| Identification | Back Directory | [Name]
1H-Pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione, 11-chloro-10-(2-fluoro-6-hydroxyphenyl)-2,3,4,4a,6,8-hexahydro-6-methyl-8-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-3-(1-oxo-2-propen-1-yl)-, (4aR,8R)- | [CAS]
2641747-54-6 | [Synonyms]
GFH925）
Fulzerasib
Fulzerasib（IBI351
Fulzerasib (IBI351，GFH925)
1H-Pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione, 11-chloro-10-(2-fluoro-6-hydroxyphenyl)-2,3,4,4a,6,8-hexahydro-6-methyl-8-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-3-(1-oxo-2-propen-1-yl)-, (4aR,8R)- | [Molecular Formula]
C32H30ClFN6O4 | [MOL File]
2641747-54-6.mol | [Molecular Weight]
617.07 |
| Chemical Properties | Back Directory | [Boiling point ]
819.5±65.0 °C(Predicted) | [density ]
1.49±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
6.74±0.35(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Fulzerasib (GFH925) is an irreversible KRAS G12C inhibitor, has a synergistic anti-cancer effect with cetuximab (HY-P9905).[1][2]. | [in vivo]
Fulzerasib shows strong anti-tumor activity in various models, including the pancreatic cancer cell line MIA Paca-2 CDX, human lung adenocarcinoma NCI-H358 CDX, patient-derived xenograft colon adenocarcinoma SW837 CDX, and lung cancer LU2529 PDX[1]. | [IC 50]
KRAS(G12C) | [References]
[1] Rafael Rosell, et al. KRAS G12C-mutant driven non-small cell lung cancer (NSCLC). Crit Rev Oncol Hematol. 2024 Mar:195:104228. DOI:10.1016/j.critrevonc.2023.104228
[2] Vanesa Gregorc, et al. KROCUS: A phase II study investigating the efficacy and safety of fulzerasib. Free access.June 05, 2024 |
| Spectrum Detail | Back Directory | [Spectrum Detail]
1H-Pyrazino[1',2':4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione, 11-chloro-10-(2-fluoro-6-hydroxyphenyl)-2,3,4,4a,6,8-hexahydro-6-methyl-8-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-3-(1-oxo-2-propen-1-yl)-, (4aR,8R)-(2641747-54-6)1HNMR
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