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首页-小分子抑制剂&激动剂-Tyrosine Kinase-EGFR-HKI-357
HKI-357

Chemical Structure : HKI-357

CAS No.: 848133-17-5

HKI-357 (HKI 357)

货号: PC-38733Not For Human Use, Lab Use Only.

HKI-357 is a potent, irreversible inhibitor of ErbB2 (HER2) and EGFR with IC50 values of 33 and 34 nM respectively.

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10 mg ¥2480 In stock
25 mg ¥4280 In stock
50 mg ¥7280 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

HKI-357 is a potent, irreversible inhibitor of ErbB2 (HER2) and EGFR with IC50 values of 33 and 34 nM respectively.
HKI-357 inhibits ligand-induced EGFR autophosphorylation and cell proliferation in NCI-H1975 cells containing L858R and T790M mutations.
HKI-357 demonstrate increased killing of NSCLC cells harboring an EGFR mutation, compared with cells expressing wild-type receptor.
HKI-357 is 10-fold more effective than gefitinib in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation.

物理化学性质&存储条件

分子量 574.05
分子式 C31H29ClFN5O3
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

10 mM in DMSO

Chemical Name/SMILES

(2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide

参考文献

1. Eunice L Kwak, et al. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7665-70.

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