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1269662-73-8

1269662-73-8 Structure

1269662-73-8 Structure
IdentificationBack Directory
[Name]

SHR1258
[CAS]

1269662-73-8
[Synonyms]

SHR1258
SHR-1258
HTI-1001
Pyrotinib
SHR-1258;SHR1258
Pyrotinib (SHR-1258)
Pyrotinib (free base)
2-Propenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2E)-
[Molecular Formula]

C32H31ClN6O3
[MOL File]

1269662-73-8.mol
[Molecular Weight]

583.08
Chemical PropertiesBack Directory
[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)
[form ]

Solid
[pka]

12.30±0.43(Predicted)
[color ]

Light yellow to yellow
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H312-H332
[Precautionary statements ]

P280
Hazard InformationBack Directory
[Uses]

Pyrotinib, 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 50]

EGFR: 13 nM (IC50); HER2: 38 nM (IC50)
[storage]

Store at -20°C
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