SHR1258
- CAS No.
- 1269662-73-8
- Chemical Name:
- SHR1258
- Synonyms
- SHR1258;HTI-1001;SHR-1258;Pyrotinib;SHR-1258;SHR1258;Pyrotinib (SHR-1258);Pyrotinib (free base);(R,E)-N-(4-((3-Chloro-4-(pyridin-2-ylmethoxy)phenyl)amino)-3-cyano-7-ethoxyquinolin-6-yl)-3-(1-methylpyrrolidin-2-yl)acrylamide;2-Propenamide, N-[4-[[3-chloro-4-(2-pyridinylmethoxy)phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-3-[(2R)-1-methyl-2-pyrrolidinyl]-, (2E)-
- CBNumber:
- CB33159982
- Molecular Formula:
- C32H31ClN6O3
- Molecular Weight:
- 583.08
- MDL Number:
- MOL File:
- 1269662-73-8.mol
| 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) |
| pka | 12.30±0.43(Predicted) |
| form | Solid |
| color | Light yellow to yellow |
| FDA UNII | CJN36EQM0H |
| NCI Drug Dictionary | pyrotinib |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H312-H332 |
| Precautionary statements | P280 |
SHR1258 Chemical Properties,Uses,Production
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)
