Home Apoptosis Ras inhibitor MCB-294

research use only

MCB-294 Ras inhibitor

MCB-294 is a pan-KRAS inhibitor that targets both active (GTP-bound) and inactive (GDP-bound) KRAS states, exhibiting Kd values of about 1 pM and 10 nM, respectively. It shows preferential inhibition of KRAS over NRAS and HRAS. The compound inhibits proliferation of hTERT-HPNE cells harboring G12D, G12C, G12V, G12S, G13D, and wild-type KRAS variants, with IC50 values around 700 nM. MCB-294 triggers apoptosis in KRAS-mutated tumors and demonstrates activity against KRASG12C inhibitor-resistant cancer cells while modulating the tumor immune microenvironment. This compound serves as a research tool for pancreatic, colorectal, and lung cancer investigations.

Chemical Structure

Molecular Weight: 635.65

Purity & Quality Control

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Signaling Pathway

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Ras Signaling Pathway

Mechanism of Action

In Vivo
In vivo MCB-36 (10 mg/kg, i.p., single dose) achieves rapid systemic exposure, reaching peak plasma concentration at 0.5 h post-dosing with a plasma elimination half-life (t1/2) of 1.1 h. MCB-294 (30 mg/kg, i.p., twice daily for 1-16 days) effectively suppresses KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment in mice.

References
  • https://pubmed.ncbi.nlm.nih.gov/40780213/

Chemical Information

Molecular Weight 635.65 Formula C34H29D2F4N5O3
CAS No. SDF --
Smiles O[C@](C1)(C)CCCN1C2=NC(OC([2H])([2H])C3(CCC4)N4C/C(C3)=C(F)/F)=NC5=C(F)C(C6=C(C(C#C)=C(F)C=C7)C7=CC(O)=C6)=NC=C52

Storage and Stability

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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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