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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 |
产品价格查看更多规格...
产品编号 | 包装单位 | 单价(元) | 国内现货 | 国外库存 | 询价单 |
4145144 | 250 MG | 2210 |
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 |