(Rac)-Opnurasib
(Rac)-Opnurasib ((Rac)-JDQ-443; (Rac)-NVP-JDQ443) is the levorotomer of Opnurasib (HY-139612). Opnurasib is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity.
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- CAS No.: 2653201-38-6
- Formule: C29H28ClN7O
- Masse moléculaire:526.03
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
[1]|
KRas G12C |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1437 | GI50 |
4.4 μM
Compound: 21; JDQ443
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Antiproliferative activity against human NCI-H1437 cells by resazurin assay
Antiproliferative activity against human NCI-H1437 cells by resazurin assay
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[PMID: 36399068] |
In Vitro
Opnurasib traps the GDP-bound inactive conformation of KRAS[1].
Opnurasib 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 values of 0.018 and 0.063 μM, respectively[2].
Opnurasib covalently and selectively binds and inhibits GDP-bound KRASG12C with low reversible binding affinity to the RAS switch II pocket, and also inhibits proliferation of KRASG12C-mutated and KRAS G12C/H95, G12C/R68S, and G12C/Y96 double-mutant cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Opnurasib (Orally, 100 mg/kg, daily (JDQ443) + 7.5 mg/kg, twice daily (TNO155), for 36 days) shows greater cell growth inhibition or cell killing compared with single-agent JDQ443 when combined with TNO155[2].
Opnurasib generates categorical antitumor responses in PDX models of NSCLC and colorectal tumors that are improved by combination treatment with other agents[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2653201-38-6
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Masse moléculaire 526.03
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Formule C29H28ClN7O
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SMILES
O=C(N1CC2(CC(C2)N3N=C(C(C4=C5C=NNC5=CC(C)=C4Cl)=C3C)C6=CC=C7C(C=NN7C)=C6)C1)C=C
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Synonyms
(Rac)-JDQ-443; (Rac)-NVP-JDQ443
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. LIU BO, et al. PYRAZOLYL DERIVATIVES USEFUL AS ANTI-CANCER AGENTS. Patent WO2021120890A1.
[2]. Weiss A, Lorthiois E, Barys L, et al. Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent and Selective, Covalent Oral Inhibitor of KRASG12C. Cancer Discov. 2022;candisc.0158.2022. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(Rac)-Opnurasib Related Classifications
HY-139612B Related Classifications
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