VER-49009 940289-57-6

.cp_wz table {border-top: 1px solid #ccc;border-left:1px solid #ccc; } .cp_wz table td{border-right: 1px solid #ccc; border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;} .cp_wz table th {border-right: 1px solid #ccc;border-bottom: 1px solid #ccc; padding: 5px 0px 0px 5px;}


Molecular Weight:

387.82 VER-49009 is a potent HSP90 inhibitor with IC50 of 47 nM for HSP90β.


Biological Activity


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 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.


Protocol(Only for Reference)


Kinase Assay:


[1]

Fluorescence Polarization Assay	Binding of HSP90 Inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.

Cell Assay:


[1]

Cell lines	Melanoma cells (SKMEL 2, SKMEL 5, SKMEL 28, WM266.4); Colon cancer cells (HCT116, BEneg, BE2, HT29, HT29oxaliR); Ovarian cancer cells (CH1, CH1doxR); Breast cancer cells (MB-231, MB-468, BT20, ZR751, MCF7, BT-474); nontumorigenic cells (HUVEC, MCF10a, PNT
Concentrations	~10 μM
Incubation Time	4 days
Method	Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method.

Animal Study:


[1]

Animal Models	Mice bearing established OVCAR3 human ovarian xenografts.
Formulation	10% DMSO, 5% Tween 20, 85% saline
Dosages	~4 mg/kg
Administration	i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

Species	Baboon	Dog	Monkey	Rabbit	Guinea pig	Rat	Hamster	Mouse
Weight (kg)	12	10	3	1.8	0.4	0.15	0.08	0.02
Body Surface Area (m2)	0.6	0.5	0.24	0.15	0.05	0.025	0.02	0.007
Km factor	20	20	12	12	8	6	5	3

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×	mouse Km(3)	= 11.2 mg/kg
	rat Km(6)

Chemical Information

Molecular Weight (MW)	387.82
Formula	C19H18ClN3O4
CAS No.	940289-57-6

Storage	3 years -20℃Powder
	6 months-80℃in solvent (DMSO, water, etc.)
Synonyms	CCT0129397

Solubility (25°C) *	In vitro	DMSO	77 mg/mL (198.54 mM)
		Water	<1 mg/mL (
		Ethanol	<1 mg/mL (
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Name	3-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide

Molarity Calculator
Dilution Calculator
Molecular Weight Calculator

Contact us if you need more details on 940289-57-6. We are ready to answer your questions on packaging, logistics, certification or any other aspects about VER-49009 940289-57-6、940289-57-6 VER-49009. If these products fail to match your need, please contact us and we would like to provide relevant information.

Product Categories : Cytoskeletal Signaling > HSP Inhibitor