MRTX849-amide-C4-(o)-carborane
MRTX849-amide-C4-(o)-carborane is a KRASG12C inhibitor with mutation selectivity for cells expressing KRASG12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRASG12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRASG12C-positive cancers.
For research use only. We do not sell to patients.
- Formula: C38H51B10ClFN7O3
- Molecular Weight:816.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biological Activity
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Chemical Information
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Biological Activity
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KRAS(G12C) |
Cdk4/cyclin D1 |
Caspase-3 |
HY8 (up to 50 μM; 72 h) shows no cytotoxicity at concentrations up to 50 μM in NCI-H23, MIA Paca-2, and HCT116 cells after 72 h of treatment, with an IC50 >50 μM in all lines[1].
HY8 (50 μM; 8 h, following 2 h pre-incubation with 5 μM MRTX849) covalently binds to the same Cys12 site on KRASG12C as MRTX849 in NCI-H23 cells, as pre-treatment with MRTX849 blocks HY8-induced KRASG12C degradation[1].
HY8 (50 μM; 8 h, co-incubated with MG132) induces degradation of KRASG12C in NCI-H23 cells that is dependent on the proteasome pathway, as co-treatment with MG132 abrogates degradation[1].
HY8 (10-50 μM; 8 h) activates pro-apoptotic signaling in NCI-H23 cells in vitro in a dose-dependent manner after 8 h treatment with 10, 30, or 50 μM, as shown by cleavage of PARP and caspase 3, and reduced CDK4 and cyclin D1 levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H23 (KRASG12C-positive)
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Concentration:10-50 μM
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Incubation Time:24 h
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Result:Induced dose-dependent degradation of KRASG12C and concurrent reduction in phosphorylated ERK (p-ERK) levels, with maximal effects observed at 50 μM.
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Cell Line:NCI-H23 (KRASG12C-positive)
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Concentration:10 μM, 30 μM, 50 μM
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Incubation Time:8 h
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Result:Induced dose-dependent cleavage of PARP and caspase 3, and reduced levels of CDK4, indicating activation of apoptotic signaling.
Chemical Information
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Molecular Weight 816.42
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Formula C38H51B10ClFN7O3
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SMILES
ClC1=CC=CC2=C1C(N(C3)CCC(C3=NC(OC[C@@H]4N(C(CCCCC5678[BH]9%10%11[BH]%12%13([BH]%10%14%15[BH]8%11%16[BH]%17%15%18%19)[BH]%20%14%18[BH]%21%22%17[CH]5%16%19[BH]%216%23[BH]9%127[BH]%20%13%22%23)=O)CCC4)=N%24)=C%24N%25C[C@H](CC#N)N(C(C(F)=C)=O)CC%25)=CC=C2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MRTX849-amide-C4-(o)-carborane Related Classifications
HY-182044 Related Classifications
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