Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively).
説明 | Afatinib (BIBW 2992) is an irreversible inhibitor of EGFR family (EGFR-wt, EGFR-L858R, EGFR-L858R/T790M and HER2 with IC50s of 0.5 nM, 0.4 nM, 10 nM and 14 nM , respectively). |
ターゲット&IC50 | EGFR:0.5 nM, EGFR (L858R/T790M):10 nM, EGFR (L858R):0.4 nM, HER2:14 nM |
In vitro | ESCC cell lines were sensitive to afatinib with IC50 concentrations at lower micro-molar range (at 72 hour incubation: HKESC-1 = 0.002 μM, HKESC-2 = 0.002 μM, KYSE510 = 1.090 μM, SLMT-1 = 1.161 μM and EC-1 = 0.109 μM) with a maximum growth inhibition over 95%.?Afatinib can strongly induce G0/G1 cell cycle arrest in HKESC-2 and EC-1 in a dose- and time-dependent manner.?The phosphorylation of ErbB family downstream effectors such as pAKT, pS6 and pMAPK were significantly inhibited in HKESC-2 and EC-1.?Apoptosis was observed in both cell lines at 24 hours after exposure to afatinib, as determined by the presence of cleaved PARP[1]. |
In vivo | Afatinib could effectively inhibit HKESC-2 tumor growth in mice without obvious toxicity[1]. |
別名 | Afatinib free base, BIBW 2992 |
分子量 | 485.94 |
分子式 | C24H25ClFN5O3 |
CAS No. | 850140-72-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (92.6 mM)
You can also refer to dose conversion for different animals. 詳細
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Afatinib 850140-72-6 Angiogenesis Autophagy JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR NIH-3T3 cells ESCC NSCLC NCI-H1975 inhibit ErbB-1 HKESC-2 EC-1 PKB H1666 c-Met/HGFR Afatinib free base Apoptosis SLMT-1 H3255 BIBW 2992 A431 BIBW-2992 lung cancer Akt Inhibitor BIBW2992 HER2 Epidermal growth factor receptor HKESC-1 anticancer Protein kinase B orally active p38 MAPK HER1 inhibitor