阿法替尼 T21312

Product Introduction
Bioactivity


英文名: Afatinib

描述: Afatinib (BIBW 2992) 是一种不可逆的 EGFR 家族抑制剂，抑制 EGFRwt、EGFRL858R、EGFRL858R/T790M 和 HER2的 IC50分别为0.5 nM、0.4 nM、10 nM 和 14 nM。

体外活性: 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].

体内活性: Afatinib could effectively inhibit HKESC-2 tumor growth in mice without obvious toxicity[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 45 mg/mL (92.6 mM)


关键字: NIH-3T3 cells | ESCC | NSCLC | NCI-H1975 | Afatinib | inhibit | ErbB-1 | HKESC-2 | EC-1 | PKB | H1666 | c-Met/HGFR | Apoptosis | SLMT-1 | H3255 | A431 | BIBW-2992 | lung cancer | EGFR | Akt | Inhibitor | BIBW2992 | HER2 | Autophagy | Epidermal growth factor receptor | HKESC-1 | anticancer | Protein kinase B | orally active | p38 MAPK | HER1

相关产品: Olmutinib | Panitumumab | Saracatinib | DBPR112 | SYR127063 | DZD1516 | Tyrphostin AG 112 | EGFR-IN-12 | Pertuzumab | EMI1

相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Kinase Inhibitor Library | Inhibitor Library | Tyrosine Kinase Inhibitor Library | Anti-Cancer Active Compound Library | EMA Approved Drug Library

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