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Hh Signaling Antagonist X, Itraconazole-CAS 84625-61-6-Calbiochem

品牌
Sigma-Aldrich
CAS
84625-61-6
货号
419825
规格纯度
The Hh Signaling Antagonist X, Itraconazole, also referenced under CAS 84625-61-6, controls the biological activity of Hh pathway. This small molecule/inhibitor is primarily used for Cell Signaling applications.
参考价格
2012.39 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

A cell-permeable, orally available triazole-class antifungal agent that, in addition to its known inhibitory activity against fungal cytochrome P450 14-α-demethylase, also acts as an effective Hh signaling inhibitor (IC50 ~0.8 µM against SHHN-induced Gli transcription activity in Shh-Light2 cells) in a Ptch-independent manner (IC50 ~0.9 µM against Ptch promoter-mediated transcription activity in murine Ptch-/- fibroblasts), presumably by binding smoothened (smo) at a site distinct from that targeted by cyclopamine (Cat. No. 239803) and SAG (Cat. No. 566660), as Itraconazole does not compete with BODIPY-cyclopamine binding, and it alters only the magnitude, but not the EC50, of SAG-induced Gli transcription activity in Shh-Light2 cells. Shown to effectively suppress Hh pathway-dependent growth of both engrafted medulloblastoma and endogenous basal cell carcinoma in mice in vivo (37.5 to 100 mg/kg/12 hr, p.o.) in a reversible manner.
A cell-permeable, orally available triazole-class antifungal agent that, in addition to its known inhibitory activity against fungal cytochrome P450 14-α-demethylase, also acts as an effective Hh signaling inhibitor (IC50 ~ 0.8 µM against SHHN-induced Gli transcription activity in Shh-Light2 cells) in a Ptch-independent manner (IC50 ~ 0.9 µM against Ptch promoter-mediated transcription activity in murine Ptch-/- fibroblasts), presumably by binding smoothened (smo) at a site distinct from that targeted by cyclopamine (Cat. No. 239803) and SAG (Cat. No. 566660), as Itraconazole does not compete with BODIPY-cyclopamine binding, and it alters only the magnitude, but not the EC50, of SAG-induced Gli transcription activity in Shh-Light2 cells. Shown to effectively suppress Hh pathway-dependent growth of both engrafted medulloblastoma and endogenous basal cell carcinoma in mice in vivo (37.5 to 100 mg/kg/12 hr, p.o.) in a reversible manner.

包装

250 mg in Glass bottle
Packaged under inert gas

警告

Toxicity: Harmful (C)

重悬

Following reconstituiton, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Kim, J., et al. 2010. Cancer Cell17, 388.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C35H38Cl2N8O4
分子量705.63
MDL编号MFCD00870168

产品性质

质量水平100
测定≥98% (HPLC)
形式powder
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色 white
溶解性DMSO: 10 mg/mL
运输ambient
储存温度2-8℃
InChI1S/C35H38Cl2N8O4/c1-3-25(2)45-34(46)44(24-40-45)29-7-5-27(6-8-29)41-14-16-42(17-15-41)28-9-11-30(12-10-28)47-19-31-20-48-35(49-31,21-43-23-38-22-39-43)32-13-4-26(36)18-33(32)37/h4-13,18,22-25,31H,3,14-17,19-21H2,1-2H3/t25?,31-,35-/m0/s1
InChI keyVHVPQPYKVGDNFY-ZPGVKDDISA-N

安全信息

象形图GHS07
警示用语:Warning
危险声明H302 - H315 - H319 - H335
预防措施声明P261 - P264 - P270 - P301 + P312 - P302 + P352 - P305 + P351 + P338
危险分类Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官Respiratory system
储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

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