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Chemical Structure : RSC-1255
CAS No.: 2171015-78-2
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 1 mg | $248 | In stock | |
| 5 mg | $498 | In stock | |
| 10 mg | $758 | In stock | |
| 25 mg | Get quote | ||
| 100 mg | Get quote |
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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.
| M.Wt | 564.966 | |
| Formula | C27H25ClF4N4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Bhairavi Tolani, et al. Nat Biotechnol. 2022 Dec;40(12):1834-1844.
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