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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-Ras-JDQ443
JDQ443

Chemical Structure : JDQ443

CAS No.: 2653994-08-0

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JDQ443 (Opnurasib, NVP-JDQ443)

货号: PC-72897Not For Human Use, Lab Use Only.

JDQ443 (Opnurasib, NVP-JDQ443) is a potent, mutant-selective, covalent KRAS G12C inhibitor.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Opnurasib (JDQ443, NVP-JDQ443) is a potent, mutant-selective, covalent KRAS G12C inhibitor.
JDQ443 promotes dose-dependent reductions of phosphorylated ERK (pERK) levels and the proliferation of the KRASG12C-mutated cell lines NCI-H358 and NCI-H2122 with IC50 of 18 and 63 nM, respectively. 
JDQ443 binds under the switch II loop with a novel binding mode, exploiting unique interactions with the KRAS G12C protein compared to sotorasib and adagrasib.
JDQ443 potently inhibits KRASG12C cellular signaling and proliferation in a mutant selective manner.
JDQ443 exhibits dose-dependent anti-tumor activity in mice bearing KRAS G12C mutated tumor xenografts comparable to sotorasib and adagrasib.
JDQ443 is orally bioavailable and is well-tolerated.
Combination of JDQ443 with the SHP2 inhibitor TNO155 further increases KRAS G12C target occupancy in vivo, enhanced pre-clinical anti-tumor activity, and delayed the emergence of resistance in xenografts.

物理化学性质&存储条件

分子量 526.03
分子式 C29H28ClN7O
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 (5.3 mg/mL)
Chemical Name/SMILES

2-Propen-1-one, 1-[6-[(4R)-4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methyl-1H-indazol-5-yl)-1H-pyrazol-1-yl]-2-azaspiro[3.3]hept-2-yl]-

参考文献

1. Saskia M. Brachmann, et al. Mol Cancer Ther (2021) 20 (12_Supplement): P124.

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