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| | VU0661013 Basic information |
| Product Name: | VU0661013 | | Synonyms: | VU0661013;VU661013;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- | | CAS: | 2131184-57-9 | | MF: | C39H39Cl2N5O4 | | MW: | 712.66 | | EINECS: | | | Product Categories: | | | Mol File: | 2131184-57-9.mol |  |
| | VU0661013 Chemical Properties |
| 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 |
| | VU0661013 Usage And Synthesis |
| 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 |
| | VU0661013 Preparation Products And Raw materials |
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