MRTX 849
Tocris Bioscience, part of Bio-Techne | Catalog # 7488
Mutation-selective inhibitor of KRASG12C
Key Product Details
Description
Mutation-selective inhibitor of KRASG12C
Alternative Names
Adagrasib
Product Description
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.Product Specifications
Molecular Weight
604.13
Formula
C32H35ClFN7O2
Storage
Store at -20°C
Purity
≥98% (HPLC)
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
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.
Solubility
| 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 all 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for MRTX 849
For research use only
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