN88US=> NFS3R3RUSU6JRWK=
NCI-H292 M2nDXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlTXTWM2OD1yLkC2NFkh|ryP M4ryXXNCVkeHUh?=
H9 MkHuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHfHdmdKSzVyPUCuNFcyOzJizszN NFfQRoJUSU6JRWK=
NCI-H526 NUHFXpl1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MULJR|UxRTBwMEe4NlMh|ryP MnXIV2FPT0WU
NCI-H1623 MX7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1\LSmlEPTB;MD6wPFAzPSEQvF2= M{mxdXNCVkeHUh?=
KYSE-140 M{jpcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnvkTWM2OD1yLkC4N|Mh|ryP MkH2V2FPT0WU
Ca9-22 NYG3VYt{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{jwPWlEPTB;MD6wPFM2OyEQvF2= MYjTRW5ITVJ?
AU565 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXTJR|UxRTBwMEi1NFQh|ryP M2nCO3NCVkeHUh?=
ZR-75-30 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVXJR|UxRTBwMEm1OFUh|ryP M2HmN3NCVkeHUh?=
NCI-H1770 NIXGNmJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MW\JR|UxRTBwMUCyPEDPxE1? MnrEV2FPT0WU
LB2241-RCC NXX5bFlCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1K1dmlEPTB;MD6xNFg5PCEQvF2= MVnTRW5ITVJ?
CAL-39 M4jjN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEW5bmJKSzVyPUCuNVE4QTJizszN MUXTRW5ITVJ?
UACC-893 M3HQNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPSOI1LUUN3ME2wMlEyQDh3IN88US=> MonIV2FPT0WU
LU-65 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjPNGd3UUN3ME2wMlEzPjN|IN88US=> NWXTemNYW0GQR1XS
HN NFnPV3RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHBTWM2OD1yLkGzNFc4KM7:TR?= MnnPV2FPT0WU
TI-73 NFniOINIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3PqRWlEPTB;MD6xOFcyPSEQvF2= MnzpV2FPT0WU
KU812 NGfUeJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUfJR|UxRTBwMUW0OVYh|ryP M{[3RnNCVkeHUh?=
SW13 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFXYWnlKSzVyPUCuNVYzOTZizszN NHq4[G5USU6JRWK=
BB30-HNC NWK1[W9yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXr2OoVPUUN3ME2wMlE3PTd4IN88US=> MlXvV2FPT0WU
HSC-2 NIK0dIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXvJR|UxRTBwMU[4N|ch|ryP NX64SIhjW0GQR1XS
BV-173 NX7ofYxYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4O2RWlEPTB;MD6xO|U6PiEQvF2= M1HxOXNCVkeHUh?=
CAL-27 NUDwWJZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MY\JR|UxRTBwMUe2N|Yh|ryP NGHsO5hUSU6JRWK=
SBC-1 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1raPWlEPTB;MD6xPFk2QSEQvF2= MlPkV2FPT0WU
CAL-33 NV;zV4R[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXvJR|UxRTBwMkCxPFQh|ryP Mli2V2FPT0WU
NCI-H209 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX30OVZQUUN3ME2wMlIxPDZizszN M4rBUXNCVkeHUh?=
COR-L105 M2PuU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkXGTWM2OD1yLkKxNFg1KM7:TR?= MmDBV2FPT0WU
HSC-3 MknLS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIfZWo5KSzVyPUCuNlEyQThizszN M4\sSHNCVkeHUh?=
NCI-H69 M{W5R2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYfJR|UxRTBwMkG0OVEh|ryP MXHTRW5ITVJ?
MOLT-13 MkTKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3HWcWlEPTB;MD6yN|k4PSEQvF2= MVvTRW5ITVJ?
ML-2 MmWyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjObIlKSzVyPUCuNlQ5ODJizszN NHnydllUSU6JRWK=
IGROV-1 NGqw[JdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXnrVnFpUUN3ME2wMlI2QTV{IN88US=> M2nmfXNCVkeHUh?=
TK10 Mn\jS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mm\CTWM2OD1yLkK2O|M5KM7:TR?= NYO4b5RQW0GQR1XS
EoL-1-cell M{fJd2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPCTWM2OD1yLkK2PFkzKM7:TR?= MoToV2FPT0WU
HO-1-N-1 NVr3OGV[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1jmd2lEPTB;MD6yO|g2OyEQvF2= MkLFV2FPT0WU
BHY NWixd5JHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4Sx[mlEPTB;MD6yPFY2PSEQvF2= NWDBXJhCW0GQR1XS
LU-139 M3nOU2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTBwM{C1NUDPxE1? NYT3VnFlW0GQR1XS
23132-87 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwM{G5NlMh|ryP NIrhUHBUSU6JRWK=
ACHN MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPQcppKSzVyPUCuN|E6QTRizszN MXjTRW5ITVJ?
DoTc2-4510 NULKeo13T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF71T5lKSzVyPUCuN|IzOTlizszN MWPTRW5ITVJ?
BB65-RCC M{DzVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFzhdmRKSzVyPUCuN|Q2QTNizszN NGi5VmRUSU6JRWK=
HLE MnziS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4qyZWlEPTB;MD6zOVA1PiEQvF2= MWHTRW5ITVJ?
HCC1419 M3\wNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVTjWGVRUUN3ME2wMlM3PDB6IN88US=> M1HJZ3NCVkeHUh?=
A388 NYi2b5RYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{T5PGlEPTB;MD6zOlg2PyEQvF2= NHLocmdUSU6JRWK=
NUGC-3 NELmSFVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn\3TWM2OD1yLkO4N|c{KM7:TR?= NH3OdnpUSU6JRWK=
KYSE-180 MmSxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGm0cY1KSzVyPUCuN|kxQDlizszN NWTYWI5RW0GQR1XS
TE-6 NHv6dWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4nqfWlEPTB;MD60NFI1PiEQvF2= MmDUV2FPT0WU
A498 M4\uXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4XiVmlEPTB;MD60NFY4PCEQvF2= NVz6U3B5W0GQR1XS
NCI-H1648 NVXzPItjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2m1dmlEPTB;MD60OFE5OiEQvF2= NWXNSXpQW0GQR1XS
DU-145 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTBTGhKSzVyPUCuOFQ5OzNizszN MXTTRW5ITVJ?
CW-2 M3\pXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn3nTWM2OD1yLkS2PVE1KM7:TR?= NIniVnFUSU6JRWK=
A431 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2T3V2lEPTB;MD60PFI{OyEQvF2= NIHmRlJUSU6JRWK=
SAS M4m2T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mki4TWM2OD1yLkS4N|k5KM7:TR?= M2HkVXNCVkeHUh?=
NCI-H2126 M1PPUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGG4[HdKSzVyPUCuOVE6OjZizszN M3;LUnNCVkeHUh?=
NCI-H358 NYixNmcyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\XOWlEPTB;MD61N|IyKM7:TR?= NX;IboE1W0GQR1XS
FADU M3fxS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXrJR|UxRTBwNUS0NFQh|ryP NWf3WZFlW0GQR1XS
ACN NWPlbllDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHKTWM2OD1yLkW1NFk1KM7:TR?= NV;VbIpMW0GQR1XS
HCC70 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M33QeGlEPTB;MD61O|Y3OSEQvF2= NYHoSphNW0GQR1XS
NCI-H1838 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\vTWM2OD1yLk[wNlk6KM7:TR?= MVHTRW5ITVJ?
CAL-54 MlPsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTEcpFKSzVyPUCuOlE3OjFizszN NVzmW4syW0GQR1XS
NCI-H1975 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwNkG3Nlgh|ryP NEezNoJUSU6JRWK=
COR-L88 NEXzbXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV3hXJdCUUN3ME2wMlY1OTF|IN88US=> NV;EOWlEW0GQR1XS
CTV-1 NFjJN2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHrPWlNKSzVyPUCuOlQ{QTJizszN MnvUV2FPT0WU
EW-18 M{fnZWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{XubWlEPTB;MD62PFY6QCEQvF2= NH;yVJRUSU6JRWK=
HCC1806 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlfBTWM2OD1yLk[5OlY3KM7:TR?= M1nn[nNCVkeHUh?=
HuP-T4 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;wRo1KSzVyPUCuOlk4PiEQvF2= NEHpOI1USU6JRWK=
MDA-MB-361 NFrkVFRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2rPUWlEPTB;MD63NlY3OiEQvF2= Mn74V2FPT0WU
NCI-H1573 NWHXV2JnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVHJR|UxRTBwN{O2N{DPxE1? NX3JRmVFW0GQR1XS
KU-19-19 MkXhS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LlPGlEPTB;MD63O|Q3PCEQvF2= MmHrV2FPT0WU
COLO-678 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWDJR|UxRTBwOEC4N|Qh|ryP MmToV2FPT0WU
C-33-A MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DRZWlEPTB;MD64NVI6PyEQvF2= M2PEWXNCVkeHUh?=
Calu-3 MkDzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHScFlKSzVyPUCuPFE1OzRizszN MVTTRW5ITVJ?
AGS Mnf6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTBwOEO2OFgh|ryP MV3TRW5ITVJ?
SCC-25 Ml\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7wc2VKSzVyPUCuPFQyPzFizszN NXjlO5BzW0GQR1XS
JVM-2 NHL0VHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIPWRVlKSzVyPUCuPFgzQTlizszN MYLTRW5ITVJ?
HCE-T MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MU\JR|UxRTBwOEi0Nlgh|ryP M13DfnNCVkeHUh?=
ES4 NUPSOYRPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHYTWM2OD1yLkm3PFM3KM7:TR?= NYLvVYNyW0GQR1XS
EKVX M3XafGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37hfWlEPTB;MT6wNVA3PCEQvF2= NYSxfJlyW0GQR1XS
D-542MG NXjxXHl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIDwbVFKSzVyPUGuNFExPjRizszN NUS5bXpRW0GQR1XS
SW1116 MmjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX3JR|UxRTFwMEGyPFch|ryP NXToPJJsW0GQR1XS
5637 M{Haemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXfJR|UxRTFwMEG1NUDPxE1? NUXpRXREW0GQR1XS
HT-1376 MkTJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVXad5ZvUUN3ME2xMlAyPTF|IN88US=> NVTZXZlOW0GQR1XS
NB69 NYT4RYZrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml\MTWM2OD1zLkCyPVQ2KM7:TR?= NFTl[XVUSU6JRWK=
YKG-1 MnntS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF75Z3BKSzVyPUGuNFU1OTlizszN NHv5XHBUSU6JRWK=
EW-3 M132fGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFwMEe4PFMh|ryP MUjTRW5ITVJ?
GCIY MmriS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTFwMEixNFQh|ryP MnvQV2FPT0WU
SK-MES-1 NEXyUmlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVK0XVBqUUN3ME2xMlEyPDh5IN88US=> Ml7MV2FPT0WU
PANC-08-13 MlznS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NILSeHNKSzVyPUGuNVY1OTZizszN MUTTRW5ITVJ?
SK-NEP-1 M{\DV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4H0XmlEPTB;MT6xO|UyOyEQvF2= Mnj1V2FPT0WU
SW954 NELWfVRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmLITWM2OD1zLkKwNlE1KM7:TR?= MoDGV2FPT0WU
NCI-SNU-5 NE\n[IJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37zWGlEPTB;MT6yN|kh|ryP MnmyV2FPT0WU
SW48 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYTJR|UxRTFwMkW0N|Ih|ryP NEnlOlZUSU6JRWK=
HT-3 NHTE[2xIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4n3O2lEPTB;MT6yPFc2OyEQvF2= MoDxV2FPT0WU
ETK-1 M{f3Vmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPaTWM2OD1zLkO3OFU3KM7:TR?= NXu0UZRHW0GQR1XS
SCC-15 M{m1NWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1G4WGlEPTB;MT6zPVQ2OSEQvF2= NIT6dXhUSU6JRWK=
DU-4475 M3fDV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTFwNECxNlEh|ryP NX\CXFJQW0GQR1XS
NB5 M2HrNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkK2TWM2OD1zLkSxN|E4KM7:TR?= NYDuVFNbW0GQR1XS
CFPAC-1 NGe0V2lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIDheJZKSzVyPUGuOFI1QTNizszN NUXEdot2W0GQR1XS
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NCI-H727 MlG4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nCZmlEPTB;OD6xNFQzKM7:TR?= M2LFO3NCVkeHUh?=
SW1710 NFL5fWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonDTWM2OD16LkG4OVE2KM7:TR?= NXi4SFh2W0GQR1XS
D-502MG M1nNN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjmTWM2OD16LkK5NlgzKM7:TR?= MW\TRW5ITVJ?
NCI-H1993 NFXkV2VIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRThwM{O2N|Eh|ryP NV76fmRwW0GQR1XS
SCC-4 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmTHTWM2OD16LkS0NFU6KM7:TR?= MVjTRW5ITVJ?
HAL-01 MkLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLncpk1UUN3ME24MlUyQTFizszN M4jxenNCVkeHUh?=
GT3TKB M3O3eGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUPqfJIyUUN3ME24MlY4QTZ2IN88US=> Mn[0V2FPT0WU
SK-OV-3 NV\0d3NUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NET1TlBKSzVyPUiuO|E{OjlizszN NFPEdHBUSU6JRWK=
COLO-829 M4LrW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkG4TWM2OD16LkiwPVc3KM7:TR?= M33XTHNCVkeHUh?=
OCI-AML2 NGHVV|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn;aTWM2OD16Lkm1OFgyKM7:TR?= M4jwNXNCVkeHUh?=
OS-RC-2 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NILQUpNKSzVyPUmuNFIyQSEQvF2= MWrTRW5ITVJ?
BFTC-909 M1n4fmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MV3JR|UxRTlwME[3PVkh|ryP NEDJ[4lUSU6JRWK=
EW-11 M3vO[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3EfFhKSzVyPUmuNVc3PTNizszN M3H6eXNCVkeHUh?=
HCE-4 Mm\hS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NITaTHRKSzVyPUmuNlE2PThizszN NHK1e2hUSU6JRWK=
BALL-1 NV;LPJZDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWSzOXdiUUN3ME25MlIyQTB5IN88US=> M3ziUXNCVkeHUh?=
SF539 NEDINWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYf0R4tVUUN3ME25MlI{PTZ{IN88US=> NFe5[llUSU6JRWK=
CAMA-1 MkD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmT3TWM2OD17LkK4NVI5KM7:TR?= MoT4V2FPT0WU
C32 M2G4N2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGnXPHZKSzVyPUmuN|MxPjRizszN M4izWnNCVkeHUh?=
NCI-H1703 NF:4XItIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXnJR|UxRTlwM{SzO|Uh|ryP NYfpdI1qW0GQR1XS
NCI-H1650 NX\GUGVlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTlwNkC5OFYh|ryP NG[1SlJUSU6JRWK=
NCI-H1563 Mn;PS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHwTWM2OD17Lke2NFMyKM7:TR?= M2LPcHNCVkeHUh?=
CAL-85-1 M331V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NH24V5JKSzVyPUmuPFc{QDNizszN MVXTRW5ITVJ?
UM-UC-3 M1LDRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWTJR|UxRTlwOUWwN{DPxE1? NGrI[mxUSU6JRWK=
BxPC-3 NHzFS4dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmXITWM2OD1zMD6wPVczKM7:TR?= M4Pje3NCVkeHUh?=
MHH-PREB-1 NIS0fZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1TJdGlEPTB;MUCuNVk6QSEQvF2= NHLr[FNUSU6JRWK=
DEL MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkPrTWM2OD1zMD6zPVQ3KM7:TR?= NFXWSGpUSU6JRWK=
HuCCT1 M{D5c2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoXFTWM2OD1zMD62NFM{KM7:TR?= MonHV2FPT0WU
OVCAR-4 Mnv6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnvnTWM2OD1zMD64PFM2KM7:TR?= NH;xbY5USU6JRWK=
CAL-72 NVrJUJBnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTFyLkmzPVEh|ryP M2HSWHNCVkeHUh?=
HCC1954 MkTsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MX;JR|UxRTFzLkC3OVQh|ryP NIT2[XNUSU6JRWK=
EFO-21 NH\PNnVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnFbXJKSzVyPUGxMlExPDVizszN M4SzenNCVkeHUh?=
FTC-133 NEjXUXNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWnYXWN5UUN3ME2xNU4yPDB5IN88US=> NEmyOXNUSU6JRWK=
SK-MEL-24 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fCXmlEPTB;MUGuNlM3PiEQvF2= NEPoT4RUSU6JRWK=
UACC-62 M{\pSmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXXSZXFlUUN3ME2xNU4zOzZ6IN88US=> NXixNJVIW0GQR1XS
NCI-H650 M2G4S2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MofHTWM2OD1zMT6yOFE5KM7:TR?= M1fsZ3NCVkeHUh?=
ALL-PO MlztS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXO4R5F{UUN3ME2xNU4zPTF{IN88US=> MofpV2FPT0WU
T84 NYHWc3ZST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGfmWItKSzVyPUGxMlM6ODdizszN NI\zbnZUSU6JRWK=
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SW626 Mk\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NE[4OWhKSzVyPUGxMlU4PTVizszN NEjJNohUSU6JRWK=
RPMI-2650 NHrzOVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPRTWM2OD1zMT61PFg2KM7:TR?= M3zYRnNCVkeHUh?=
MC-IXC M{LrTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkTmTWM2OD1zMT62O|I5KM7:TR?= MYXTRW5ITVJ?
HOP-62 NWXNT|ljT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\YZXY{UUN3ME2xNU43PzZ2IN88US=> NH72b|FUSU6JRWK=
NOS-1 NWWybmlIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVvJR|UxRTFzLkexNFkh|ryP M13wUXNCVkeHUh?=
SW1573 M{TxSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTFzLkeyPVUh|ryP MoXaV2FPT0WU
WM-115 M4WyN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTFzLke1PFgh|ryP MYrTRW5ITVJ?
HuO9 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlO4TWM2OD1zMT64O|c1KM7:TR?= NFXJZ3pUSU6JRWK=
YAPC MnfpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmrBTWM2OD1zMT65NlU6KM7:TR?= NI\kVWVUSU6JRWK=
MDA-MB-453 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml6zTWM2OD1zMT65OVE2KM7:TR?= MYPTRW5ITVJ?
NCI-H596 MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7HTWM2OD1zMj6wN|Y6KM7:TR?= NUDRNlM{W0GQR1XS
A172 MmfOS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH7zTWNKSzVyPUGyMlA4QThizszN NH3o[ldUSU6JRWK=
RS4-11 M2PsdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmLiTWM2OD1zMj6xO|I2KM7:TR?= NX30W5A3W0GQR1XS
HCC1937 NHHBd4tIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX\JR|UxRTF{Lke1OlQh|ryP M1XybXNCVkeHUh?=
SW837 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3ib|RXUUN3ME2xNk46ODJ6IN88US=> MkD4V2FPT0WU
NMC-G1 NFPV[2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoDlTWM2OD1zMj65NlM1KM7:TR?= M2\VV3NCVkeHUh?=
PFSK-1 NIjYWmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVXJR|UxRTF|LkC2JO69VQ>? NUK3ZXU3W0GQR1XS
DBTRG-05MG NXyyTnBPT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTUTWM2OD1zMz6wOlMzKM7:TR?= MnzyV2FPT0WU
SK-UT-1 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXvJR|UxRTF|LkGwPFMh|ryP NWTJR4Q2W0GQR1XS
OVCAR-5 NU\GWZFDT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkX6TWM2OD1zMz6xOVk{KM7:TR?= NFn3dHlUSU6JRWK=
8505C NULkXIhjT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXP3fVdpUUN3ME2xN{4zODZ5IN88US=> MlP0V2FPT0WU
SK-MEL-1 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTF|LkexN|Uh|ryP NWTp[WN4W0GQR1XS
LK-2 Mn36S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVXJR|UxRTF|Lke2N|kh|ryP NFTSeYtUSU6JRWK=
OE33 MnzPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWfN[YVCUUN3ME2xN{44QDZizszN M{LMVXNCVkeHUh?=
Ramos-2G6-4C10 NUizVldtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEXhSYNKSzVyPUG0MlAzODJizszN MoDDV2FPT0WU
EW-13 NF;PSZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1jyS2lEPTB;MUSuNFM2OiEQvF2= NYm5Wo5RW0GQR1XS
NCI-H1793 MkD6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTF2LkKwPFch|ryP Ml6yV2FPT0WU
BHT-101 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWm5fXJrUUN3ME2xOE4zPDFizszN Mn;WV2FPT0WU
RKO MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmfoTWM2OD1zND61NFc2KM7:TR?= NU\6[oJWW0GQR1XS
NEC8 NELNU2hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoPmTWM2OD1zND61OFczKM7:TR?= MnnyV2FPT0WU
PANC-10-05 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoG0TWM2OD1zND62NlQ4KM7:TR?= M2GzUnNCVkeHUh?=
NCI-H2030 NHzX[4ZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkDGTWM2OD1zND62OFQ5KM7:TR?= MmPEV2FPT0WU
C2BBe1 NV;QR5hsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnTTWM2OD1zND63OlQh|ryP MoDmV2FPT0WU
EM-2 MkC3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUjJR|UxRTF2Lki1O|Yh|ryP MnrQV2FPT0WU
HCC1395 NUTSdo1sT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvWTnpRUUN3ME2xOE46OzN6IN88US=> M2rHfHNCVkeHUh?=
A2058 NYjTVY5ET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIi2UIFKSzVyPUG1MlA1ODlizszN MVzTRW5ITVJ?
SW1463 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXTLToVlUUN3ME2xOU4xPDh3IN88US=> NUjyVWFLW0GQR1XS
J82 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF3OVJlKSzVyPUG1MlA2PyEQvF2= MWDTRW5ITVJ?
CAL-120 MkXuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEHjVYRKSzVyPUG1MlE1PDdizszN NFzMV4ZUSU6JRWK=
COLO-824 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mon1TWM2OD1zNT6xOVc6KM7:TR?= NV;vO|Y2W0GQR1XS
LNCaP-Clone-FGC M1HZZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXLJR|UxRTF3LkSyOFgh|ryP NELMNZNUSU6JRWK=
CP66-MEL NETBbmFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2LaXGlEPTB;MUWuOFY5QCEQvF2= MXjTRW5ITVJ?
OC-314 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkTGTWM2OD1zNT60O|E1KM7:TR?= MmLLV2FPT0WU
OVCAR-8 MlH5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlLhTWM2OD1zNT64PFYyKM7:TR?= NXK1fldoW0GQR1XS
MFE-280 M3H2[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXteGtzUUN3ME2xOk4xPDh6IN88US=> M2DOdHNCVkeHUh?=
MHH-NB-11 NI\hXFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFzmRpRKSzVyPUG2MlA5OzlizszN M{nXZ3NCVkeHUh?=
SW1990 MkP3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV\JR|UxRTF4LkG3OVUh|ryP NVPodVNoW0GQR1XS
U-266 M3\NXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUmwU2V[UUN3ME2xOk4zOjl7IN88US=> MYTTRW5ITVJ?
MFM-223 MorlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MULJR|UxRTF4LkO5OlUh|ryP Mor0V2FPT0WU
L-363 MnzrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPmTWM2OD1zNj60OVc4KM7:TR?= M1vDT3NCVkeHUh?=
MCF7 NWS3SVhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH3Z[ZNKSzVyPUG2MlQ4OjNizszN MlOwV2FPT0WU
SK-MEL-3 NFTXNGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPXTWM2OD1zNj60O|g4KM7:TR?= MX3TRW5ITVJ?
HH NV\oUJlUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVPDXph5UUN3ME2xOk42OTZ{IN88US=> NGLrOXdUSU6JRWK=
no-10 NXjRWVhvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUfJR|UxRTF4Lk[zOFMh|ryP NG\ZTIFUSU6JRWK=
HuP-T3 NHu4enJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYP3VZRCUUN3ME2xOk43PTd4IN88US=> M{XS[XNCVkeHUh?=
QIMR-WIL NWrWW41GT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVLJR|UxRTF4LkexNFUh|ryP NF;wVI5USU6JRWK=
NCI-H1092 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{e1TmlEPTB;MU[uPFMyPiEQvF2= NY\BZ4pxW0GQR1XS
MZ2-MEL M2joVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPE[VNXUUN3ME2xOk45PDB|IN88US=> Ml3zV2FPT0WU
ES3 MmTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoDzTWM2OD1zNj65NVM1KM7:TR?= MkPQV2FPT0WU
COLO-684 NU\FNVdFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUTJR|UxRTF4Lkm0O|ch|ryP MoXYV2FPT0WU
NCI-H661 NVXOeXRET3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXfnPVA3UUN3ME2xOk46Pjl2IN88US=> Mnn6V2FPT0WU
CP50-MEL-B MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWrJR|UxRTF5LkCzOFMh|ryP M1XOWnNCVkeHUh?=
NCI-H2405 NFTYSHNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{\YW2lEPTB;MUeuNVk4PCEQvF2= NG\MWWpUSU6JRWK=
U-2-OS MoHmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2DDb2lEPTB;MUeuOVMxPyEQvF2= M1PmV3NCVkeHUh?=
RERF-LC-MS NXTrem9yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NILFSXNKSzVyPUG3MlU2ODhizszN M3\BVXNCVkeHUh?=
NCI-H2342 M4\3eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NG[1OodKSzVyPUG3MlU2PyEQvF2= NXjkSYR4W0GQR1XS
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MOLT-16 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnfNTWM2OD1zNz64PVM1KM7:TR?= MkS0V2FPT0WU
RH-18 MnjWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYrJR|UxRTF6LkCwN|Uh|ryP M2HTe3NCVkeHUh?=
D-283MED NHPYe5JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1rsPGlEPTB;MUiuNFA5QCEQvF2= NYPG[4pVW0GQR1XS
RCC10RGB M2jWTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUnHbYtzUUN3ME2xPE4xPTV7IN88US=> NEDI[4lUSU6JRWK=
NCI-H1437 M{TZXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{Pje2lEPTB;MUiuNVY1OSEQvF2= MV7TRW5ITVJ?
SW982 NInPbXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoXyTWM2OD1zOD6yOlcyKM7:TR?= NYizS2lJW0GQR1XS
IST-MES1 NHPjd5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUTMTIJ2UUN3ME2xPE41PDJ6IN88US=> NYXGfpdoW0GQR1XS
A704 M4T2b2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX\JR|UxRTF6LkS3OVMh|ryP NYHxcXFLW0GQR1XS
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SCH MoHkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYSzdY93UUN3ME2xPE43PDV4IN88US=> NH;1fWpUSU6JRWK=
COLO-320-HSR NEfGfXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVfJR|UxRTF6Lke0OkDPxE1? NF3oRWZUSU6JRWK=
Mo-T NEfSSG9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoWxTWM2OD1zOD64NlA1KM7:TR?= MlvHV2FPT0WU
Saos-2 MnnTS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPlVYlKSzVyPUG5MlEyPjJizszN NXe2Z|UxW0GQR1XS
SW684 NUK5cG1MT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1Xnb2lEPTB;MUmuNVMzPiEQvF2= NX3RXoNzW0GQR1XS
KMOE-2 NXThTIhrT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTF7LkKyOFIh|ryP NHHUbJVUSU6JRWK=
MMAC-SF M2DaRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1jqNWlEPTB;MUmuNlYxPyEQvF2= NWfDNIJJW0GQR1XS
JAR MoHxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXLYSmYyUUN3ME2xPU4zQTlizszN NF3CUGRUSU6JRWK=
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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 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 (37)

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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