MRTX 849

Name: MRTX 849
Brand: Tocris Bioscience
SKU: 7488

Tocris Bioscience, part of Bio-Techne | Catalog # 7488

COA / SDS

Mutation-selective inhibitor of KRASG12C

Key Product Details

Description:	Mutation-selective inhibitor of KRAS^G12C
Alternative Names:	Adagrasib
Chemical Name:	4-[7-(8-Chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoro-1-oxo-2-propen-1-yl)-(2S)-2-piperazineacetonitrile
Purity:	≥98% (HPLC)
Molecular Weight:	604.13

View Full Technical Details for MRTX 849

Technical Data
Citations

Biological Activity for MRTX 849

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.

Technical Data for MRTX 849

M. Wt	604.13
Formula	C₃₂H₃₅ClFN₇O₂
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2326521-71-3
PubChem ID	138611145
InChi Key	PEMUGDMSUDYLHU-ZEQRLZLVSA-N
Smiles	O(C[C@@H]1CCCN1C)C2=NC(=C3C(CN(CC3)C=4C5=C(C=CC4)C=CC=C5Cl)=N2)N6C[C@H](CC#N)N(C(C(=C)F)=O)CC6

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

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for MRTX 849

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	60.41	100
	ethanol	60.41	100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for MRTX 849

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