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Adagrasib

Catalog No. T8369   CAS 2326521-71-3
Synonyms: MRTX849

Adagrasib (MRTX849) is a potent, selective and covalent KRASG12C inhibitor with potential antineoplastic activity. It selectively modifies mutant cysteine 12 in GDP-bound KRASG12C, and inhibits KRAS-dependent signaling.

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Adagrasib Chemical Structure
Adagrasib, CAS 2326521-71-3
Pack Size Availability Price/USD Quantity
10 mg In stock $ 94.00
25 mg In stock $ 207.00
50 mg In stock $ 369.00
100 mg In stock $ 553.00
500 mg In stock $ 996.00
1 mL * 10 mM (in DMSO) In stock $ 94.00
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Purity: 99.9%
Purity: 99.84%
Purity: 99.59%
Purity: 99.10%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Adagrasib (MRTX849) is a potent, selective and covalent KRASG12C inhibitor with potential antineoplastic activity. It selectively modifies mutant cysteine 12 in GDP-bound KRASG12C, and inhibits KRAS-dependent signaling.
In vivo MRTX849 demonstrated pronounced tumor regression in 17 of 26 (65%) KRASG12C-positive cell line- and patient-derived xenograft models from multiple tumor types, and objective responses have been observed in patients with KRASG12C-positive lung and colon adenocarcinomas[1].
Synonyms MRTX849
Molecular Weight 604.12
Formula C32H35ClFN7O2
CAS No. 2326521-71-3

Storage

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

Solubility Information

DMSO: 100 mg/mL (165.53 mM), sonification is recommended.

TargetMolReferences and Literature

1. Jill Hallin , Lars D Engstrom , Lauren Hargis.The KRAS G12C Inhibitor MRTX849 Provides Insight Toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.Cancer Discov. 2020 Jan;10(1):54-71. 2. Jay B Fell , John P Fischer , Brian R Baer.Identification of the Clinical Development Candidate MRTX849, a Covalent KRAS G12C Inhibitor for the Treatment of Cancer.J Med Chem. 2020 Apr 6.

TargetMolCitations

1. Yang F, Wen Y, Wang C, et al. Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC. European Journal of Medicinal Chemistry. 2022: 114088 2. Yun S D, Scott E, Moghadamchargari Z, et al.2′-Deoxy Guanosine Nucleotides Alter the Biochemical Properties of Ras.Biochemistry.2023

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Kinase Inhibitor Library GPCR Compound Library Anti-Pancreatic Cancer Compound Library FDA-Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Anti-Colorectal Cancer Compound Library

Related Products

Related compounds with same targets
6H05 KRAS G12D inhibitor 14 ARS-1323-alkyne Kras4B G12D-IN-1 Glecirasib TH-Z835 KRAS G12C inhibitor 58 KRAS G12D modulator-1

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Keywords

Adagrasib 2326521-71-3 GPCR/G Protein MAPK Ras inhibit GDP-bound mutant MIA PaCa-2 selective Inhibitor MRTX 849 inactive MRTX-849 state G12C H1373 covalent MRTX849 anti-tumor KRAS cells inhibitor

 

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