MRTX 849

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Description: Mutation-selective inhibitor of KRASG12C
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)
Datasheet
Citations
Reviews
Literature (4)
Pathways (1)

Biological Activity for MRTX 849

MRTX 849 is a mutant-selective inhibitor of KRASG12C (IC50 = 142 nM). MRTX 849 covalently binds to KRASG12C 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%) KRASG12C -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 Data 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.

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

Hallin et al (2020) The KRAS G12C inhibitor MRTX849 provides insight toward therapeutic susceptibility of KRAS-mutant cancers in mouse models and patients. Cancer Discov. 10 54 PMID: 31658955

Fell et al (2020) Identification of the clinical development candidate MRTX849, a covalent KRASG12C inhibitor for the treatment of cancer. J.Med.Chem. 63 6679 PMID: 32250617


If you know of a relevant reference for MRTX 849, please let us know.

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Keywords: MRTX 849, MRTX 849 supplier, MRTX, 849, potent, mutation-selective, inhibitors, inhibits, KRASG12C, Ras, GTPases, 7488, Tocris Bioscience

Citations for MRTX 849

Citations are publications that use Tocris products.

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Reviews for MRTX 849

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Cancer Research Product Guide

Cancer Research Product Guide

A collection of over 750 products for cancer research, the guide includes research tools for the study of:

  • Cancer Metabolism
  • Epigenetics in Cancer
  • Receptor Signaling
  • Cell Cycle and DNA Damage Repair
  • Angiogenesis
  • Invasion and Metastasis
RAS Oncoproteins Scientific Review

RAS Oncoproteins Scientific Review

Written by Kirsten L. Bryant, Adrienne D. Cox and Channing J. Der, this review provides a comprehensive overview of RAS protein function and RAS mutations in cancer. Key signaling pathways are highlighted and therapeutic vulnerabilities are explored. This review also includes a detailed section on RAS drug discovery and targeting synthetic lethal interactors of mutant RAS. Compounds available from Tocris are listed.

Cell Cycle & DNA Damage Repair Poster

Cell Cycle & DNA Damage Repair Poster

In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. Adapted from the 2015 Cancer Product Guide, Edition 3, this poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.

Epigenetics in Cancer Poster

Epigenetics in Cancer Poster

Adapted from the 2015 Cancer Product Guide Edition 3, this poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.

Pathways for MRTX 849

Akt Signaling Pathway

Akt Signaling Pathway

The Akt signaling pathway plays a key role in the mediation of protein synthesis, metabolism, proliferation and cell cycle progression. It may be referred to as a 'prosurvival' pathway.
MAPK Signaling Pathway

MAPK Signaling Pathway

The mitogen-activated protein kinase pathway evokes an intracellular signaling cascade in response to extracellular stimuli such as heat and stress. It can influence cell division, metabolism and survival.