DC Chemicals Limited
China
Product Name: VER-49009
Price: $550.0/100mg $1000.0/250mg $1900.0/1g
Purity: 98.0%
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: VER-49009
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

558640-51-0

558640-51-0 structure

558640-51-0 structure

Name: VER 49009
Chemical Name: 5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)pyrazole-3-carboxamide
CAS Number: 558640-51-0
Molecular Formula: C₁₉H₁₈ClN₃O₄
Molecular Weight: 387.817
Catalog: Research Areas Cancer
Create Date: 2018-01-02 05:50:37
Modify Date: 2024-01-10 15:22:28
VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.

Name	5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)pyrazole-3-carboxamide
Synonyms	5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)pyrazole-3-carboxamide 3-(5-Chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)-1H-pyrazole-5-carboxamide 1H-Pyrazole-5-carboxamide, 3-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)- VER-49009

Description	VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM and a Kd of 78 nM.
Related Catalog	Research Areas >> Cancer
Target	HSP90:25 nM (IC50)
In Vitro	VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM. VER-49009 binds to the ATPase of full length yeast Hsp90 protein, with an IC50 of 140 nM[1]. VER-49009 inhibits Hsp90, with a Kd of 78 nM. VER-49009 also shows antiproliferative activities against various human cancer cells, with a mean GI50 of 685 ± 119 nM. VER-49009 suppressses the proliferation of human umbilical vein endothelial cells (HUVEC) with GI50 values of 444 ± 91.1 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) and prostate (PNT2) epithelial cells. VER-49009 displays no differences in cellular activities of isogenic cell lines, and these activities are independent of NQO1 expression[2]. VER-49009 inhibits the proliferation (1, 2.5 μM), induces G2 phase arrest and reduces total Akt and phospho-Akt expression levels in CFSC cells (1-5 μM)[3].
In Vivo	VER-49009 (4 mg/kg, i.p.) results in clear depletion of ERBB2 at 3 and 8 h following the final dose, with client protein levels returning to normal by 24 h, in the athymic mice bearing well-established OVCAR3 human ovarian ascites tumors[2].
Cell Assay	Briefly, 5 × 103 cells/well are plated in 96-well culture plates. After an overnight incubation, the cells are treated with various concentrations of VER-49009 and VER-49009M (0, 1, 2.5, and 5 μM) for 24 h[3].
Animal Admin	In some studies, female NCr athymic mice are implanted i.p. with 10 million OVCAR3 ovarian carcinoma cells harvested from donor mice. This tumor mimics late-stage malignant disease. Once tumors are well established, mice are injected i.p. with 4 mg/kg VER-49009 or VER-50589 twice daily over 2 days (four doses total). Tumors are harvested at intervals after the last dose and snap frozen for pharmacodynamic analyses[1].
References	[1]. Dymock BW, et al. Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 discovered through structure-based design. J Med Chem. 2005 Jun 30;48(13):4212-5. [2]. Sharp SY, et al. Inhibition of the heat shock protein 90 molecular chaperone in vitro and in vivo by novel, synthetic, potent resorcinylic pyrazole/isoxazole amide analogues. Mol Cancer Ther. 2007 Apr;6(4):1198-211. [3]. Sun X, et al. Inhibition of hepatic stellate cell proliferation by heat shock protein 90 inhibitors in vitro. Mol Cell Biochem. 2009 Oct;330(1-2):181-5.

Density	1.4±0.1 g/cm3
Boiling Point	620.2±55.0 °C at 760 mmHg
Molecular Formula	C₁₉H₁₈ClN₃O₄
Molecular Weight	387.817
Flash Point	328.9±31.5 °C
Exact Mass	387.098572
LogP	0.96
Vapour Pressure	0.0±1.9 mmHg at 25°C
Index of Refraction	1.642
Storage condition	2-8℃