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Adagrasib

CAT: 0804-HY-130149-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-130149-01Size:5 mg
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Description
Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction[1][2].
CAS Number
2326521-71-3
Product Name Alternative
MRTX849
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Ras
Type
Reference compound
Related Pathways
GPCR/G Protein; MAPK/ERK Pathway
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/mrtx849.html
Concentration
10mM
Purity
99.79
Solubility
DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
N#CC[C@@H]1N(C(C(F)=C)=O)CCN(C2=C3C(CN(C4=C5C(Cl)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1
Molecular Formula
C32H35ClFN7O2
Molecular Weight
604.12
Precautions
H302, H315, H319, H335
References & Citations
[1]Christensen JG, et al. The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients. Cancer Discov. 2019 Oct 28. pii: CD-19-1167.|[2]Kyriakos P. Papadopoulos, et al. A phase I/II multiple expansion cohort trial of MRTX849 in patients with advanced solid tumors with KRAS G12C mutation. Journal of Clinical Oncology 2019 37:15_suppl, TPS3161-TPS3161.|[3]Fell JB, Fischer JP, Baer BR, et al. Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer. J Med Chem. 2020;63 (13) :6679-6693. |[4]Awad MM, Liu S, Rybkin II, et al. Acquired Resistance to KRASG12C Inhibition in Cancer. N Engl J Med. 2021;384 (25) :2382-2393.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
K-Ras

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