Afatinib (BIBW2992)

Catalog No.S1011

Afatinib (BIBW2992) Chemical Structure

Molecular Weight(MW): 485.94

Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively.

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In DMSO USD 240 In stock
USD 120 In stock
USD 210 In stock
USD 570 In stock
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Cited by 37 Publications

4 Customer Reviews

  • Cytoxicity of irreversible EGFR TKIS and ethacrynic acid on breast cells lines. A, Mean IC50 value of Afatinib.

    Oncotarget, 2016, 7(36):58038-58050. Afatinib (BIBW2992) purchased from Selleck.

    Inhibition of signaling pathway activation in lung tumor cell lines by kinase inhibitors. Lung tumor cells were cultured in 10% FBS until reaching ∼80% confluence and then the cells were starved in serum-free medium for overnight, followed by 4-hour treatment with the inhibitors. Cell lysates were then prepared and used for determination of the pathway activation signals by the CEER assay.

    Int J Proteomics 2011 2011, 215496. Afatinib (BIBW2992) purchased from Selleck.

  • Inhibition of anchorage-independent growth of lung tumor cell lines by selected inhibitors. Each selected cell line was treated with the indicated inhibitor at 0.1 μM and 1 μM concentrations for two weeks and cell colony size formation was scored under the Nikon inverted-phase microscope.

    Int J Proteomics 2011 2011, 215496. Afatinib (BIBW2992) purchased from Selleck.

    After starved in serum-free medium for 24h, Breast cancer cells incubated with the indicated concentrations of BIBW2992 for 3h,followed by 15-minute stimolation of 100ng/ml EGF

    Dr. Zhang of Tianjin Medical University. Afatinib (BIBW2992) purchased from Selleck.

Purity & Quality Control

Choose Selective EGFR Inhibitors

Biological Activity

Description Afatinib (BIBW2992) inhibits EGFR/ErbB irreversibly in vitro with IC50 of 0.5, 0.4, 10, 14, 1 nM for EGFRwt, EGFR L858R , EGFR L858R/T790M ErbB2 (HER2) and ErbB4 (HER4), respectively.
Targets
EGFR (L858R) [1]
(Cell-free assay)
EGFR (wt) [1]
(Cell-free assay)
ErbB4 [2]
(Cell-free assay)
EGFR (L858R/T790M) [1]
(Cell-free assay)
HER2 [1]
(Cell-free assay)
0.4 nM 0.5 nM 1 nM 10 nM 14 nM
In vitro

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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HDLM-2 NIX0cW1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkHITWM2OD1yLkCwOVczKM7:TR?= NWrxU3c1W0GQR1XS
KASUMI-1 Ml;ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NECwTmRKSzVyPUCuNFA6OTFizszN NV;wN4pUW0GQR1XS
HCC2218 NE\oS2JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MonVTWM2OD1yLkCwPVg4KM7:TR?= NUfpS|h2W0GQR1XS
KARPAS-45 NXfJboNCT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HOdWlEPTB;MD6wNVY4OSEQvF2= M1y5SHNCVkeHUh?=
HSC-4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jtd2lEPTB;MD6wNVc1QCEQvF2= M2DJW3NCVkeHUh?=
CHL-1 MoHJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoHkTWM2OD1yLkCxPFM6KM7:TR?= M3j4O3NCVkeHUh?=
KY821 MmfIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPMUlJKSzVyPUCuNFIxPiEQvF2= MnrSV2FPT0WU
NCI-N87 NFPCeZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVPWfVNPUUN3ME2wMlAzPzd|IN88US=> M2n6cnNCVkeHUh?=
DOK NILBZ4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlHKTWM2OD1yLkCzNVk1KM7:TR?= NEDDeWdUSU6JRWK=
DSH1 NWj4[oxyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFnLVHVKSzVyPUCuNFM{OTRizszN NFXX[XlUSU6JRWK=
MDA-MB-175-VII MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUnJR|UxRTBwMEO0NVYh|ryP MlvmV2FPT0WU
NCI-H2170 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDCfYdDUUN3ME2wMlA{PzJ6IN88US=> NWmzb4hOW0GQR1XS
BT-474 Mo\uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXTDZ4FvUUN3ME2wMlA1QTh4IN88US=> M2H1SXNCVkeHUh?=
EFO-27 NVj2O|RwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\uZpJKSzVyPUCuNFUyQDJizszN MmjWV2FPT0WU
NCI-H720 M336cmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUXJR|UxRTBwMEWzNlUh|ryP M2jBXXNCVkeHUh?=
PC-14 NV;DdohLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlG0TWM2OD1yLkC1OlY5KM7:TR?= MV\TRW5ITVJ?
EC-GI-10 NVXMN4xuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwMEW5NVIh|ryP NVXQTWJWW0GQR1XS
KYSE-450 NFvSVWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmTzTWM2OD1yLkC1PVc5KM7:TR?= MXTTRW5ITVJ?
BPH-1 NIPJeopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELUfYVKSzVyPUCuNFU6QDhizszN MV7TRW5ITVJ?
NCI-H292 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEnpVpdKSzVyPUCuNFYxQSEQvF2= NG\JVmNUSU6JRWK=
H9 NXv6U49mT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEPjSnRKSzVyPUCuNFcyOzJizszN MmLaV2FPT0WU
NCI-H526 NV;4doFvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2PBfWlEPTB;MD6wO|gzOyEQvF2= M2nrcXNCVkeHUh?=
NCI-H1623 NH\jSlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUjNfYh6UUN3ME2wMlA5ODJ3IN88US=> NGXOUG5USU6JRWK=
KYSE-140 MljVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUPJR|UxRTBwMEizN{DPxE1? MnPIV2FPT0WU
Ca9-22 NFriZXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV;JR|UxRTBwMEizOVMh|ryP MVXTRW5ITVJ?
AU565 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWnJR|UxRTBwMEi1NFQh|ryP Mk\oV2FPT0WU
ZR-75-30 NHq2bWpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGToOZlKSzVyPUCuNFk2PDVizszN NIq5TWpUSU6JRWK=
NCI-H1770 M1XN[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2C3OWlEPTB;MD6xNFI5KM7:TR?= MlzoV2FPT0WU
LB2241-RCC NUPne4lyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmjnTWM2OD1yLkGwPFg1KM7:TR?= NVu2XnY6W0GQR1XS
CAL-39 Ml3KS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3TW5J7UUN3ME2wMlEyPzl{IN88US=> M1v0NHNCVkeHUh?=
UACC-893 M1\iO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4fL[2lEPTB;MD6xNVg5PSEQvF2= M364WHNCVkeHUh?=
LU-65 NV\yZYh2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIH5WZJKSzVyPUCuNVI3OzNizszN NF;VcpZUSU6JRWK=
HN M17E[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGHSUFVKSzVyPUCuNVMxPzdizszN MlzkV2FPT0WU
TI-73 MnezS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWHSUo5mUUN3ME2wMlE1PzF3IN88US=> NFyzZ4RUSU6JRWK=
KU812 MVTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV3JR|UxRTBwMUW0OVYh|ryP Mo\sV2FPT0WU
SW13 M17J[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIe0T45KSzVyPUCuNVYzOTZizszN M4LtO3NCVkeHUh?=
BB30-HNC NWf6XXdGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWrJR|UxRTBwMU[1O|Yh|ryP NHf0fnpUSU6JRWK=
HSC-2 M2LwdWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVvJR|UxRTBwMU[4N|ch|ryP MnHMV2FPT0WU
BV-173 M2\4T2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIW2W4xKSzVyPUCuNVc2QTZizszN MW\TRW5ITVJ?
CAL-27 NUHuTodQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVzTSZVVUUN3ME2wMlE4PjN4IN88US=> M4rEOHNCVkeHUh?=
SBC-1 NUX3fJBYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYPJR|UxRTBwMUi5OVkh|ryP M2TXSHNCVkeHUh?=
CAL-33 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnxeGxKSzVyPUCuNlAyQDRizszN NFHmd4lUSU6JRWK=
NCI-H209 NXLVSnlST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYjJR|UxRTBwMkC0OkDPxE1? M1\VbXNCVkeHUh?=
COR-L105 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV\ISppYUUN3ME2wMlIyODh2IN88US=> Mk\PV2FPT0WU
HSC-3 NVjMTIxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGDLbnFKSzVyPUCuNlEyQThizszN NUfvNZJCW0GQR1XS
NCI-H69 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXzJR|UxRTBwMkG0OVEh|ryP MWjTRW5ITVJ?
MOLT-13 NXPYTo9ZT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkKyTWM2OD1yLkKzPVc2KM7:TR?= M{TLXHNCVkeHUh?=
ML-2 M3XWT2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoPTTWM2OD1yLkK0PFAzKM7:TR?= M{S5RnNCVkeHUh?=
IGROV-1 MkPpS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LYUWlEPTB;MD6yOVk2OiEQvF2= MUHTRW5ITVJ?
TK10 MmrCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3LtUGlEPTB;MD6yOlc{QCEQvF2= NYPOOnpwW0GQR1XS
EoL-1-cell M4m2OGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVrJR|UxRTBwMk[4PVIh|ryP MWLTRW5ITVJ?
HO-1-N-1 M4fPPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2XXUWlEPTB;MD6yO|g2OyEQvF2= NG\XWYpUSU6JRWK=
BHY MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEjoU3NKSzVyPUCuNlg3PTVizszN MYPTRW5ITVJ?
LU-139 NILMWIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWXjOI5OUUN3ME2wMlMxPTFizszN MXTTRW5ITVJ?
23132-87 MnG3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3:xcmlEPTB;MD6zNVkzOyEQvF2= Mk\HV2FPT0WU
ACHN NYnqU3JUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NW\xV3hKUUN3ME2wMlMyQTl2IN88US=> M4fn[3NCVkeHUh?=
DoTc2-4510 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX;JR|UxRTBwM{KyNVkh|ryP M{C4T3NCVkeHUh?=
BB65-RCC NGH6WIJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGDsU|dKSzVyPUCuN|Q2QTNizszN NUXLZWlsW0GQR1XS
HLE NXvJbWRlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn7tTWM2OD1yLkO1NFQ3KM7:TR?= M1HIRXNCVkeHUh?=
HCC1419 NWDWNndmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MljyTWM2OD1yLkO2OFA5KM7:TR?= NFLZUGFUSU6JRWK=
A388 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NG\L[GNKSzVyPUCuN|Y5PTdizszN MXHTRW5ITVJ?
NUGC-3 M2e0WWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwM{izO|Mh|ryP NUmwTmZ{W0GQR1XS
KYSE-180 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTBwM{mwPFkh|ryP MnnyV2FPT0WU
TE-6 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTBwNECyOFYh|ryP NVjBS4lSW0GQR1XS
A498 NXnGfI56T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFHE[HdKSzVyPUCuOFA3PzRizszN NFv1N4NUSU6JRWK=
NCI-H1648 M3GzO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGX2[IhKSzVyPUCuOFQyQDJizszN MmmwV2FPT0WU
DU-145 MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnryTWM2OD1yLkS0PFM{KM7:TR?= NHLZXGhUSU6JRWK=
CW-2 M4HyeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGXUUYFKSzVyPUCuOFY6OTRizszN NIDjPHpUSU6JRWK=
A431 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFy4W5VKSzVyPUCuOFgzOzNizszN NY\5TXMzW0GQR1XS
SAS NVW5VFRUT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHmTWM2OD1yLkS4N|k5KM7:TR?= M4HuTnNCVkeHUh?=
NCI-H2126 M4D3[Wdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXfyOIM{UUN3ME2wMlUyQTJ4IN88US=> MnznV2FPT0WU
NCI-H358 Mle3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\j[mlEPTB;MD61N|IyKM7:TR?= NIPJZlhUSU6JRWK=
FADU NFTlZ3hIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn7TTWM2OD1yLkW0OFA1KM7:TR?= NGXtXnpUSU6JRWK=
ACN MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUTKbGRxUUN3ME2wMlU2ODl2IN88US=> NHPre2pUSU6JRWK=
HCC70 MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn3CTWM2OD1yLkW3OlYyKM7:TR?= M2PQdXNCVkeHUh?=
NCI-H1838 NVvjUYQ6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnzvTWM2OD1yLk[wNlk6KM7:TR?= NVTkb4ZTW0GQR1XS
CAL-54 MlzjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M13odmlEPTB;MD62NVYzOSEQvF2= MUfTRW5ITVJ?
NCI-H1975 M{iw[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{HiWWlEPTB;MD62NVczQCEQvF2= MYLTRW5ITVJ?
COR-L88 MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTNPXpOUUN3ME2wMlY1OTF|IN88US=> NF3VdZRUSU6JRWK=
CTV-1 NXXESXgxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGXKOpBKSzVyPUCuOlQ{QTJizszN NH\pOlRUSU6JRWK=
EW-18 MmLDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVnJR|UxRTBwNki2PVgh|ryP NFK5d4JUSU6JRWK=
HCC1806 M3;vW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NVPndZFDUUN3ME2wMlY6PjZ4IN88US=> MmfOV2FPT0WU
HuP-T4 MmjsS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2TDPWlEPTB;MD62PVc3KM7:TR?= M2\x[nNCVkeHUh?=
MDA-MB-361 M1rNOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXLFUIMyUUN3ME2wMlczPjZ{IN88US=> NUjoN3lkW0GQR1XS
NCI-H1573 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWXJR|UxRTBwN{O2N{DPxE1? NVvpNWNPW0GQR1XS
KU-19-19 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHLYOphKSzVyPUCuO|c1PjRizszN NXXKUIk3W0GQR1XS
COLO-678 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPPc2RKSzVyPUCuPFA5OzRizszN Mk\uV2FPT0WU
C-33-A M3vMV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkPKTWM2OD1yLkixNlk4KM7:TR?= NFvjcHRUSU6JRWK=
Calu-3 NXPqcnB7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Pq[mlEPTB;MD64NVQ{PCEQvF2= M3\EU3NCVkeHUh?=
AGS NYXRbmFVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NF[zfVVKSzVyPUCuPFM3PDhizszN NI\U[VRUSU6JRWK=
SCC-25 MlLPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGDDd2dKSzVyPUCuPFQyPzFizszN NXHheVlEW0GQR1XS
JVM-2 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmnxTWM2OD1yLki4Nlk6KM7:TR?= MWDTRW5ITVJ?
HCE-T NYLrSo9zT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTBwOEi0Nlgh|ryP MWnTRW5ITVJ?
ES4 MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU\JR|UxRTBwOUe4N|Yh|ryP MXvTRW5ITVJ?
EKVX NFPYZndIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NELhc4NKSzVyPUGuNFExPjRizszN M33RWXNCVkeHUh?=
D-542MG MnO5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mki1TWM2OD1zLkCxNFY1KM7:TR?= MVHTRW5ITVJ?
SW1116 NVX0Rpl5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmXaTWM2OD1zLkCxNlg4KM7:TR?= NWD5TYY5W0GQR1XS
5637 NIHSW|BIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXzHZ4p5UUN3ME2xMlAyPTFizszN M1\1fXNCVkeHUh?=
HT-1376 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGS0cHRKSzVyPUGuNFE2OTNizszN MYPTRW5ITVJ?
NB69 Mlr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NG\3eolKSzVyPUGuNFI6PDVizszN MlXtV2FPT0WU
YKG-1 NGnp[ZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGLoOVFKSzVyPUGuNFU1OTlizszN M4L4c3NCVkeHUh?=
EW-3 NGL0VIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWTJR|UxRTFwMEe4PFMh|ryP NF;yOYpUSU6JRWK=
GCIY MmW5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWrJR|UxRTFwMEixNFQh|ryP Ml\zV2FPT0WU
SK-MES-1 NYLveFVmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHy2NodKSzVyPUGuNVE1QDdizszN M2D1bnNCVkeHUh?=
PANC-08-13 M{Di[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3rl[mlEPTB;MT6xOlQyPiEQvF2= NV23eWk6W0GQR1XS
SK-NEP-1 NFe2RWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXvYeoZTUUN3ME2xMlE4PTF|IN88US=> NFTJeI1USU6JRWK=
SW954 M13uWWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MnPMTWM2OD1zLkKwNlE1KM7:TR?= NY\sfmtMW0GQR1XS
NCI-SNU-5 NIC1OFlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnYNW9KSzVyPUGuNlM6KM7:TR?= MoCwV2FPT0WU
SW48 M1zWOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWn1ZlZxUUN3ME2xMlI2PDN{IN88US=> MlzGV2FPT0WU
HT-3 M2PhTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{TucGlEPTB;MT6yPFc2OyEQvF2= MVrTRW5ITVJ?
ETK-1 M4PVZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPjU4lKSzVyPUGuN|c1PTZizszN NW\WSVVVW0GQR1XS
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OVCAR-8 M{ixUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV\VTWJYUUN3ME2xOU45QDZzIN88US=> NIq2NJFUSU6JRWK=
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GCT NFP4e3JIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPQRY5KSzVyPUKwMlMxOjZizszN NIDuTG1USU6JRWK=
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Becker MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M37DT2lEPTB;MkCuO|IxOSEQvF2= M3LNU3NCVkeHUh?=
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CHP-212 Mom0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXnuToVTUUN3ME2yNk4{OjJ{IN88US=> NX;ZOVVTW0GQR1XS
KM12 NIj4dYJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4H0VWlEPTB;MkKuN|U3KM7:TR?= MV\TRW5ITVJ?
JEG-3 M3fHUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3TyN2lEPTB;MkKuN|c5KM7:TR?= NVrZNmJyW0GQR1XS
LN-405 MmLnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJ{LkW5NVMh|ryP NF3oPGJUSU6JRWK=
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GI-1 NF3QZZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3jOemlEPTB;MkKuO|Y2QCEQvF2= MnnzV2FPT0WU
RT-112 NVy1VYgyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoXPTWM2OD1{Mj64OlE3KM7:TR?= MlXNV2FPT0WU
MPP-89 MmL5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX3XRlNGUUN3ME2yNk45PjZzIN88US=> MWTTRW5ITVJ?
A3-KAW M3ridGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDLUFhzUUN3ME2yN{4yODB|IN88US=> M{\USXNCVkeHUh?=
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KG-1 MmXjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NX7FUnNiUUN3ME2yOE4yQTJ6IN88US=> MnzaV2FPT0WU
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COLO-792 NIjzeo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NUPzdVN3UUN3ME2yOU4zPzN{IN88US=> Mly2V2FPT0WU
NB12 NVTCd5dbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1HTcWlEPTB;MkWuNlk1PyEQvF2= M3;UTnNCVkeHUh?=
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SW780 NUXGSWc{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYfO[49LUUN3ME2yOU4{OjZ2IN88US=> MnryV2FPT0WU
GB-1 Mnj5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYHJR|UxRTJ3LkSwOlkh|ryP M1HzTHNCVkeHUh?=
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KE-37 Ml3mS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlfsTWM2OD1{NT63N|E2KM7:TR?= M3rjeXNCVkeHUh?=
CCRF-CEM M1[ydGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTJ3Lkm2O{DPxE1? NIHNXWhUSU6JRWK=
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EGI-1 NITsfYpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYTPcmtbUUN3ME2yPE42QTJ6IN88US=> NE\PeYpUSU6JRWK=
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MIA-PaCa-2 NUD1[XB7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnTWTWM2OD1{OD63PVU6KM7:TR?= NUfQPFd7W0GQR1XS
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BFTC-905 NFG4fphIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVzJR|UxRTJ7LkK3NFUh|ryP MVjTRW5ITVJ?
NCI-H1581 MnjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPtZZRKSzVyPUK5MlMyPDVizszN NEjYdnBUSU6JRWK=
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SF268 MkXSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV7kfHlZUUN3ME2yPU42QTNzIN88US=> M4f0fnNCVkeHUh?=
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D-566MG M{WzNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTJ7LkmzPVMh|ryP NHXzUllUSU6JRWK=
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D-336MG M2fUbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2LRR2lEPTB;M{CuNlg6OiEQvF2= MmPvV2FPT0WU
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Calu-6 MX\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVzJR|UxRTNyLkK5OlMh|ryP NFXPd2VUSU6JRWK=
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DK-MG Moj3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXTJR|UxRTNyLkW0OVYh|ryP NV7rO|JsW0GQR1XS
SK-HEP-1 NFruT|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGjycGJKSzVyPUOwMlY{OjZizszN MW\TRW5ITVJ?
MS-1 NHXHfZFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmPhTWM2OD1|MD64PFg6KM7:TR?= MVHTRW5ITVJ?
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NB17 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MULJR|UxRTNzLkWxPFUh|ryP NYDWOVF{W0GQR1XS
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CAL-51 NFr5No1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\Ge4FpUUN3ME2zNU42PjZ5IN88US=> NITlTY1USU6JRWK=
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GOTO NV\jTXE6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M133RWlEPTB;M{GuPFUxPiEQvF2= Ml32V2FPT0WU
ChaGo-K-1 M2riOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIDCPZdKSzVyPUOyMlAxPyEQvF2= MYXTRW5ITVJ?
RO82-W-1 NEDTNXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NX\jW2FEUUN3ME2zNk4yPjB2IN88US=> NWjRSm16W0GQR1XS
SH-4 NF\BNZVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4TOc2lEPTB;M{KuNVg2QCEQvF2= M3[wSnNCVkeHUh?=
A204 NW\LeWM2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MX3JR|UxRTN{LkWwOlkh|ryP MXvTRW5ITVJ?
DMS-273 NIHrVJhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4ixR2lEPTB;M{KuOVMzOiEQvF2= NEPXOnlUSU6JRWK=
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SK-MEL-2 NHq1fJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MknCTWM2OD1|Mj62OVI4KM7:TR?= NHLveHJUSU6JRWK=
NCI-H2228 MYLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NY\FenY1UUN3ME2zNk43PjB{IN88US=> NFXwV4lUSU6JRWK=
MKN28 NX32cok3T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mo[4TWM2OD1|Mj63PFM5KM7:TR?= NIThcW5USU6JRWK=
H-EMC-SS NXjxdYxuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HZeGlEPTB;M{KuPVY4QCEQvF2= MkjUV2FPT0WU
ATN-1 M2\BZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXXJR|UxRTN|LkG0NVYh|ryP NHXvNmJUSU6JRWK=
D-263MG M{DkUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmjuTWM2OD1|Mz64N|c5KM7:TR?= M1i4dHNCVkeHUh?=
LU-135 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHPZN3lKSzVyPUOzMlg5OjlizszN NYH4TWlvW0GQR1XS
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KM-H2 NYnSO5pNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4njSGlEPTB;M{SuNVc4QSEQvF2= NU\UVFFYW0GQR1XS
NCI-H2122 M33Pcmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEmwVpVKSzVyPUO0MlM1PzFizszN MXTTRW5ITVJ?
ABC-1 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX\JR|UxRTN2LkO2PVMh|ryP MYnTRW5ITVJ?
NCI-H1355 Ml:2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTN2LkO4PFkh|ryP Mo\1V2FPT0WU
NOMO-1 NIDlSFFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFHsPHdKSzVyPUO0MlU4ODNizszN NU\tb3N2W0GQR1XS
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NCI-H810 Mof6S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn;OTWM2OD1|ND63Nlc5KM7:TR?= MoLkV2FPT0WU
D-392MG MoLiS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4nnTmlEPTB;M{WuNFU3PSEQvF2= NUPFUnJkW0GQR1XS
LB771-HNC NF\oZ5FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\PcFN5UUN3ME2zOU4yPjV6IN88US=> NHfSZ3FUSU6JRWK=
COLO-679 Mm\tS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlX6TWM2OD1|NT6zPFgh|ryP NV65WmVWW0GQR1XS
SK-PN-DW MmfqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYjHZotEUUN3ME2zOU41OzZ7IN88US=> NV;OR29ZW0GQR1XS
VA-ES-BJ MmHDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVPJR|UxRTN3LkS2OFkh|ryP NIXX[|BUSU6JRWK=
KNS-42 MWfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFexNlNKSzVyPUO1MlU5OjZizszN M1jWbXNCVkeHUh?=
RVH-421 MmLzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH3YRXVKSzVyPUO1Mlc3PDVizszN MVXTRW5ITVJ?
P30-OHK M2fB[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mk\0TWM2OD1|NT64O|UzKM7:TR?= NFrLb2NUSU6JRWK=
G-402 M{fLNGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlXVTWM2OD1|NT65PFY4KM7:TR?= NITIbGZUSU6JRWK=
S-117 Mm\ZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIPMRXhKSzVyPUO2MlMxODhizszN M2T3W3NCVkeHUh?=
RXF393 M2TqN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEjlZ4hKSzVyPUO2MlM4QDVizszN NYXCSo5mW0GQR1XS
LCLC-103H NXnBNJFxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFflRohKSzVyPUO2Mlc5ODNizszN NXfWTHJDW0GQR1XS
U-118-MG NWTINZdyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTN4Lki4OFch|ryP NILnUVhUSU6JRWK=
8-MG-BA NV35UXVnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mn\PTWM2OD1|Nj65OFg{KM7:TR?= NXKxbJJNW0GQR1XS
MFH-ino M1;mNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXjJR|UxRTN5LkOzO|Eh|ryP NGP6PGxUSU6JRWK=
NCI-H23 NXPEWHdlT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NY\tbJNTUUN3ME2zO{41OTl4IN88US=> MVjTRW5ITVJ?
NCI-H446 M3vsemdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfae2lKSzVyPUO3MlQ5PjJizszN MnLVV2FPT0WU
LU-99A NIG3SWJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MV\JR|UxRTN5LkW3N|Eh|ryP NIjrXnFUSU6JRWK=
KP-N-YN NXP6XJF2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NICzVHlKSzVyPUO3MlYyQTVizszN NHztVGxUSU6JRWK=
SCC-9 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;zeIRKSzVyPUO3Mlc5OzhizszN MlT6V2FPT0WU
EFM-19 NWnsZ2ZNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVztNWVEUUN3ME2zO{44QTZ5IN88US=> MlLjV2FPT0WU
A427 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NETsSodKSzVyPUO3MlkyODdizszN MYfTRW5ITVJ?
LB831-BLC NH3ofZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT3TWM2OD1|OD62NFM6KM7:TR?= M13sfXNCVkeHUh?=
HOS M3HZS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfRRoFsUUN3ME2zPU43Ojd|IN88US=> NV;XOGZLW0GQR1XS
LAN-6 NIj5R5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NULZWIs4UUN3ME20NE4xOTF{IN88US=> NH75cXFUSU6JRWK=
U251 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{jER2lEPTB;NECuOFA2PCEQvF2= M4LzPHNCVkeHUh?=
SNU-387 NHjpNG5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkT2TWM2OD12MD60OVU{KM7:TR?= NWHIflFFW0GQR1XS
DMS-79 Mnm3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoiyTWM2OD12MD61PFg6KM7:TR?= MWXTRW5ITVJ?
SK-LU-1 M4fDTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHMTWM2OD12MD62OVY5KM7:TR?= NUjF[4dIW0GQR1XS
HT NETvZ2RIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX0TWM2OD12MD62OlM6KM7:TR?= MYXTRW5ITVJ?
KP-N-YS NFvkemxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1r2Z2lEPTB;NECuOlc3QCEQvF2= M1X1d3NCVkeHUh?=
DMS-114 MlTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2\T[2lEPTB;NECuPFM4PCEQvF2= NYjXNnVMW0GQR1XS
HUTU-80 NUDaZWxiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWSwT3J3UUN3ME20NU4xPTZ7IN88US=> NEPJZ3NUSU6JRWK=
ONS-76 MmLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVjOSGpQUUN3ME20NU41PzB7IN88US=> M3PjVXNCVkeHUh?=
A673 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml\TTWM2OD12MT61NVU4KM7:TR?= NEO4SXpUSU6JRWK=
HPAF-II MV7Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3fPemlEPTB;NEGuOlcxQSEQvF2= MU\TRW5ITVJ?
UACC-257 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUDJR|UxRTRzLkezOlkh|ryP NG\Qe49USU6JRWK=
EW-22 NHf5fY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYL6U3RHUUN3ME20NU45Pjl5IN88US=> MX\TRW5ITVJ?
NCI-H1755 NXrQbYRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Mnn6TWM2OD12MT64O|I2KM7:TR?= M37TZ3NCVkeHUh?=
KYSE-150 MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M33WUmlEPTB;NEKuNVc5OiEQvF2= MmXqV2FPT0WU
CGTH-W-1 M17rS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3jKVmlEPTB;NEKuOFk2PSEQvF2= NEPHW3ZUSU6JRWK=
NB13 M4rQNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFTCWFVKSzVyPUSyMlYzOTdizszN NUHQT2VHW0GQR1XS
SW872 NVrtSFlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{PxSWlEPTB;NEKuOlM{OSEQvF2= MVHTRW5ITVJ?
KP-4 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTR{Lki4N|Ih|ryP NX;EXHFvW0GQR1XS
HCC38 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkniTWM2OD12Mj65OlE5KM7:TR?= NF3RPJlUSU6JRWK=
BB49-HNC NFnH[21Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn3WTWM2OD12Mz6yN|U3KM7:TR?= MUHTRW5ITVJ?
CAL-62 MmTSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3ZR5B{UUN3ME20N{41ODJ6IN88US=> MlrwV2FPT0WU
NCI-H2029 NETWUXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXrJR|UxRTR|LkW1PFEh|ryP MnvZV2FPT0WU
M14 NUf0e4lWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnPTTWM2OD12ND6xN|MzKM7:TR?= NVGzNFBPW0GQR1XS
COLO-680N MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGXuRY5KSzVyPUS0MlM{QSEQvF2= MlvmV2FPT0WU
Hs-578-T M2ribmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MlPCTWM2OD12NT6wNlk1KM7:TR?= NFrHXGFUSU6JRWK=
MSTO-211H NETVPXlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVzBRm1ZUUN3ME20OU46PDh{IN88US=> M1nLb3NCVkeHUh?=
EW-1 Mk\pS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjJR|UxRTR3Lkm2PFkh|ryP MmnXV2FPT0WU
SW948 NILscXBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYHUVHREUUN3ME20Ok41PDZ{IN88US=> NF33N2VUSU6JRWK=
NCI-H460 MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTR4LkWyN{DPxE1? M1fQV3NCVkeHUh?=
CAS-1 NUXv[otNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{n0PWlEPTB;NE[uO|cxOSEQvF2= NXvzbotMW0GQR1XS
TGBC11TKB MnLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWjqT3FjUUN3ME20O{4yPzd5IN88US=> MnTGV2FPT0WU
HD-MY-Z NYjDVo15T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYnJR|UxRTR6Lke4OkDPxE1? NUezN5BIW0GQR1XS
NCI-H226 MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoSzTWM2OD12OT63O|g2KM7:TR?= MV\TRW5ITVJ?
PA-1 M2TDTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYHI[YdEUUN3ME20PU45OzN3IN88US=> NIfpellUSU6JRWK=
LB2518-MEL M4PIfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEnLOIFKSzVyPUS5Mlg4OjNizszN M1Tme3NCVkeHUh?=
A101D NXrFXmJ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4HVVmlEPTB;NEmuPVQzPSEQvF2= NF\wZotUSU6JRWK=
NCI-H2087 MoHjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUDmfVAxUUN3ME20PU46Pjh{IN88US=> M2fO[3NCVkeHUh?=

... Click to View More Cell Line Experimental Data

In vivo 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]

Protocol

Kinase Assay:

[1]

+ Expand

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.
Cell Research:

[1]

+ Expand
  • Cell lines: NSCLC cells
  • Concentrations: 0-10 μM
  • Incubation Time: 1 hour
  • Method:

    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.


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Athymic NMRI-nu/nu female mice
  • Formulation: In 0.5% methocellulose-0.4% polysorbate-80 (Tween 80)
  • Dosages: 20 mg/kg
  • Administration: Oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 97 mg/mL (199.61 mM)
Ethanol 15 mg/mL (30.86 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order:
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
10mg/mL

* 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.

Chemical Information

Molecular Weight 485.94
Formula

C24H25ClFN5O3

CAS No. 439081-18-2
Storage powder
in solvent
Synonyms N/A

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
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    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

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Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02795156 Recruiting Non-small Cell Lung Carcinoma|Urothelial Carcinoma|Gastrointestinal Carcinoma, Non-colon|Upper Aerodigestive Tract Carcinoma SCRI Development Innovations, LLC|Foundation Medicine|Boehringer Ingelheim|Bayer September 28, 2016 Phase 2
NCT03054038 Not yet recruiting Non-Small Cell Lung Carcinoma Vanderbilt-Ingram Cancer Center|National Cancer Institute (NCI) February 2017 Phase 1
NCT02979977 Not yet recruiting Squamous Cell Cancers of the Head and Neck Aarti Bhatia|National Comprehensive Cancer Network|Boehringer Ingelheim|Yale University December 2016 Phase 2
NCT02876081 Not yet recruiting SMALL CELL LUNG CARCINOMA Groupe Hospitalier Paris Saint Joseph December 2016 Phase 2
NCT02183883 Recruiting Non-small Cell Lung Cancer University College, London|Boehringer Ingelheim December 2016 Phase 2
NCT02423525 Recruiting Brain Cancer Santosh Kesari|Boehringer Ingelheim|John Wayne Cancer Institute October 2016 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

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.

EGFR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID