CB-6644 is a novel allosteric selective inhibitor of the ruvbl1/2 complex with anti-cancer activity. CB-6644 blocks the ATPase activity of RUVBL1/2 with an IC50 of 15 nM. CB-6644 interacts specifically with RUVBL1/2 in cancer cells, leading to cell death. Importantly, drug-acquired-resistant cell clones have amino acid mutations in either RUVBL1 or RUVBL2, suggesting that cell killing is an on-target consequence of RUVBL1/2 engagement. In xenograft models of acute myeloid leukemia and multiple myeloma, CB-6644 significantly reduced tumor growth without obvious toxicity.
MedKoo Cat#: 565585
Name: CB-6644
CAS#: 2316817-88-4
Chemical Formula: C29H34ClFN4O5
Exact Mass: 572.2202
Molecular Weight: 573.06
Elemental Analysis: C, 60.78; H, 5.98; Cl, 6.19; F, 3.32; N, 9.78; O, 13.96
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
DMSO | 100.0 | 174.50 |
The following data is based on the product molecular weight 573.06 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 |