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Submit ReviewMRTX 849
Description: Mutation-selective inhibitor of KRASG12C
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)
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.
| 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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Product Datasheets for MRTX 849
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, KRAS, G12C, Adagrasib, Ras, GTPases, 7488, Tocris Bioscience
Citations 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.
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Pathways for MRTX 849
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.