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VER-50589
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
VER-50589图片
CAS NO:747413-08-7
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)388.80
FormulaC19H17ClN2O5
CAS No.747413-08-7
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 77 mg/mL (198.0 mM)
Water: <1 mg/mL
Ethanol: 77 mg/mL (198.0 mM)
Other info

Chemical Name: 5-(5-chloro-2,4-dihydroxyphenyl)-N-ethyl-4-(4-methoxyphenyl)isoxazole-3-carboxamide

InChi Key: JXPCDMPJCKNLBY-UHFFFAOYSA-N

InChi Code: InChI=1S/C19H17ClN2O5/c1-3-21-19(25)17-16(10-4-6-11(26-2)7-5-10)18(27-22-17)12-8-13(20)15(24)9-14(12)23/h4-9,23-24H,3H2,1-2H3,(H,21,25)

SMILES Code: O=C(C1=NOC(C2=CC(Cl)=C(O)C=C2O)=C1C3=CC=C(OC)C=C3)NCC

Synonyms

VER 50589; VER-50589; VER50589;

实验参考方法
In Vitro

In vitro activity: 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.


Kinase 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: Antiproliferative effects are measured using the sulforhodamine B assay. HUVEC sensitivity is determined by an alkaline phosphatase method. Cells: 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)

In VivoIn 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.
Animal modelHCT116 human colon cancer xenografts
Formulation & DosageDissolved in 10% DMSO, 5% Tween 20, 85% saline; 100 mg/kg; i.p. injection
References

Mol Cancer Ther. 2007 Apr;6(4):1198-211.