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Opnurasib (JDQ-443) K-Ras inhibitor

Name: Opnurasib (JDQ-443)
Brand: Selleck Chemicals
SKU: E1056
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.E1056

Opnurasib (JDQ-443,NVP-JDQ443) , a potent and selective, orally bioavailable covalent inhibitor of GDP-bound KRAS^G12C with an IC50 of 0.012 µM for inhibition of c-Raf recruitment.

Chemical Structure

Molecular Weight: 526.03

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Quality Control

Batch: Purity: 99.33%

99.33

Related Targets	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras Aurora Kinase Casein Kinase
Other K-Ras Products	Adagrasib (MRTX849) MRTX1133 BI-2852 RMC-7977 HRS-4642 Daraxonrasib (RMC-6236) Zoldonrasib (RMC-9805) ARS-1620 ARS-853 BI-3406

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (190.1 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (9.51mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.650mg/ml (1.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	526.03	Formula	C₂₉H₂₈CIN₇O	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	2653994-08-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

Targets/IC₅₀/Ki	KRAS(G12C) 0.012 μM
References	[1] https://pubmed.ncbi.nlm.nih.gov/35404998/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05445843	Recruiting	Locally Advanced or Metastatic KRAS G12C-mutated NSCLC With a PD-L1 Expression <1% or a PD-L1 Expression ≥ 1% and an STK11 Co-mutation	Novartis Pharmaceuticals\|Novartis	December 6 2022	Phase 2
NCT05132075	Recruiting	Non-Small Cell Lung Cancer	Novartis Pharmaceuticals\|Novartis	June 15 2022	Phase 3
NCT05329623	Recruiting	Small Cell Lung Carcinoma	Novartis Pharmaceuticals\|Novartis	May 3 2022	Phase 1
NCT04699188	Recruiting	KRAS G12C Mutant Solid Tumors\|Carcinoma Non-Small-Cell Lung\|Carcinoma Colorectal\|Cancer of Lung\|Cancer of the Lung\|Lung Cancer\|Neoplasms Lung\|Neoplasms Pulmonary\|Pulmonary Cancer\|Pulmonary Neoplasms	Novartis Pharmaceuticals\|Novartis	February 24 2021	Phase 1\|Phase 2

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Handling Instructions

Tel: +1-832-582-8158 Ext:3

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