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VU661013

Catalog No.
A8783
Novel, potent, selective MCL-1 inhibitor
Grouped product items
SizePriceStock Qty
5mg
$866.00
Ship with 10-15 days
10mg
$1,339.00
Ship with 10-15 days
25mg
$2,756.00
Ship with 10-15 days
50mg
$4,331.00
Ship with 10-15 days

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

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]

 

Reference:

[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

Chemical Properties

StorageStore at -20°C
M.Wt712.66
Cas No.2131184-57-9
FormulaC39H39Cl2N5O4
Solubility≥125mg/mL in DMSO;insoluble in H2O
Chemical Name3-((4R)-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
SDFDownload SDF
Canonical SMILESClC1=C(C2=C(C)N(C)N=C2C)C3=C(C(CCCOC4=CC(C)=C(Cl)C(C)=C4)=C5N3[[email protected]](C)CN(C6=CN(C)C7=C6C=C(C(O)=O)C=C7)C5=O)C=C1
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Protocol

Cell experiment [1]:

Cell lines

AML cell lines MV-411, Kasumi-1, K-562, HL-60, U-937 Kasumi-3, KG-1, NB4, SKM-1, PL-21, MOLM-16 and THP-1, and leukemia mantle cell lymphoma cell line Z-138.

Preparation method

This compound can be soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.

Reaction Conditions

48 h, 100 nM to 5 μM

Applications

Multiple AML cell lines displayed a high sensitivity to VU661013.

Animal experiment [1]:

Animal models

Xenograft transplantation model of MV-4-11 cell line in NSGS mice; AML patient PDX models

Dosage form

10, 25 or 75 mg/kg , daily i.p injection for 21 days

Applications

VU661013 treatment of disseminated human AML resulted in a dose-dependent decrease in tumor burden.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[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

Quality Control

Quality Control & MSDS

View current batch:

Chemical structure

VU661013