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Chemical Structure : VU661013
CAS No.: 2131184-57-9
Catalog No.: PC-35655Not For Human Use, Lab Use Only.
VU661013 (VU-661013) is a novel potent, selective MCL-1 inhibitor with Ki of 97 pM (human MCL-1) in TR-FRET assay, shows no significant inhibition on BCL-xL (Ki>40 uM) or BCL-2 (Ki=0.73 uM).
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|---|---|---|---|
| 5 mg | $458 | In stock | |
| 10 mg | $758 | In stock | |
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| 50 mg | Get quote | ||
| 100 mg | Get quote |
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VU661013 (VU-661013) is a novel potent, selective MCL-1 inhibitor with Ki of 97 pM (human MCL-1) in TR-FRET assay, shows no significant inhibition on BCL-xL (Ki>40 uM) or BCL-2 (Ki=0.73 uM).
VU661013 de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML.
VU661013 is active in venetoclax-resistant cells and patient derived xenografts.
| M.Wt | 712.672 | |
| Formula | C39H39Cl2N5O4 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(R)-3-(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 |
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1. Ramsey HE, et al. Cancer Discov. 2018 Sep 5. pii: CD-18-0140.
2. Zhao B, et al. Biochemistry. 2018 Aug 14;57(32):4952-4958.
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