Welcome to Shanghai Probechem Biochemicals Co Ltd !Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : JDQ443
CAS No.: 2653994-08-0
Catalog No.: PC-72897Not For Human Use, Lab Use Only.
JDQ443 (Opnurasib, NVP-JDQ443) is a potent, mutant-selective, covalent KRAS G12C inhibitor.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $258 | In stock | |
| 10 mg | $398 | In stock | |
| 25 mg | $558 | In stock | |
| 100 mg | Get quote | ||
| 200 mg | Get quote | ||
| 1 g | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
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.
| M.Wt | 526.03 | |
| Formula | C29H28ClN7O | |
| Appearance | Solid | |
| Storage |
|
|
| 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]- |
|
1. Saskia M. Brachmann, et al. Mol Cancer Ther (2021) 20 (12_Supplement): P124.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
