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Opnurasib

Catalog No. T40292 CAS 2653994-08-0

Synonyms: NVP-JDQ443, JDQ-443, Opnurasib

Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.

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Opnurasib, CAS 2653994-08-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 107.00
5 mg	In stock	$ 372.00
10 mg	In stock	$ 555.00
25 mg	In stock	$ 893.00
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 428.00

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Purity: 98.88%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.
In vitro	Opnurasib selectively forms a covalent bond with and inhibits GDP-bound KRASG12C, demonstrating a low reversible binding affinity to the RAS switch II pocket. Additionally, it effectively hinders the proliferation of cell lines carrying KRASG12C mutations, as well as those with double mutations G12C/H95, G12C/R68S, and G12C/Y96.[2] Opnurasib induces dose-dependent decreases in phosphorylated ERK (pERK) levels and inhibits the proliferation of KRASG12C-mutated cell lines NCI-H358 and NCI-H2122, exhibiting IC50 values of 0.018 and 0.063 μM, respectively.[2]
In vivo	Opnurasib elicits distinct antitumor responses in patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal tumors, and these responses are further enhanced when Opnurasib is used in combination with other therapeutic agents.[2]

Synonyms	NVP-JDQ443, JDQ-443, Opnurasib
Molecular Weight	526.03
Formula	C29H28ClN7O
CAS No.	2653994-08-0

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 70 mg/mL (133.07 mM), Sonication is recommended.

References and Literature

1. LIU BO, et al. PYRAZOLYL DERIVATIVES USEFUL AS ANTI-CANCER AGENTS. WO2021120890A1. 2. Weiss A, 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 Jun 2;12(6):1500-1517.

Related compound libraries

This product is contained In the following compound libraries：

Membrane Protein-targeted Compound Library GPCR Compound Library

Related Products

Related compounds with same targets

KRAS G12C inhibitor 17 CID44216842 EHop-016 KRAS G12C inhibitor 32 SOS1/KRAS-IN-1 ML-210 ML-099 Methylophiopogonanone B

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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 add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Opnurasib 2653994-08-0 GPCR/G Protein MAPK Ras JDQ 443 NVP-JDQ443 JDQ-443 NVP-JDQ-443 NVP-JDQ 443 JDQ443 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.