VER-49009-CCT-129397-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEVER-49009Cat. No.: HY-15986CAS No.: 558640-51-0Synonyms: CCT 129397分式: CHClNO分量: 387.82作靶点: HSP作通路: Cell Cycle/DNA Damage; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验

2、DMSO : 100 mg/mL (257.85 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.75 mg/mL (7.09 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.75 mg/mL (7.09 mM); Clear solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 VER-49009种 Hs

3、p90 抑制剂，IC50 值为 25 nM，Kd 值为 78 nM。IC50 & Target HSP9025 nM (IC50)体外研究 VER-49009 is a Hsp90 inhibitor, with an IC50 of 25 nM. VER-49009 binds to the ATPase of full length yeastHsp90 protein, with an IC50 of 140 nM 1. VER-49009 inhibits Hsp90, with a Kd of 78 nM. VER-49009 alsoshows antiproliferative

4、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 GI50values of 444 91.1 nM, and shows higher GI50s against nontumorigenic human breast (MCF10a) andprostate (PNT2) epithelial ce

5、lls. 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 M), induces G2 phase arrest and reduces total Akt and phospho-Akt expression levels in CFSC cells (1-5 M) 3.体内研

6、究 VER-49009 (4 mg/kg, i.p.) results in clear depletion of ERBB2 at 3 and 8 h following the final dose, with clientprotein levels returning to normal by 24 h, in the athymic mice bearing well-established OVCAR3 humanovarian ascites tumors 2.PROTOCOLCell Assay 3 Briefly, 5 103 cells/well are plated in

7、 96-well culture plates. After an overnight incubation, the cells aretreated with various concentrations of VER-49009 and VER-49009M (0, 1, 2.5, and 5 M) for 24 h 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal In some studies, female NCr athym

8、ic mice are implanted i.p. with 10 million OVCAR3 ovarian carcinomaAdministration 2 cells harvested from donor mice. This tumor mimics late-stage malignant disease. Once tumors are wellestablished, mice are injected i.p. with 4 mg/kg VER-49009 or VER-50589 twice daily over 2 days (fourdoses total).

9、Tumors are harvested at intervals after the last dose and snap frozen for pharmacodynamicanalyses 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Dymock BW, et al. Novel, potent small-molecule inhibitors of the molecular chaperone Hsp90 d

10、iscovered through structure-baseddesign. 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 resorcinylicpyrazole/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.McePdfHeight2/2 Master of Small Molecules 您边的抑制剂师www.MedChemECaution: Product has not been