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Lapatinib(GW572016)对ErbB-2和EGFR酪氨酸激酶结构域具有强效抑制作用,对纯化EGFR和ErbB-2的IC50值分别为10.2 nM和9.8 nM。
Afatinib(BIBW 2992)是一种口服活性强且不可逆的ErbB家族(EGFR和HER2)双特异性抑制剂,对EGFRwt、EGFRL858R、EGFRL858R/T790M和HER2的IC50值分别为0.5 nM、0.4 nM、10 nM和14 nM。阿法替尼用于研究食管鳞状细胞癌(ESCC)、非小细胞肺癌(NSCLC)和胃癌。
Dacomitinib is a potent, orally available, irreversible tyrosine kinase HER 1 (EGFR), HER2 and HER4 inhibitor with IC50 of 6, 45.7 and 73.7 nM for EGFR, ERBB2 and ERBB4, respectively.
Allitinib tosylate(AST-1306(TsOH))是一种口服活性和不可逆的EGFR和ErbB2抑制剂,其IC50值分别为0.5和3 nM。Allitinib tosylate以0.8 nM的IC50抑制ErbB4,是一种具有抗癌活性的苯基氨基喹唑啉化合物。
TAK-285 is a dual HER2 and EGFR (HER1) inhibitor with IC50 of 17 nM and 23 nM, > 10-fold selectivity for HER1/2 than HER4, less potent to MEK1/5, c-Met, Aurora B, Lck, CSK etc.
AST-1306 is an irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, also effective in mutation EGFR T790M/L858R, more potent to ErbB2-overexpressing cells, 3000-fold selective for ErbB family than other kinases.
EGFR/ErbB-2/ErbB-4 inhibitor-2是一种三重靶向抑制剂,能够有效抑制 EGFR、ErbB-2 和 ErbB-4,应用于癌症治疗研究中。
Zipalertinib是一种新型的 EGFR 突变抑制剂,专门针对肿瘤中存在的特定 EGFR 突变。它在治疗各种 EGFR 突变相关癌症,如非小细胞肺癌等方面具有显著潜力。
Poziotinib is an irreversible Pan-HER inhibitor with IC50s of 3/5/23 nM for HER1/HER2/HER4 respectively.
AZ5104 is an irreversible inhibitor of EGFR-L858R/T790M, EGFR-L858R, EGFR-L861Q, and EGFR (IC50s of < 1 nM, 6 nM, 1 nM, and 25 nM respectively). AZ5104 is the demethylated metabolite of AZD-9291.
AEE788 is an inhibitor of both EGFR and VEGFR, the IC50s for EGFR and ErbB2 is 2 nM, 6 nM respectively.
AC480 is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, ~8-fold less potent to HER4, > 100-fold to VEGFR2, c-Kit, Lck, MET etc.
Tags: ErbB4 | EGFR | ErbB4 相关产品
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