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Product introduction

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

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Chinese name

VU661013

English name

VU661013

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 Å²

Logp

8.100

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