VU661013 ( VU 661013;VU-661013 )

Catalog No. M13394 CAS No. 2131184-57-9

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Product Name

VU661013
Note

Research use only, not for human use.
Brief Description

VU661013 (VU-661013) is a novel potent, selective MCL-1 inhibitor with Ki of 97 pM (human MCL-1) in TR-FRET assay.
Description

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); de-stabilizes BIM/MCL-1 association, leads to apoptosis in AML, and is active in venetoclax-resistant cells and patient derived xenografts.
Synonyms

VU 661013;VU-661013
Pathway

Angiogenesis
Target

Bcl-2
Recptor

Bcl-2
Research Area

——
Indication

——

CAS Number

2131184-57-9
Formula Weight

712.67
Molecular Formula

C39H39Cl2N5O4
Purity

>98% (HPLC)
Solubility

DMSO : ≥ 125 mg/mL 175.40 m; MH2O : < 0.1 mg/mL
SMILES

ClC1=C(C2=C(C)N(C)N=C2C)C3=C(C(CCCOC4=CC(C)=C(Cl)C(C)=C4)=C5N3[C@H](C)CN(C6=CN(C)C7=C6C=C(C(O)=O)C=C7)C5=O)C=C1
Chemical Name

(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

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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