Pyrotinib maleate

Research use only, not for human use.

Pyrotinib maleate (SHR-1258 maleate)is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively.

Pyrotinib maleate (SHR-1258 maleate)is a potent and selective EGFR/HER2 dual inhibitor with IC50 of 13/38 nM, respectively; displays high selectivity in a panel of different kinases such as KDR, c-Kit, PDGFRβ, c-Src and c-Met (c-Src with an IC50 of 790 nM, and others >3,000 nM); exhibits robust anti-tumor effects on HER2-overexpressing xenograft models and sufficiently safety windows in animals as well as favorable pharmacokinetic properties in human.Breast Cancer Phase 3 Clinical

SHR-1258 maleate;SHR1258 maleate

Angiogenesis

EGFR

EGFR

Cancer

Breast Cancer

1397922-61-0

699.16

C36H35ClN6O7

>98% (HPLC)

H2O : ≥ 106 mg/mL 130.03 mM

CCOC1=C(C=C2C(=C1)N=CC(=C2NC3=CC(=C(C=C3)OCC4=CC=CC=N4)Cl)C#N)NC(=O)C=CC5CCCN5C.C(=CC(=O)O)C(=O)O.C(=CC(=O)O)C(=O)O

(R,E)-N-(4-((3-chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide dimaleate

(-20℃)

With Ice Pack

≥ 2 years