[CAS NO. 747413-08-7]  VER-50589

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PRODUCTS SPECIFICATIONS [747413-08-7]

Catalog
SLK-S7459
Brand
Selleck
CAS
747413-08-7

DESCRIPTION [747413-08-7]

Overview

MDLMFCD18382095
Molecular Weight388.80
Molecular FormulaC19H17ClN2O5
SMILESO=C(C1=NOC(C2=CC(Cl)=C(O)C=C2O)=C1C3=CC=C(OC)C=C3)NCC

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.5720 mL12.8601 mL25.7202 mL
5 mM0.5144 mL2.5720 mL5.1440 mL
10 mM0.2572 mL1.2860 mL2.5720 mL
50 mM0.0514 mL0.2572 mL0.5144 mL

Description

VER-50589 is a potent inhibitor with of 21 nM for HSP90β.

Targets

HSP90β [1]
21 nM

In vitro

VER-50589 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 143 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-50589 causes induction of HSP72 and HSP27 alongside depletion of client proteins, including C-RAF, B-RAF, and survivin, and the protein arginine methyltransferase PRMT5, which further result in cell cycle arrest and apoptosis.

In vivo

In HCT116 human colon cancer xenografts, VER-50589 (100 mg/kg i.p.) results in a statistically significant reduction of ∼30% in tumor volume and weight, as well as induction of HSP72 and depletion of ERBB2 and C-RAF.