Adagrasib (MRTX849)

Catalog No.S8884

For research use only.

Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.

Adagrasib (MRTX849) Chemical Structure

CAS No. 2326521-71-3

Selleck's Adagrasib (MRTX849) has been cited by 5 Publications

Purity & Quality Control

Choose Selective Ras Inhibitors

Biological Activity

Description Adagrasib (MRTX849) is a potent, selective, and covalent KRASG12C inhibitor that exhibits favorable drug-like properties, selectively modifies mutant cysteine 12 in GDP-bound KRASG12C and inhibits KRAS-dependent signaling.
Targets
K-Ras(G12C) [1]
In vitro

To evaluate the breadth of MRTX849 activity, its effect on cell viability is determined across a panel of 17 KRASG12C-mutant and three non-KRASG12C-mutant cancer cell lines using 2D (3-day, adherent cells) and 3D (12-day, spheroids) cell growth conditions. MRTX849 potently inhibits cell growth in the vast majority of KRASG12C-mutant cell lines with IC50 values ranging between 10 nM and 973 nM in the 2D format and between 0.2 nM and 1042 nM in the 3D format.[1].

In vivo

Rapid tumor regression is observed at the earliest posttreatment tumor measurement and animals in the 30 mg/kg and 100 mg/kg cohorts exhibits evidence of a complete response at study Day 15. Dosing is stopped at study Day 16 and all 4 mice in the 100 mg/kg cohort and 2 out of 7 mice in the 30 mg/kg cohort remains tumor-free through study Day 70.[1].

Protocol (from reference)

Cell Research:

[1]

  • Cell lines: MIA PaCa-2, H1373, H358, H2122, SW1573, H2030, KYSE-410 cells (G12C); H1299 (WT); A549 (G12S), HCT116 (G13D) cells
  • Concentrations: --
  • Incubation Time: 24 h
  • Method:

    All cell lines were maintained at 37 ℃ in a humidified incubator at 5% CO2 and were periodically checked for mycoplasma. CellTiter-Glo assay to evaluate cell viability performed on seven KRAS G12C-mutant cell lines and three non-KRAS G12C-mutant cell lines cells grown in 2D tissue culture conditions in a 3-day assay or 3D conditions using 96-well, ULA plates in a 12-day assay.

Animal Research:

[1]

  • Animal Models: MIA PaCa-2 model
  • Dosages: 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 604.12
Formula

C32H35ClFN7O2

CAS No. 2326521-71-3
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CCCC1COC2=NC3=C(CCN(C3)C4=CC=CC5=C4C(=CC=C5)Cl)C(=N2)N6CCN(C(C6)CC#N)C(=O)C(=C)F

In vivo Formulation Calculator (Clear solution)

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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
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05375994 Not yet recruiting Drug: VS-6766 and adagrasib Non Small Cell Lung Cancer|KRAS Activating Mutation|Advanced Cancer|Metastatic Cancer|Malignant Neoplasm of Lung|Malignant Neoplastic Disease Verastem Inc.|Mirati Therapeutics Inc. August 1 2022 Phase 1|Phase 2
NCT04685135 Recruiting Drug: MRTX849|Drug: Docetaxel Metastatic Non Small Cell Lung Cancer|Advanced Non Small Cell Lung Cancer Mirati Therapeutics Inc. April 1 2021 Phase 3
NCT04418661 Recruiting Drug: SAR442720|Drug: Pembrolizumab|Drug: Adagrasib Metastatic Neoplasm Sanofi|Revolution Medicines Inc.|Mirati Therapeutics Inc. June 9 2020 Phase 1|Phase 2
NCT04330664 Active not recruiting Drug: MRTX849|Drug: TNO155 Advanced Cancer|Metastatic Cancer|Malignant Neoplastic Disease Mirati Therapeutics Inc.|Novartis April 22 2020 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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