RSC-1255 | V-ATPase inhibitor | Probechem Biochemicals

Chemical Structure : RSC-1255

CAS No.: 2171015-78-2

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RSC-1255 (KRAS inhibitor 249C, RSC1255)

货号: PC-49554Not For Human Use, Lab Use Only.

RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity.

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1 mg	￥2480	In stock
5 mg	￥4980	In stock
10 mg	￥7580	In stock
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生物&药学活性

RSC-1255 (KRAS inhibitor 249C, V-ATPase inhibitor) is a Ras-mutant selective cytotoxic agent with nanomolar potency against a spectrum of Ras-mutant cancer cells (A549 (KRASG12S), IC50=73 nM), binds to V-ATPase (Kd=23 nM) and inhibits its activity.
249C (RSC-1255) shows inhibition of viability in both Ras- and Raf-mutant cells with IC50 of 73 nM, 60 nM and 22 nM for A549 (KRASG12S), LOX IMVI (BRAFV600E), and MelJuso (HRASG13D and NRASQ61L), respectively.
249C (RSC-1255) blocks lysosomal acidification and autophagy progression. blocked ATP hydrolysis of intact mammalian V-ATPase purified from pig kidneys (but not yeast).
249C (RSC-1255) differentially inhibits fibroblasts bearing mutations in KRAS and BRAF via inhibition of lysosomal pH, V-ATPase activity, and macropinocytosis.
249C (RSC-1255) preferentially kills mouse embryonic fibroblasts bearing specific KRAS mutations with IC50 values: KRAS WT (1.25 µM); G13D (0.07 µM); G12V (0.15 µM); G12S (0.23 µM); G12D (0.3 µM); Q61L (0.31 µM); G12C (0.44 µM); Q61R (0.55 µM); and for BRAFV600E (0.11 µM).
249C (RSC-1255) inhibits macropinocytosis in a KRAS-mutant-dependent manner in MEFs expressing KRAS/BRAF mutants (KRASG13D, KRASG12V, and BRAFV600E), but less so in MEFs expressing KRAS WT.
249C (RSC-1255) treatment (10 mg/kg, twice a day, i.p.) inhibits in vivo growth of mutant KRAS (KRASG12S) in mouse xenograft models and shows pharmacodynamic safety.

物理化学性质&存储条件

分子量	564.966
分子式	C27H25ClF4N4O3
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	4-(5-chlorofuran-2-yl)-1,3-bis(2,4-difluorophenyl)-5-methyl-N-((4-methylmorpholin-2-yl)methyl)-4,5-dihydro-1H-pyrazole-5-carboxamide

参考文献

1. Bhairavi Tolani, et al. Nat Biotechnol. 2022 Dec;40(12):1834-1844.

RSC-1255 (KRAS inhibitor 249C, RSC1255)

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RSC-1255 (KRAS inhibitor 249C, RSC1255)

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物理化学性质&存储条件

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