Afatinib (BIBW2992)

製品コードS1011

Afatinib (BIBW2992)化学構造

分子量(MW):485.94

Afatinib (BIBW2992) 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 in cell-free assays, respectively.

サイズ 価格(税別)  
JPY 39840.00
JPY 19920.00
JPY 34860.00
JPY 94620.00

文献中Selleckの製品使用例(38)

カスタマーフィードバック(5)

  • Immunoblot analysis of serum starved H2030 cells pre-treated with 500 nM or 1 µM of gefitinib, crizotinib, CP-724714, or afatinib for 12 hr, followed by stimulation with EGF, HGF, NRG1, or their combination (50 ng/ml) for 10 min.

    Nature, 2016, 534(7609):647-51. Afatinib (BIBW2992) purchased from Selleck.

    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.

製品安全説明書

EGFR阻害剤の選択性比較

生物活性

製品説明 Afatinib (BIBW2992) 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 in cell-free assays, respectively.
ターゲット
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
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HDLM-2 MluxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVLJR|UxRTBwMEC1O|Ih|ryP M1HjZ3NCVkeHUh?=
KASUMI-1 NHnP[W9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGW5c4xKSzVyPUCuNFA6OTFizszN NI\6VXNUSU6JRWK=
HCC2218 NVS3SJB{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{Xr[2lEPTB;MD6wNFk5PyEQvF2= M2PaXXNCVkeHUh?=
KARPAS-45 M1TNTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXvPUmNoUUN3ME2wMlAyPjdzIN88US=> NEfQXFlUSU6JRWK=
HSC-4 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVTJR|UxRTBwMEG3OFgh|ryP MXHTRW5ITVJ?
CHL-1 NHi4NpRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NHPYXmVKSzVyPUCuNFE5OzlizszN MnTNV2FPT0WU
KY821 M3TIV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYHJR|UxRTBwMEKwOkDPxE1? NWHkTFl2W0GQR1XS
NCI-N87 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoDQTWM2OD1yLkCyO|c{KM7:TR?= NYL3Uo9LW0GQR1XS
DOK NVf5bmRTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjCNFBsUUN3ME2wMlA{OTl2IN88US=> MVTTRW5ITVJ?
DSH1 MlvQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVTUdlNlUUN3ME2wMlA{OzF2IN88US=> NWeyZpBUW0GQR1XS
MDA-MB-175-VII NYLqfZlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3izVmlEPTB;MD6wN|QyPiEQvF2= M2S4UHNCVkeHUh?=
NCI-H2170 MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXLJR|UxRTBwMEO3Nlgh|ryP MmCwV2FPT0WU
BT-474 MYPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3K2fWlEPTB;MD6wOFk5PiEQvF2= NUWxdVBNW0GQR1XS
EFO-27 M3HJOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M36zWWlEPTB;MD6wOVE5OiEQvF2= MYfTRW5ITVJ?
NCI-H720 M{PNSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWrJR|UxRTBwMEWzNlUh|ryP MUfTRW5ITVJ?
PC-14 M1TlRmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYDJR|UxRTBwMEW2Olgh|ryP NHrObGZUSU6JRWK=
EC-GI-10 NEf6UJZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4\OPWlEPTB;MD6wOVkyOiEQvF2= M4rqW3NCVkeHUh?=
KYSE-450 MnvES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MW\JR|UxRTBwMEW5O|gh|ryP MlLMV2FPT0WU
BPH-1 MlLlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYrXdnpkUUN3ME2wMlA2QTh6IN88US=> M4fscHNCVkeHUh?=
NCI-H292 NHzofpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYWyb5BnUUN3ME2wMlA3ODlizszN M{H3[3NCVkeHUh?=
H9 MnvCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLuTWM2OD1yLkC3NVMzKM7:TR?= MYLTRW5ITVJ?
NCI-H526 Mo\YS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXPTSXBRUUN3ME2wMlA4QDJ|IN88US=> NULubFNmW0GQR1XS
NCI-H1623 Mn7JS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFi3bWxKSzVyPUCuNFgxOjVizszN MmfxV2FPT0WU
KYSE-140 M3H6[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGf1dnNKSzVyPUCuNFg{OyEQvF2= NXzQOHBFW0GQR1XS
Ca9-22 NVnkNItoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHrTWM2OD1yLkC4N|U{KM7:TR?= MnrSV2FPT0WU
AU565 NEXneXZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnjETWM2OD1yLkC4OVA1KM7:TR?= MYrTRW5ITVJ?
ZR-75-30 M{m4V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4ni[2lEPTB;MD6wPVU1PSEQvF2= MV\TRW5ITVJ?
NCI-H1770 M1LwbWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFXjNHZKSzVyPUCuNVAzQCEQvF2= NHKzcXZUSU6JRWK=
LB2241-RCC M1XxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MkLxTWM2OD1yLkGwPFg1KM7:TR?= NHvzRpdUSU6JRWK=
CAL-39 NGrUUmpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIG3N|ZKSzVyPUCuNVE4QTJizszN M1fuc3NCVkeHUh?=
UACC-893 NEG4WIZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlXqTWM2OD1yLkGxPFg2KM7:TR?= M3;xcHNCVkeHUh?=
LU-65 NXfaOJAxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnnHTWM2OD1yLkGyOlM{KM7:TR?= NEfne2NUSU6JRWK=
HN NFiybFBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPoS25KSzVyPUCuNVMxPzdizszN NFra[ZlUSU6JRWK=
TI-73 M2TN[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWXJR|UxRTBwMUS3NVUh|ryP MU\TRW5ITVJ?
KU812 M4fGeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoHDTWM2OD1yLkG1OFU3KM7:TR?= M2DOR3NCVkeHUh?=
SW13 M2SyTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1rXUWlEPTB;MD6xOlIyPiEQvF2= NH74WJpUSU6JRWK=
BB30-HNC MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUTJR|UxRTBwMU[1O|Yh|ryP MUDTRW5ITVJ?
HSC-2 MnLmS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDJR|UxRTBwMU[4N|ch|ryP MnHyV2FPT0WU
BV-173 MljQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlPuTWM2OD1yLkG3OVk3KM7:TR?= NILLXoxUSU6JRWK=
CAL-27 M2TGXmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4PuTGlEPTB;MD6xO|Y{PiEQvF2= NUX5eIZPW0GQR1XS
SBC-1 M{CyTGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{facGlEPTB;MD6xPFk2QSEQvF2= MmjUV2FPT0WU
CAL-33 NFjITY5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1qzT2lEPTB;MD6yNFE5PCEQvF2= NHewUWpUSU6JRWK=
NCI-H209 M1m2V2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MW\JR|UxRTBwMkC0OkDPxE1? MnjWV2FPT0WU
COR-L105 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX\pUGdsUUN3ME2wMlIyODh2IN88US=> MYjTRW5ITVJ?
HSC-3 MmK4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4HyNGlEPTB;MD6yNVE6QCEQvF2= MmnXV2FPT0WU
NCI-H69 NGrFWopIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEjNWYFKSzVyPUCuNlE1PTFizszN M1T6RnNCVkeHUh?=
MOLT-13 NXz6Z3FIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXPKNnVnUUN3ME2wMlI{QTd3IN88US=> NGPseWxUSU6JRWK=
ML-2 NHrO[JlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUTJR|UxRTBwMkS4NFIh|ryP NYrXTlBoW0GQR1XS
IGROV-1 M{\YXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXzrelN[UUN3ME2wMlI2QTV{IN88US=> M1fZ[3NCVkeHUh?=
TK10 M2OzO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjuTZR5UUN3ME2wMlI3PzN6IN88US=> NHH1SGhUSU6JRWK=
EoL-1-cell MkOzS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwMk[4PVIh|ryP NV7Se5NzW0GQR1XS
HO-1-N-1 MlPUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{\W[mlEPTB;MD6yO|g2OyEQvF2= MVPTRW5ITVJ?
BHY MnrJS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2rxOWlEPTB;MD6yPFY2PSEQvF2= NYftSnlWW0GQR1XS
LU-139 Mk\yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{C0VmlEPTB;MD6zNFUyKM7:TR?= MY\TRW5ITVJ?
23132-87 MlzWS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTBwM{G5NlMh|ryP MlnFV2FPT0WU
ACHN NHvWfnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnXsTWM2OD1yLkOxPVk1KM7:TR?= MUPTRW5ITVJ?
DoTc2-4510 NF\uNmRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX;JR|UxRTBwM{KyNVkh|ryP MXTTRW5ITVJ?
BB65-RCC MmGxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmjaTWM2OD1yLkO0OVk{KM7:TR?= Mn;mV2FPT0WU
HLE NVTD[3pXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M16xTmlEPTB;MD6zOVA1PiEQvF2= NV\GW4gxW0GQR1XS
HCC1419 MojYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmKwTWM2OD1yLkO2OFA5KM7:TR?= NULrNmhyW0GQR1XS
A388 MYDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFPLTnlKSzVyPUCuN|Y5PTdizszN NYXrbY97W0GQR1XS
NUGC-3 M33J[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWPJR|UxRTBwM{izO|Mh|ryP NXfvZ2NEW0GQR1XS
KYSE-180 MmLQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NH:5UJJKSzVyPUCuN|kxQDlizszN NUftfld2W0GQR1XS
TE-6 NFO5V2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVTJR|UxRTBwNECyOFYh|ryP NGjGSXlUSU6JRWK=
A498 NHrhRYhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFLV[G9KSzVyPUCuOFA3PzRizszN MoqwV2FPT0WU
NCI-H1648 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlq4TWM2OD1yLkS0NVgzKM7:TR?= MYfTRW5ITVJ?
DU-145 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX;OR2VHUUN3ME2wMlQ1QDN|IN88US=> M2fZcHNCVkeHUh?=
CW-2 NEi1c5dIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYfJR|UxRTBwNE[5NVQh|ryP NEDGZXBUSU6JRWK=
A431 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFnZRWJKSzVyPUCuOFgzOzNizszN MoH0V2FPT0WU
SAS NFfIOZhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnlUlVKSzVyPUCuOFg{QThizszN M4HQeXNCVkeHUh?=
NCI-H2126 MoKwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHrGN5dKSzVyPUCuOVE6OjZizszN MYTTRW5ITVJ?
NCI-H358 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVW1cJFZUUN3ME2wMlU{OjFizszN MYHTRW5ITVJ?
FADU Mof1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1zRbmlEPTB;MD61OFQxPCEQvF2= NUTWeFg6W0GQR1XS
ACN MnvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVv2[GVRUUN3ME2wMlU2ODl2IN88US=> NUfnVmdSW0GQR1XS
HCC70 Ml76S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{iwSmlEPTB;MD61O|Y3OSEQvF2= MmPqV2FPT0WU
NCI-H1838 M3jjTWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUDJR|UxRTBwNkCyPVkh|ryP NEjJWVRUSU6JRWK=
CAL-54 NY[yflZWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlraTWM2OD1yLk[xOlIyKM7:TR?= M1f6N3NCVkeHUh?=
NCI-H1975 NXPzUnhbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWHJR|UxRTBwNkG3Nlgh|ryP Mn7iV2FPT0WU
COR-L88 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHfaW5VKSzVyPUCuOlQyOTNizszN NHu0dGZUSU6JRWK=
CTV-1 NFHkbm5Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mm\yTWM2OD1yLk[0N|kzKM7:TR?= MY\TRW5ITVJ?
EW-18 MmrKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIDYcpZKSzVyPUCuOlg3QThizszN M1jFSHNCVkeHUh?=
HCC1806 NWn0PWZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXzCTFJHUUN3ME2wMlY6PjZ4IN88US=> MWHTRW5ITVJ?
HuP-T4 MVrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVjJR|UxRTBwNkm3OkDPxE1? NHXD[FRUSU6JRWK=
MDA-MB-361 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYnJR|UxRTBwN{K2OlIh|ryP MknSV2FPT0WU
NCI-H1573 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHTvXo1KSzVyPUCuO|M3OyEQvF2= MnLCV2FPT0WU
KU-19-19 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF\PdnBKSzVyPUCuO|c1PjRizszN Mo\vV2FPT0WU
COLO-678 NW\lN2ZyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFfIb5JKSzVyPUCuPFA5OzRizszN MXLTRW5ITVJ?
C-33-A MmXoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVvzUFNkUUN3ME2wMlgyOjl5IN88US=> MlPLV2FPT0WU
Calu-3 Moq5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MY\JR|UxRTBwOEG0N|Qh|ryP MWPTRW5ITVJ?
AGS MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHrSVGxKSzVyPUCuPFM3PDhizszN NFj6O2dUSU6JRWK=
SCC-25 MnvRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVjJR|UxRTBwOESxO|Eh|ryP MVfTRW5ITVJ?
JVM-2 Mlr5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHHtXHZKSzVyPUCuPFgzQTlizszN MWnTRW5ITVJ?
HCE-T Mn;XS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHGXZZKSzVyPUCuPFg1OjhizszN NEPse2hUSU6JRWK=
ES4 MVLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXsPGdFUUN3ME2wMlk4QDN4IN88US=> M4\5fHNCVkeHUh?=
EKVX MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEPjbWdKSzVyPUGuNFExPjRizszN MVzTRW5ITVJ?
D-542MG NG\2V|lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV76UWF1UUN3ME2xMlAyODZ2IN88US=> NIrDb3VUSU6JRWK=
SW1116 MYXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW\JR|UxRTFwMEGyPFch|ryP NX7EbGhyW0GQR1XS
5637 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3XYXWlEPTB;MT6wNVUyKM7:TR?= NFm0VIxUSU6JRWK=
HT-1376 NVHPSnpvT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1PGdWlEPTB;MT6wNVUyOyEQvF2= MVPTRW5ITVJ?
NB69 MmnlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWe1NoRmUUN3ME2xMlAzQTR3IN88US=> MnHMV2FPT0WU
YKG-1 MXfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVHJR|UxRTFwMEW0NVkh|ryP NWXTU24{W0GQR1XS
EW-3 NWjhfI5yT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXPJR|UxRTFwMEe4PFMh|ryP NETIToZUSU6JRWK=
GCIY Ml7sS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M37tZ2lEPTB;MT6wPFExPCEQvF2= MYnTRW5ITVJ?
SK-MES-1 M134W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zVR2lEPTB;MT6xNVQ5PyEQvF2= NWnxV3JKW0GQR1XS
PANC-08-13 NF7zSVVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M37GU2lEPTB;MT6xOlQyPiEQvF2= M{C5e3NCVkeHUh?=
SK-NEP-1 NVvV[WxKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXTJR|UxRTFwMUe1NVMh|ryP MXTTRW5ITVJ?
SW954 NFSxbohIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NV;xPWlXUUN3ME2xMlIxOjF2IN88US=> Mnv5V2FPT0WU
NCI-SNU-5 M3[4bmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIjZR4NKSzVyPUGuNlM6KM7:TR?= MVvTRW5ITVJ?
SW48 NGK5dWdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEfjclhKSzVyPUGuNlU1OzJizszN NGrpdolUSU6JRWK=
HT-3 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYL6WmJTUUN3ME2xMlI5PzV|IN88US=> NYPnWHNpW0GQR1XS
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OAW-28 NVLWdFBwT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYi0fIpbUUN3ME23Mlk1PTd6IN88US=> M3TMOHNCVkeHUh?=
KURAMOCHI MnzCS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXvCc3NkUUN3ME23Mlk1QDFzIN88US=> MonLV2FPT0WU
BE-13 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4PxUmlEPTB;Nz65PFEyOiEQvF2= MoDIV2FPT0WU
VMRC-RCZ MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVrJR|UxRThwMEG2PVch|ryP MUPTRW5ITVJ?
NCI-H727 NV;NcVNWT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUfIO4lEUUN3ME24MlExPDJizszN NIrLbWpUSU6JRWK=
SW1710 MkiyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHy0[pBKSzVyPUiuNVg2OTVizszN MYHTRW5ITVJ?
D-502MG MXjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mn7sTWM2OD16LkK5NlgzKM7:TR?= Mo\IV2FPT0WU
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HAL-01 MkDaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIS5NJVKSzVyPUiuOVE6OSEQvF2= M2\idnNCVkeHUh?=
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EW-11 NFXPSVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2nHd2lEPTB;OT6xO|Y2OyEQvF2= M1L5fXNCVkeHUh?=
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BALL-1 NVfF[3RYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NE\sR4tKSzVyPUmuNlE6ODdizszN M4fTTHNCVkeHUh?=
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CAL-72 MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4LX[2lEPTB;MUCuPVM6OSEQvF2= M{LsfXNCVkeHUh?=
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UACC-62 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LBVWlEPTB;MUGuNlM3QCEQvF2= NXSyZ2FqW0GQR1XS
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ALL-PO MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnnETWM2OD1zMT6yOVEzKM7:TR?= MmjBV2FPT0WU
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SW626 NGe2VplIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEPReFNKSzVyPUGxMlU4PTVizszN M3\VWXNCVkeHUh?=
RPMI-2650 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGTaSINKSzVyPUGxMlU5QDVizszN M4LaVnNCVkeHUh?=
MC-IXC Mn;US5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWnaOZRyUUN3ME2xNU43PzJ6IN88US=> NG\wSJhUSU6JRWK=
HOP-62 NG[wVHhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MmiyTWM2OD1zMT62O|Y1KM7:TR?= M4XK[nNCVkeHUh?=
NOS-1 NFvyOIpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH\lcWdKSzVyPUGxMlcyODlizszN M{SweXNCVkeHUh?=
SW1573 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NGPzWIVKSzVyPUGxMlczQTVizszN M3XHVXNCVkeHUh?=
WM-115 MoraS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3lUXpEUUN3ME2xNU44PTh6IN88US=> MYrTRW5ITVJ?
HuO9 NInHOVhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFrGUGJKSzVyPUGxMlg4PzRizszN MYjTRW5ITVJ?
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NCI-H596 M3vmUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2Pqd2lEPTB;MUKuNFM3QSEQvF2= NES3WpdUSU6JRWK=
A172 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DCZWlEPTB;MUKuNFc6QCEQvF2= Mki2V2FPT0WU
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PFSK-1 Mm\iS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVzJR|UxRTF|LkC2JO69VQ>? M3\jT3NCVkeHUh?=
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OVCAR-5 M1rPdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYXPb4dJUUN3ME2xN{4yPTl|IN88US=> NFmxTYlUSU6JRWK=
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EW-13 NFrYOVBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVHQSVdMUUN3ME2xOE4xOzV{IN88US=> M3fZWHNCVkeHUh?=
NCI-H1793 NGnRNYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3r1WmlEPTB;MUSuNlA5PyEQvF2= NF;3XWlUSU6JRWK=
BHT-101 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnSzTWM2OD1zND6yOFEh|ryP Mni5V2FPT0WU
RKO M3rEOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYPIUlVzUUN3ME2xOE42ODd3IN88US=> NGXYTldUSU6JRWK=
NEC8 NHmz[nFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NYPnSYU1UUN3ME2xOE42PDd{IN88US=> NG\zXWlUSU6JRWK=
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NCI-H2030 NYj0OXkxT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvUTHV2UUN3ME2xOE43PDR6IN88US=> MV3TRW5ITVJ?
C2BBe1 M3:4Wmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mlm3TWM2OD1zND63OlQh|ryP M{DHZnNCVkeHUh?=
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SW1463 NGHQNFZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3ywc2lEPTB;MUWuNFQ5PSEQvF2= M3ixbXNCVkeHUh?=
J82 NEfrcJRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NG\tXnJKSzVyPUG1MlA2PyEQvF2= MYnTRW5ITVJ?
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COLO-824 M4rVN2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmrNTWM2OD1zNT6xOVc6KM7:TR?= MYTTRW5ITVJ?
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CP66-MEL MnW0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3jYdmlEPTB;MUWuOFY5QCEQvF2= MWfTRW5ITVJ?
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OVCAR-8 MoDNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{jTVWlEPTB;MUWuPFg3OSEQvF2= MlTVV2FPT0WU
MFE-280 NVLTT2FXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1\l[WlEPTB;MU[uNFQ5QCEQvF2= NXP2fmVFW0GQR1XS
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MFM-223 MmDkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWrjO4pRUUN3ME2xOk4{QTZ3IN88US=> MVXTRW5ITVJ?
L-363 MmPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYLMZmNsUUN3ME2xOk41PTd5IN88US=> MXXTRW5ITVJ?
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HH M1y2Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFm1e3NKSzVyPUG2MlUyPjJizszN MkW0V2FPT0WU
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NCI-H2405 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mlv2TWM2OD1zNz6xPVc1KM7:TR?= NXX3Z|N{W0GQR1XS
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RH-18 Ml7ES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NGHGWoJKSzVyPUG4MlAxOzVizszN M{LBN3NCVkeHUh?=
D-283MED MW\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzLbmluUUN3ME2xPE4xODh6IN88US=> MnqzV2FPT0WU
RCC10RGB M1TEZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDndodKSzVyPUG4MlA2PTlizszN NHT0eXpUSU6JRWK=
NCI-H1437 M3rnO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGC5SmhKSzVyPUG4MlE3PDFizszN MVXTRW5ITVJ?
SW982 NYfiTXlbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2HnUWlEPTB;MUiuNlY4OSEQvF2= NV22S3doW0GQR1XS
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SCH Mki3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPpN|JKSzVyPUG4MlY1PTZizszN MoPRV2FPT0WU
COLO-320-HSR M3rvNWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHKRVBEUUN3ME2xPE44PDZizszN MnfYV2FPT0WU
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LU-135 M365W2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrZZmNyUUN3ME2zN{45QDJ7IN88US=> M3e4fnNCVkeHUh?=
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KM-H2 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmD1TWM2OD1|ND6xO|c6KM7:TR?= M1L6OHNCVkeHUh?=
NCI-H2122 MnX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NXzOTmFJUUN3ME2zOE4{PDdzIN88US=> NHHxXIxUSU6JRWK=
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NCI-H1355 NIX3RnpIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1\BUGlEPTB;M{SuN|g5QSEQvF2= M4PoVHNCVkeHUh?=
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D-392MG M4O1eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFfxUlVKSzVyPUO1MlA2PjVizszN NYnvWGVLW0GQR1XS
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P30-OHK MlLuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHLCS3NKSzVyPUO1Mlg4PTJizszN M13ZfnNCVkeHUh?=
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LCLC-103H MoXQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlGyTWM2OD1|Nj63PFA{KM7:TR?= M3HIeHNCVkeHUh?=
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8-MG-BA MoftS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVTJR|UxRTN4Lkm0PFMh|ryP MV7TRW5ITVJ?
MFH-ino MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH;NbIFKSzVyPUO3MlM{PzFizszN M1TrPHNCVkeHUh?=
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NCI-H446 NGjD[VRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MorqTWM2OD1|Nz60PFYzKM7:TR?= NVXoRYt5W0GQR1XS
LU-99A MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{TNZ2lEPTB;M{euOVc{OSEQvF2= M3qyPXNCVkeHUh?=
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LB831-BLC Mni4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXfJR|UxRTN6Lk[wN|kh|ryP NI\1WJFUSU6JRWK=
HOS MnLRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWD4UZdMUUN3ME2zPU43Ojd|IN88US=> NVjXbZQzW0GQR1XS
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U251 NVPldHl2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIfkfodKSzVyPUSwMlQxPTRizszN MVnTRW5ITVJ?
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HUTU-80 M4Xy[mdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXvJR|UxRTRzLkC1Olkh|ryP NEPGcI1USU6JRWK=
ONS-76 MlPtS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mo\WTWM2OD12MT60O|A6KM7:TR?= Mn7PV2FPT0WU
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UACC-257 NIP5W2pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXzJR|UxRTRzLkezOlkh|ryP MknZV2FPT0WU
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M14 M{nXXWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXrjd|JVUUN3ME20OE4yOzN{IN88US=> MmK0V2FPT0WU
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NCI-H460 NVLOOINbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWfJR|UxRTR4LkWyN{DPxE1? NG\yRWVUSU6JRWK=
CAS-1 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MoPkTWM2OD12Nj63O|AyKM7:TR?= MmXyV2FPT0WU
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HD-MY-Z Mo\nS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M4\pZ2lEPTB;NEiuO|g3KM7:TR?= MnL0V2FPT0WU
NCI-H226 NUPhRXNkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWjJR|UxRTR7Lke3PFUh|ryP NF;kNXZUSU6JRWK=
PA-1 NWPhbZNFT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXG0O|VUUUN3ME20PU45OzN3IN88US=> MoOyV2FPT0WU
LB2518-MEL NGTwe4lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2exZ2lEPTB;NEmuPFczOyEQvF2= NFTiPFFUSU6JRWK=
A101D NUT2fIF1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHrG[XlKSzVyPUS5Mlk1OjVizszN M3X1dnNCVkeHUh?=
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他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

体内試験 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]

お薦めの試験操作(参考用のみ)

キナーゼ試験:

[1]

+ 展開

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.
細胞試験:

[1]

+ 展開
  • 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.


    (参考用のみ)
動物試験:

[1]

+ 展開
  • 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
    (参考用のみ)

溶解度 (25°C)

体外 DMSO 97 mg/mL (199.61 mM)
Ethanol 15 mg/mL (30.86 mM)
Water Insoluble
体内 左から(NMPから)右の順に溶剤を製品に加えます(文献ではなく、Selleckの実験によるデータ):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
混合させたのち直ちに使用することを推奨します。
10mg/mL

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 485.94
化学式

C24H25ClFN5O3

CAS No. 439081-18-2
保管
in solvent
別名 N/A

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (g) = 濃度 (mol/L) x 体積 (L) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとMSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとMSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03878524 Not yet recruiting Breast Cancer|Prostate Cancer|Pancreatic Cancer|Acute Myelogenous Leukemia OHSU Knight Cancer Institute|Oregon Health and Science University|Prospect Creek Foundation March 14 2019 Phase 1
NCT03827070 Recruiting Non Small Cell Lung Cancer Center Trials & Treatment Europe|Center Trials & Treatment March 5 2019 Phase 1
NCT03827070 Recruiting Non Small Cell Lung Cancer Center Trials & Treatment Europe|Center Trials & Treatment March 5 2019 Phase 1
NCT03727724 Active not recruiting Carcinoma Non-Small-Cell Lung The Netherlands Cancer Institute|Boehringer Ingelheim|Merck Serono International SA December 4 2018 Phase 2
NCT03727724 Active not recruiting Carcinoma Non-Small-Cell Lung The Netherlands Cancer Institute|Boehringer Ingelheim|Merck Serono International SA December 4 2018 Phase 2

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

  • * 必須

よくある質問(FAQ)

  • 質問1:

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

  • 回答:

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

EGFRシグナル伝達経路

EGFR Inhibitors with Unique Features

相関EGFR製品

Tags: Afatinib (BIBW2992)を買う | Afatinib (BIBW2992) ic50 | 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)化学構造 | Afatinib (BIBW2992)分子量 | Afatinib (BIBW2992)代理店
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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID