Kobe3708 | RAS/RAF inhibitor | Probechem Biochemicals

Chemical Structure : Kobe3708

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Kobe3708 (Kobe-3708)

货号: 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.

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生物&药学活性

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.

物理化学性质&存储条件

分子量	366.37
分子式	C20H18N2O5
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	(Z)-2-(4-((1-acetyl-3-oxoindolin-2-ylidene)methyl)-2-methoxyphenoxy)acetamide

参考文献

1. Yoshikawa Y, et al. Nat Commun. 2026 Aug 27;17(1):8809.

Kobe3708 (Kobe-3708)

生物&药学活性

物理化学性质&存储条件

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Kobe3708 (Kobe-3708)

生物&药学活性

物理化学性质&存储条件

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