| Identification | Back Directory | [Name]
1,8-Naphthyridine-3-carbonitrile, 7-(2-amino-3,4,5,6-tetrafluorophenyl)-6-chloro-1,2-dihydro-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-2-oxo-4-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]- | [CAS]
2657613-87-9 | [Synonyms]
JAB-21822
Glecirasib
1,8-Naphthyridine-3-carbonitrile, 7-(2-amino-3,4,5,6-tetrafluorophenyl)-6-chloro-1,2-dihydro-1-[4-methyl-2-(1-methylethyl)-3-pyridinyl]-2-oxo-4-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]- | [Molecular Formula]
C31H26ClF4N7O2 | [MOL File]
2657613-87-9.mol | [Molecular Weight]
640.03 |
| Chemical Properties | Back Directory | [Boiling point ]
753.0±60.0 °C(Predicted) | [density ]
1.50±0.1 g/cm3(Predicted) | [form ]
Solid | [pka]
5.37±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Glecirasib (Compound 1-2; JAB-21822) is an orally active and potent inhibitor of KRAS G12C. The Ras family of proteins is an important intracellular signaling molecule that plays an important role in growth and development. Glecirasib has the potential for the research of KRAS G12C-mediated cancer[1][2][3][4]. | [in vivo]
Glecirasib (10 mg/kg, p.o., daily for ~3 weeks) inhibits tumor growth in NCI-H1373 xenograft mice model[1][3].
Glecirasib (400 mg/kg, p.o., daily for 22 days) has no influence on the body weight, showing good safety in NCI-H1373 xenograft mice model[1].
| Animal Model: | NCI-H1373 xenograft mice model[1] | | Dosage: | 400 mg/kg | | Administration: | p.o., daily for 22 days | | Result: | Had no significant change on the weight of the mice. |
| Animal Model: | NCI-H1373 xenograft mice model[1] | | Dosage: | 10 mg/kg | | Administration: | p.o., daily for ~3 weeks | | Result: | Decreased the tumor volume in the NCI-H1373 xenograft mice. |
| [References]
[1] Amin LI, et al. Kras mutant protein inhibitors. Patent WO2021121367A1.
[2] Li J, Shen L, Gu Y, et al. Preliminary activity and safety results of KRAS G12C inhibitor glecirasib (JAB-21822) in patients with pancreatic cancer and other solid tumors[J]. 2024.
[3] Ma C, et al. Discovery of JAB-3312, a Potent SHP2 Allosteric Inhibitor for Cancer Treatment. J Med Chem. 2024 Aug 22;67(16):13534-13549. DOI:10.1021/acs.jmedchem.4c00360
[4] Fuerst M L. Glecirasib Induces Promising Efficacy in Patients With Advanced Lung Cancer[J]. 2024. |
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