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VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM to human MCL-1 in a TR-FRET assay. VU661013 destabilizes BIM/MCL1 association, leads to apoptosis in AML, and is active in venetoclax-resistant cells and xenografts. In addition, VU661013 was safely combined with venetoclax for synergy in murine models of AML.
| Molecular Weight | 712.66 |
| Formula | C39H39Cl2N5O4 |
| CAS Number | 2131184-57-9 |
| Solubility (25°C) | DMSO ≥ 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| AT-101
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