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

产品编号:4145144
规格: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.
CAS NO:84625-61-6
包装规格:250 MG
产品类别:进口试剂
品牌:Sigma-Aldrich
优惠价:立即咨询
产品编号包装单位单价(元)国内现货国外库存询价单
4145144250 MG2210
产品别名

84625-61-6

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

14LDM Inhibitor, Oriconazole, R51211, Smo Antagonist VII, Sporanox, 14-α-demethylase Inhibitor

基本信息
Empirical Formula【经验(实验)分子式】
C35H38Cl2N8O4
Molecular weight
705.63
MDL number
MFCD00870168
General description【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.
Warning【警告】
Toxicity: Harmful (C)
Reconstitution【重悬】
Following reconstituiton, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes【其他说明】
Kim, J., et al. 2010. Cancer Cell17, 388.
Legal Information【法律信息】
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
产品性质
Quality Level【质量水平】
100
Assay【测定】
≥98% (HPLC)
form【形式】
powder
manufacturer/tradename
Calbiochem®
storage condition【储存条件】
OK to freeze
protect from light
color【颜色】
white
solubility【溶解性】
DMSO: 10 mg/mL
shipped in【运输】
ambient
storage temp.【储存温度】
2-8℃
InChI
1S/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 key
VHVPQPYKVGDNFY-ZPGVKDDISA-N
packaging【包装】
250 mg in Glass bottle
Packaged under inert gas
安全信息
Pictograms【象形图】
GHS07
Signal word【警示用语:】
Warning
Hazard Statements
H302 - H315 - H319 - H335
Precautionary Statements
P261 - P264 - P270 - P301 + P312 - P302 + P352 - P305 + P351 + P338
Hazard Classifications【危险分类】
Acute Tox. 4 Oral - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
Target Organs【靶器官】
Respiratory system
Storage Class Code【储存分类代码】
11 - Combustible Solids
WGK
WGK 3
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