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  3. Opnurasib

Opnurasib  (Synonyms: JDQ-443; NVP-JDQ443)

Cat. No.: HY-139612 Purity: 98.94%
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Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity.

For research use only. We do not sell to patients.

Opnurasib Chemical Structure

Opnurasib Chemical Structure

CAS No. : 2653994-08-0

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Based on 1 publication(s) in Google Scholar

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Description

Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor (extracted from patent WO2021120890A1). Opnurasib shows antitumor activity[1][2].

IC50 & Target[1]

KRas G12C

 

In Vitro

Opnurasib (NVP-JDQ443) 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

Cell Line: Ba/F3 cells[2]
Concentration: 0, 0.3, 1 μM
Incubation Time: 30 min, 4 h
Result: Inhibited signaling (pERK) and proliferation of the KRAS G12C/H95 double mutants G12C/H95R and G12C/H95Q.
In Vivo

Opnurasib (10-100 mg/kg, Orally, daily for 14 days) shows antitumor activity in KRAS G12C-mutated CDX models[2].
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: KRAS G12C tumor-bearing nude mice (MIA PaCa-2 (PDAC); NCIH2122, LU99, HCC44, NCI-H2030 (NSCLC); and KYSE410 (esophageal cancer))[2]
Dosage: 10, 30, 100 mg/kg
Administration: Orally, daily for 14 days
Result: Inhibited the growth of all models in a dose-dependent manner.
Animal Model: Three KRAS G12C-mutated CDX models (LU99, NCI-H2030, and KYSE410)[2]
Dosage: 100 mg/kg (JDQ443) + 7.5 mg/kg (TNO155)
Administration: Orally, daily (JDQ443) or twice daily (TNO155), for 36 days
Result: Combined with TNO155, showed either greater tumor efficacy compared with each agent alone (H2030, KYSE410) or a delayed time to tumor progression (LU99).
Clinical Trial
Molecular Weight

526.03

Appearance

Solid

Formula

C29H28ClN7O

CAS No.
SMILES

O=C(N1CC2(CC(C2)N3N=C([[email protected]]([[email protected]]4=C(Cl)C(C)=CC5=C4C=NN5)=C3C)C6=CC=C7C(C=NN7C)=C6)C1)C=C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 80 mg/mL (152.08 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9010 mL 9.5052 mL 19.0103 mL
5 mM 0.3802 mL 1.9010 mL 3.8021 mL
10 mM 0.1901 mL 0.9505 mL 1.9010 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.95 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.94%

References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Opnurasib
Cat. No.:
HY-139612
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