MCB-294

MCB-294 is a dual-state pan-KRAS inhibitor that selectively inhibits KRAS over NRAS and HRAS. MCB-294 capable of binding both the active (GTP-bound) and inactive (GDP-bound) forms of KRAS with Kds of approximately 1 pM and 10 nM, respectively. MCB-294 broadly impairs the growth of hTERT-HPNE cells expressing G12D, G12C, G12V, G12S, G13D, and wild-type KRAS, with IC50s of approximately 700 nM. MCB-294 induces irreversible apoptosis in KRAS-mutated tumors. MCB-294 effectively suppress KRASG12C inhibitor-resistant cancer cells and remodel the tumor immune microenvironment. MCB-294 can be used for the study of pancreatic cancer, colorectal cancer and lung cancer[1].

C34H29D2F4N5O3

635.65

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

Apoptosis; Caspase; p38 MAPK; Ras; TNF Receptor

Caspase 3; K-Ras

Room temperature