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Chemical Structure : Theliatinib
CAS No.: 1353644-70-8
Catalog No.: PC-62121Not For Human Use, Lab Use Only.
Theliatinib (HMPL309) is a highly selective, potent, ATP-competitive inhibitor of EGFR with IC50 of 3 nM/22 nM for EGFR/EGFRT790M/L858R mutant, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $188 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $488 | In stock | |
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| 100 mg | Get quote |
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Theliatinib (HMPL309) is a highly selective, potent, ATP-competitive inhibitor of EGFR with IC50 of 3 nM/22 nM for EGFR/EGFRT790M/L858R mutant, respectively.
Theliatinib (HMPL309) demonstrates 50-fold greater selectivity for EGFR compared to 72 other kinases.
Theliatinib (HMPL309) inhibits EGFR phosphorylation (IC50=7 nM) and cell survival in tumor cells
Theliatinib (HMPL309) shows in vivo activity in multiple xerographs such as A-431, Bcap-37 and Fadu; generally well tolerated in animals and orally bioactive.
| M.Wt | 442.523 | |
| Formula | C25H26N6O2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(3aR,6aR)-N-(4-((3-ethynylphenyl)amino)-7-methoxyquinazolin-6-yl)-1-methylhexahydropyrrolo[3,4-b]pyrrole-5(1H)-carboxamide |
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1. Ren Y, et al. Oncotarget. 2017 Apr 19;8(31):50832-50844.
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