Cat. No. Name Size Price Add Cart
KI2535HKI35710 mg$585
HKI35750 mg$2457

Chemical Characteristic

Product NameHKI357
SynonymsN/A
CAS No.848133-17-5
Molecular Weight 574.05
FormulaC31H29ClFN5O3
Chemical Name?(2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
Smilesc1(c(cc2c(c1)c(c(cn2)C#N)Nc1ccc(c(c1)Cl)OCc1cccc(c1)F)OCC)NC(=O)/C=C/CN(C)C
Chemical Structure

Biological activities

HKI357 is a dual inhibitor of EGFR and ERBB2. HKI357 inhibits EGFR and ERBB2 with IC50s of 34 and 33 nM, respectively. HKI357 is 10-fold more effective than gefitinib in suppressing EGFR autophosphorylation.[1]

References

[1] Kwak EL, et al. Irreversible inhibitors of the EGF receptor may circumvent acquired resistance to gefitinib. Proc Natl Acad Sci U S A. 2005, 102(21): 7665-7670.

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