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)-

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)- Suppliers list
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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)- Basic information
Product 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)-
Synonyms: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)-;Fulzerasib(IBI351;GFH925);Fulzerasib (IBI351,GFH925);Fulzerasib (GFH925);IBI351;Fulzerasib;(4aR,8R)-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)-1H-pyrazino[1′,2′:4,5]pyrazino[2,3-c][1,8]naphthyridine-5,7-dione (ACI)
CAS:2641747-54-6
MF:C32H30ClFN6O4
MW:617.07
EINECS:
Product Categories:
Mol File:2641747-54-6.mol
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)- Structure
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)- Chemical Properties
Boiling point 819.5±65.0 °C(Predicted)
density 1.49±0.1 g/cm3(Predicted)
form Solid
pka6.74±0.35(Predicted)
color Light yellow to yellow
Safety Information
MSDS Information
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)- Usage And Synthesis
UsesFulzerasib (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 50KRAS(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
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)- Preparation Products And Raw materials
Tag: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) Related Product Information
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)- Glecirasib NA 1,8-Naphthyridine-3-carbonitrile, 7-(3-chloro-2-fluoro-6-hydroxyphenyl)-6-fluoro-1,2-dihydro-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-2-oxo-4-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]- Glecirasib KRAS mutant protein inhibitor 1