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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-AZD-9291 dimesylate
AZD-9291 dimesylate

Chemical Structure : AZD-9291 dimesylate

CAS No.: 2070014-82-1

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AZD-9291 dimesylate (Osimertinib dimesylate, Mereletinib dimesylate)

货号: PC-45997Not For Human Use, Lab Use Only.

Osimertinib dimesylate (AZD-9291) is a potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.

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25 mg ￥880 In stock
100 mg ￥1580 In stock
250 mg ￥2580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Osimertinib dimesylate (AZD-9291) is a potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively.
Osimertinib shows weak activity against wt EGFR (IC50=184 nM).
Osimertinib inhibits signaling pathways and cellular growth in both EGFRm(+) and EGFRm(+)/T790M(+) mutant cell lines in vitro.
Osimertinib exhibits tumor regression in EGFR-mutant tumor xenograft and transgenic models; orally active.

物理化学性质&存储条件

分子量 691.8187
分子式 C30H41N7O8S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 0.4 mg/mL
Chemical Name/SMILES

2-Propenamide, N-[2-[[2-(dimethylamino)ethyl]methylamino]-4-methoxy-5-[[4-(1-methyl-1H-indol-3-yl)-2-pyrimidinyl]amino]phenyl]-, methanesulfonate (1:2)

参考文献

1. Finlay MR, et al. J Med Chem. 2014 Oct 23;57(20):8249-67.

2. Cross DA, et al. Cancer Discov. 2014 Sep;4(9):1046-61.

3. Eberlein CA, et al. Cancer Res. 2015 Jun 15;75(12):2489-500.

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