Catalog No.: PC-27900Not For Human Use, Lab Use Only.
Kobe3708 is a small-molecule RAS/RAF inhibitor that specifically binds to the CRAF RBD but not to RAS, allosterically disrupts RAS/RAF binding, inhibits the binding between HRASG12V·GTP and CRAF RBD in ELISA with IC50 of 7.62 uM.
Kobe3708 is a small-molecule RAS/RAF inhibitor that specifically binds to CRAF RAS binding domain (RBD) but not to RAS, allosterically disrupts RAS/RAF binding, inhibits the binding between HRASG12V·GTP and CRAF RBD in ELISA with IC50 of 7.62 uM.
Kobe3708 inhibits the growth of NIH/RASG12V but not NIH/RAF CR3 cells.
Kobe3708 covalently binds to CRAF Cys95 and may interfere with RAS/RAF binding via not direct PPI inhibition but allosteric effects over the RAS/RAF binding interface.
Kobe3708 inhibits cell proliferation and activation of downstream RAS/RAF signalling in cancer cells with active RAS mutations with IC50 of 3.04 and 4.22 uM for NIH/RASG12V and human colorectal cancer SW480 (carrying the active KRASG12V mutation) cells.
Kobe3708 induces dose-dependent reductions in the levels of phosphorylated MEK, ERK, and p90RSK (RSK) in NIH/RASG12V and SW480 cells with active RAS mutations.
Kobe3708 inhibits mutant RAS-driven tumour growth by preventing RAS/RAF-mediated ERK activation.
Kobe3708 prevent BRAF inhibitor-induced paradoxical RAS signalling activation and exhibits antitumour activity against BRAF inhibitor-resistant melanoma.
