MRTX 849

Key Product Details

Product Description

MRTX 849 is a mutant-selective inhibitor of KRAS^G12C (IC₅₀ = 142 nM). MRTX 849 covalently binds to KRAS^G12C at the cysteine 12 residue and inhibits KRAS-dependent signal transduction by locking the protein in its inactive GDP-bound state. MRTX 849 induces pronounced tumor regression in 17 of 26 (65%) KRAS^G12C -positive cell lines and patient-derived xenograft models from multiple tumor types. It is orally bioavailable.

Product Specifications for MRTX 849

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for MRTX 849

The following data is based on the product molecular weight 604.13.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.66 mL	8.28 mL	16.55 mL
5 mM	0.33 mL	1.66 mL	3.31 mL
10 mM	0.17 mL	0.83 mL	1.66 mL
50 mM	0.03 mL	0.17 mL	0.33 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Fell Identification of the clinical development candidate MRTX849, a covalent KRASG12C inhibitor for the treatment of cancer. J.Med.Chem. 2020 PMID: 32250617
• Hallin The KRAS G12C inhibitor MRTX849 provides insight toward therapeutic susceptibility of KRAS-mutant cancers in mouse models and patients. Cancer Discov. 2020 PMID: 31658955

Product Documents for MRTX 849