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ChemicalBook--->CAS DataBase List--->2131184-57-9

2131184-57-9

2131184-57-9 Structure

2131184-57-9 Structure
IdentificationBack Directory
[Name]

VU0661013
[CAS]

2131184-57-9
[Synonyms]

VU661013
VU0661013
1H-Indole-5-carboxylic acid, 3-[(4R)-7-chloro-10-[3-(4-chloro-3,5-dimethylphenoxy)propyl]-3,4-dihydro-4-methyl-1-oxo-6-(1,3,5-trimethyl-1H-pyrazol-4-yl)pyrazino[1,2-a]indol-2(1H)-yl]-1-methyl-
[Molecular Formula]

C39H39Cl2N5O4
[MOL File]

2131184-57-9.mol
[Molecular Weight]

712.66
Chemical PropertiesBack Directory
[Boiling point ]

906.4±65.0 °C(Predicted)
[density ]

1.37±0.1 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

≥125mg/mL in DMSO;insoluble in H2O
[form ]

Solid
[pka]

4.44±0.30(Predicted)
[color ]

Light yellow to yellow
Spectrum DetailBack Directory
[Spectrum Detail]

VU0661013(2131184-57-9)1HNMR
Hazard InformationBack Directory
[Biological Activity]

vu661013 is a novel, potent, selective mcl-1 inhibitor (ki of 97 ± 30 pm).[1]mcl-1, an anti-apoptotic bcl-2 family member, is commonly upregulated in acute myeloblastic leukemia (aml) cells. targeting anti-apoptotic proteins in aml is a key therapeutic strategy, and mcl-1 is a critical anti-apoptotic oncoprotein. [1]vu661013 reduced expansion of multiple aml cell lines in vitro. venetoclax (a bcl-2 inhibitor) and vu661013 exhibited favorable synergy in several of aml cells lines, venetoclax-resistant aml cells were sensitive to vu661013. [1]vu661013 decreased tumor growth in an in vivo murine model. vu661013 (25mg/kg) and venetoclax (15mg/kg) can be synergistic in patient-derived xenograft transplantation models. [1][1]a novel mcl-1 inhibitor combined with venetoclax rescues venetoclax resistant acute myelogenous leukemia. cancer discov. 2018 sep 5. pmid: 30185627. doi: 10.1158/2159-8290.cd-18-0140
[storage]

Store at -20°C
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