RMC-5127 is a RAS (ON) KRASG12V tri-complex inhibitor. RMC-5127 non-covalently binds to an abundant intracellular chaperone protein cyclophilin A (CypA), resulting in a binary complex that engages RASG12V(ON) to form a high-affinity tri-complex that sterically inhibits RAS binding to effectors. RMC-5127 drove deep suppression of RAS pathway activity, inhibited cell proliferation, and induced apoptosis in a panel of KRASG12V mutant human cancer cells in vitro but only caused submaximal inhibition in the panel of K/N/HRAS wildtype cancer cells, indicative of selectivity for KRASG12V over K/N/HRAS wild type.
MedKoo Cat#: 128835
Name: RMC-5127
CAS#: N/A
Chemical Formula: C57H75N9O9S
Exact Mass: 1061.5408
Molecular Weight: 1062.34
Elemental Analysis: C, 64.45; H, 7.12; N, 11.87; O, 13.55; S, 3.02
The following data is based on the product molecular weight 1,062.34 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
