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VU661013

Chemical Structure : VU661013

CAS No.: 2131184-57-9

VU661013 (VU 661013;VU-661013)

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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 712.672
Formula C39H39Cl2N5O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

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

References

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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