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折扣/货期| 货号：SYN-1012-M001 | 规格：1 mg | 目录价：￥2870 |
| 货号：SYN-1012-M005 | 规格：5 mg | 目录价：￥5824 |
| 货号：SYN-1012-M010 | 规格：10 mg | 目录价：￥9142 |
| 货号：SYN-1012-M050 | 规格：50 mg | 目录价：￥询价 |
| 货号：SYN-1012-M100 | 规格：100 mg | 目录价：￥询价 |
产品详情
* 以下信息仅供参考，详情请以原厂网站为准
产品名称:
AV-412
别名:
MP-412; AV412
产品描述:
AV-412 is a potent dual inhibitor of EGFR and ErbB2 tyrosine kinases, including the mutant EGFR(L858R,T790M), which is clinically resistant to the EGFR-specific kinase inhibitors erlotinib and gefitinib. In enzyme assays assay the compound inhibited the EGFR variants and ErbB2 in the nanomolar range with over 100-fold selectivity compared with other kinases, apart from ABL and FLT1, which were both moderately sensitive to the compound. In cells, AV-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100nM. Moreover, AV-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. In animal studies using cancer xenograft models, AV-412 (30mg/kg) demonstrated complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively.
保存温度:
+4°C
运输温度:
Ambient
预期分子量:
507
产品形式:
solid
有效期:
Stable for at least 2 years after receipt when stored at -20°C.
产地:
瑞士
纯度:
>95%
CAS号:
451492-95-8
分子式:
C27H28ClFN6O
溶解度:
Soluble in DMSO or ethanol.
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