ChemicalBook > Product Catalog > Pharmaceutical intermediates > Heterocyclic compound > Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[(4aS)-8-chloro-10-fluoro-2,3,4,4a,5,6-hexahydro-12-oxo-3-(1-oxo-2-propen-1-yl)-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-, (4R)-
Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[(4aS)-8-chloro-10-fluoro-2,3,4,4a,5,6-hexahydro-12-oxo-3-(1-oxo-2-propen-1-yl)-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-, (4R)-
Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[(4aS)-8-chloro-10-fluoro-2,3,4,4a,5,6-hexahydro-12-oxo-3-(1-oxo-2-propen-1-yl)-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-, (4R)- Basic information
- Product Name:
- Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[(4aS)-8-chloro-10-fluoro-2,3,4,4a,5,6-hexahydro-12-oxo-3-(1-oxo-2-propen-1-yl)-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-, (4R)-
- Synonyms:
-
- Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[(4aS)-8-chloro-10-fluoro-2,3,4,4a,5,6-hexahydro-12-oxo-3-(1-oxo-2-propen-1-yl)-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-, (4R)-
- Olomorasib
- Olomorasib/KRAS G12C inhibitor 19
- CAS:
- 2771246-13-8
- MF:
- C25H19ClF2N4O3S
- MW:
- 528.96
- Mol File:
- 2771246-13-8.mol
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Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[(4aS)-8-chloro-10-fluoro-2,3,4,4a,5,6-hexahydro-12-oxo-3-(1-oxo-2-propen-1-yl)-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-, (4R)- Chemical Properties
- Boiling point:
- 815.8±65.0 °C(Predicted)
- Density
- 1.56±0.1 g/cm3(Predicted)
- pka
- -1.15±0.20(Predicted)
- form
- Solid
- color
- White to off-white
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Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[(4aS)-8-chloro-10-fluoro-2,3,4,4a,5,6-hexahydro-12-oxo-3-(1-oxo-2-propen-1-yl)-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-, (4R)- Usage And Synthesis
Uses
Olomorasib is a potent inhibitor of KRAS G12C. Olomorasib significantly inhibits tumor growth (extracted from patent WO2021118877A1)[1].
in vivo
Olomorasib (12.5-100 mg/kg, single dose) inhibits pERK and KRas in mouse models, showing a time- and dose-dependent effect[1].
| Animal Model: | H358 tumor xenograft mouse model [1] |
| Dosage: | 12.5, 25, 50, 100 mg/kg; 30 mg/kg; single dose |
| Administration: | |
| Result: | Exhibited good inhibition of pERK and active KRas after a single dose treatment from 12.5 to 100 mg/kg. 82.2%-90.6 % pERK inhibition, and 73.4%-94% active KRas inhibition were observed at these dose levels. Showed at 30 mg/kg, 82.6% pERK inhibition observed at 8 hours, and the pERK inhibition decreased to 65.2% at 24 hours. For active KRas, 80.2% inhibition was achieved at 8 hours, and the active KRas inhibition decreased to 54.9% at 24 hours. |
| Animal Model: | Pancreatic Cancer MiaPaca-2 Xenograft Mouse Model[1] |
| Dosage: | 5, 10, 30 mg/kg; single dose |
| Administration: | |
| Result: | Showed dose and time dependent inhibition of pERK and active KRas in MiaPaca-2 model. |
References
[1] Serge Louis Boulet, et al. Kras g12c inhibitors. Patent WO2021118877A1.
Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[(4aS)-8-chloro-10-fluoro-2,3,4,4a,5,6-hexahydro-12-oxo-3-(1-oxo-2-propen-1-yl)-1H,12H-pyrazino[2,1-d][1,5]benzoxazocin-9-yl]-7-fluoro-, (4R)-Supplier
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