SHR1258

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SHR1258 Basic information
Product Name:SHR1258
Synonyms:SHR1258;SHR-1258;SHR1258;Pyrotinib (SHR-1258);2-Propenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2E)-;Pyrotinib (free base);HTI-1001;(R,E)-N-(4-((3-Chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide;Pyrotinib
CAS:1269662-73-8
MF:C32H31ClN6O3
MW:583.08
EINECS:
Product Categories:
Mol File:1269662-73-8.mol
SHR1258 Structure
SHR1258 Chemical Properties
Boiling point 775.5±60.0 °C(Predicted)
density 1.35±0.1 g/cm3(Predicted)
storage temp. Store at -20°C
solubility DMSO : 0.172 mg/mL (0.29 mM)
pka12.30±0.43(Predicted)
form Solid
color Light yellow to yellow
Safety Information
MSDS Information
SHR1258 Usage And Synthesis
UsesPyrotinib, is a potent and selective EGFR/HER2 dual inhibitor.
in vivo

Pyrotinib has acceptable bioavailability of 20.6%, 43.5% and 13.5% in nude mice, rats and dogs, respectively. The TGI % (tumor growth inhibition) of Pyrotinib on day 21 is 109%, 157%, 159% at the doses of 5 mg/kg, 10 mg/kg, 20 mg/kg respectively. Pyrotinib in SK-OV-3 ovarian xenograft model shows TGI% on day 21 of 2%, 12%, 83% at the doses of 2.5 mg/kg, 5 mg/kg, 10 mg/kg respectively), which further confirms its robust in vivo antitumor efficacy at 10 mg/kg[1].

IC 50EGFR: 13 nM (IC50); HER2: 38 nM (IC50)
Tag:SHR1258(1269662-73-8) Related Product Information
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