Information VU661013 VU661013 is a novel, potent, selective MCL1 inhibitor with Ki of 97 ± 30 pM of human MCL-1 in a TR-FRET assay. However, VU661013 does not significantly inhibit BCL-xL or BCL-2 with Ki > 40 μM or = 0.73 μM. VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML. Targets MCL1 (Cell-free assay) 97 pM(Ki) In vitro VU661013 is a novel, potent, selective MCL-1 inhibitor that de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML, and is active in venetoclax-resistant cells. In vivo VU661013 is active in patient derived xenografts. In addition, VU661013 is safely combined with venetoclax for synergy in murine models of AML. Cell Research(from reference) Cell lines：MV4-11 cells Concentrations：100 nM - 5 μM Incubation Time：48 h
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
VU661013
CAS number：2131184-57-9 molecular formula：C39H39Cl2N5O4
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | VU0661013 | 3-[(4R)-7-chloro-10-[3-(4-chloro-3,5-dimethylphenoxy)propyl]-4-methyl-1-oxo-6-(1,3,5-trimethyl-1H-pyrazol-4-yl)-3,4-dihydropyrazino[1,2-a]indol-2(1H)-yl]-1-methyl-1H-indole-5-carboxylic acid | ||
| CAS number | 2131184-57-9 | molecular formula | C39H39Cl2N5O4 |
| molecular weight | 712.66 g/mol | Exact mass | ≥98% |
| PSA | 94.500 Ų | logp | 8.100 |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
