GDC-6036 (Divarasib, RG6330) | KRAS G12C inhibitor | Probechem Biochemicals

Chemical Structure : GDC-6036

CAS No.: 2417987-45-0

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GDC-6036 (Divarasib, RG6330, GDC6036, RG 6330)

货号: PC-73323Not For Human Use, Lab Use Only.

GDC-6036 (Divarasib, RG6330) is a potent, selective, covalent and orally available KRAS G12C inhibitor with HTRF IC50 of 2.9 pM.

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5 mg	￥2180	In stock
10 mg	￥3580	In stock
25 mg	￥5580	In stock
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100 mg		Get quote

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生物&药学活性

GDC-6036 (Divarasib, RG6330) is a potent, selective, covalent and orally available KRAS G12C inhibitor with HTRF IC50 of 2.9 pM.

GDC-6036 inhibits NCI-HCC1171 Alkylation with IC50 of 0.32 nM.

GDC-6036 is more potent and selective in vitro than other clinical KRAS G12C inhibitors (Sotorasib, Adagrasib).

GDC-6036 irreversibly alkylates KRAS G12C and locks it in the inactive GDP-bound state.

GDC-6036 shows a median IC50 in the sub-nanomolar range (IC50=0.18 uM) and greater than 18,000-fold selectivity for G12C versus non-G12C cell lines.

GDC-6036 (5 mg/kg QD) demonstrates complete tumor growth inhibition in multiple KRAS G12C-positive cell lines and in xenograft mouse models.

GDC-6036 is in Phase 1 clinical development (NCT04449874) as monotherapy and in multiple combinations with other agents, including SHP2 inhibitor GDC-1971 (Cat# PC-20047).

物理化学性质&存储条件

分子量	622.066
分子式	C29H32ClF4N7O2
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-((3S)-4-(7-(6-amino-4-methyl-3-(trifluoromethyl)pyridin-2-yl)-6-chloro-8-fluoro-2-(((S)-1-methylpyrrolidin-2-yl)methoxy)quinazolin-4-yl)-3-methylpiperazin-1-yl)prop-2-en-1-one

参考文献

1. Hans Purkey. Cancer Res (2022) 82 (12_Supplement): ND11.

GDC-6036 (Divarasib, RG6330, GDC6036, RG 6330)

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GDC-6036 (Divarasib, RG6330, GDC6036, RG 6330)

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