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Chemical Structure : HKI-357
CAS No.: 848133-17-5
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $298 | In stock | |
| 10 mg | $488 | In stock | |
| 25 mg | $798 | In stock | |
| 100 mg | Get quote |
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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.
| M.Wt | 574.05 | |
| Formula | C31H29ClFN5O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide |
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1. Eunice L Kwak, et al. Proc Natl Acad Sci U S A. 2005 May 24;102(21):7665-70.
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