[CAS NO. 940289-57-6]  VER-49009

Ships within Stock Price Qty Total
$0.00
$0.00
Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis
request a quote
If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [940289-57-6]

Catalog
SLK-S7458
Brand
Selleck
CAS
940289-57-6

DESCRIPTION [940289-57-6]

Overview

MDL-
Molecular Weight387.82
Molecular FormulaC19H18ClN3O4
SMILESCCNC(=O)C1=C(C(=NN1)C2=CC(=C(C=C2O)O)Cl)C3=CC=C(C=C3)OC

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 mM2.5785 mL12.8926 mL25.7852 mL
5 mM0.5157 mL2.5785 mL5.1570 mL
10 mM0.2579 mL1.2893 mL2.5785 mL
50 mM0.0516 mL0.2579 mL0.5157 mL

Description

VER-49009 (CCT0129397) is a potent inhibitor with of 47 nM for HSP90β.

Targets

HSP90β [1]
47 nM

In vitro

VER-49009 inhibits the intrinsic ATPase activity of recombinant yeast Hsp90 with IC50 of 167 nM, and produces antiproliferative activity in a panel of human cancer cell lines and nontumorigenic cells in vitro. VER-49009 causes induction of HSP72 and HSP27 with depletion of client proteins, including C-RAF, B-RAF, and survivin, and PRMT5, which further result in cell cycle arrest and apoptosis. VER-49009 inhibits the cell proliferation, and induces G2 phase arrest in hepatic stellate cell line CFSC cells, which may suggest a rational approach in the prevention of liver fibrosis.

In vivo

In athymic mice, VER-49009 (20 mg/kg, i.v.) shows rapid clearance with values of 0.187 L/h. In an orthotopic human ovarian carcinoma model, VER-49009 (4 mg/kg, i.p.) also induces the depletion of the sensitive HSP90 client protein ERBB2.