Pyrotinib dimaleate (SHR-1258 dimaleate) 是有效、选择性的 EGFR/HER2 双重抑制剂，IC50 值分别为 13 nM 和 38 nM。 Pyrotinib dimaleate is a potent and selective dual inhibitor of EGFR/HER2 with IC50s of 13 and 38 nM, respectively. Information Pyrotinib (SHR-1258, BLTN, Pyrroltinib) dimaleate is a potent and selective irreversible dual tyrosine kinase inhibitor ofEGFRandHER2with IC50 of 0.013 μM and 0.038 μM, respectively. Targets EGFR (Cell-free assay); HER2 (Cell-free assay) 0.013 μM; 0.038 μM In vitro Pyrotinib (SHR1258), as an EGFR/HER2 dual tyrosine kinase inhibitor, shows excellent in vitro potency, selectivity, and favorable PK profiles. In vivo Pyrotinib (SHR1258) displays robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human. Cell Research(from reference) Cell lines：A431, SK-BR-3, NCI-N87 Concentrations：6-7 concentrations (not specific) Incubation Time：72 h
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Pyrotinib dimaleate
CAS number：1397922-61-0 molecular formula：C40H39ClN6O11
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| Chinese alias | 吡咯替尼二马来酸酯 | ||
| English alias | (E)-N-[4-[[3-chloro-4-(2-pyridylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolyl]-3-[(2R)-1-methylpyrrolidin-2-yl]prop-2-enamide dimaleate | UNII-85KUE857XM | Pyrotinib Maleate | SCHEMBL19512296 | Pyrotinib dimaleate | 2-Propenamide, N-(4-((3-chloro-4-(2 | ||
| CAS number | 1397922-61-0 | molecular formula | C40H39ClN6O11 |
| molecular weight | 815.22 g/mol | Exact mass | - |
| PSA | 262.000 Ų | logp | - |
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