环巴胺|T2825|TargetMol

Cyclopamine
4449-51-8

￥484 5mg 起订

￥753 10mg 起订

￥1380 25mg 起订

上海更新日期：2024-09-23

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产品详情:

中文名称：: 环巴胺

英文名称：: Cyclopamine

CAS号：: 4449-51-8

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.66%

产品类别：: 抑制剂

货号：: T2825

Product Introduction

Bioactivity

名称	Cyclopamine
描述	Cyclopamine (11-Deoxojervine), a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids.
细胞实验	Cells were cultured in triplicate in 96-well plates in assay media to which 5E1 monoclonal antibody, ShhNp and/or cyclopamine were added at 0 h at concentrations indicated in the main text. Viable cell mass was determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth was calculated as OD (day 4) 2 OD (day 2)/OD (day 2) [3].
激酶实验	This assay measures the end stage of the Hh signaling pathway, that is, the transcriptional modulation of Gli, using Luciferase as readout (Gli-Luc assay). Cyclopamine is prepared for assay by serial dilution in DMSO and then added to empty assay plates. TM3Hh12 cells (TM3 cells containing Hh-responsive reporter gene construct pTA-8xGli-Luc) are resuspended in F12 Ham's/DMEM (1:1) containing 5% FBS and 15 mM Hepes pH 7.3, added to assay plates and incubated with Cyclopamine for approximately 30 minutes at 37 °C in 5% CO2. 1 nM Hh-Ag 1.5 is then added to assay plates and incubated at 37 °C in the presence of 5% CO2. After 48 hours, either Bright-Glo or MTS reagent is added to the assay plates and luminescence or absorbance at 492 nm is determined. IC50 value, defined as the inflection point of the logistic curve, is determined by non-linear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of Cyclopamine using the R statistical software pack [1].
动物实验	A total of 0.1 ml Hanks' balanced salt solution and matrigel (1:1) containing 2 × 10^6 cells were injected subcutaneously into CD-1 nude mice. Tumours were grown for 4 days to a minimum volume of 125 mm3; treatment was initiated simultaneously for all subjects. Mice were injected subcutaneously with vector alone (triolein:ethanol 4:1 v/v) or a cyclopamine suspension (1.2 mg per mouse in triolein: ethanol 4:1 v/v) daily for 7 days. At the end of the treatment period, tumours were excised from mice, weighed and then fixed for 3 h at 4 °C with 4% paraformaldehyde, embedded in paraffin wax and sectioned (6 μm). Apoptotic cells were identified by TUNEL using recombinant Tdt as previously described29. Sections were then counterstained with eosin. Eight ×20-magnified fields from regions corresponding to the exterior, middle and interior of two control and two cyclopamine-treated tumours were chosen at random [5].
体外活性	将鸡胚胎暴露于cyclopamine后，观察到显著的外部缺陷，包括单眼、小眼、象鼻形成、无肢、胸椎前凸和体积减小[2]。与tomatidine对照组相比，cyclopamine处理使来自食道、胃、胆道和胰腺的肿瘤细胞系的生长降低了75-95%[3]。在胰腺癌细胞系中，使用cyclopamine进行Hh抑制，导致snail的下调和E-细胞黏附分子的上调，与上皮-间质转变的抑制一致，并且通过体外侵袭能力的显著降低得到反映(P < 0.0001)[4]。
体内活性	为了考察Cyclopamine治疗在活体内的效果，首先在无胸腺小鼠中建立了来自HUCCT1细胞的皮下异种移植物，这些细胞来自于具有转移性的胆管癌细胞系。在Cyclopamine处理的动物中，肿瘤在12天内完全消退[3]。在延迟治疗模型中，对比未治疗的对照组，使用Cyclopamine(1.2 mg)处理的BxPC3-SMOlow肿瘤在重量上没有差异。相反，Panc 05.04和L3.6sl来源的肿瘤质量分别观察到了50-60%的减少（见图5b, c）—并且，在同时治疗模型中，L3.6sl来源的肿瘤质量减少了84%，显示了更显著的效果[5]。
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 4.12 mg/mL (10 mM), Sonication is recommended.
关键字	Endogenous Metabolite \| Hedgehog \| Smoothened \| inhibit \| Cyclopamine \| Smo \| Inhibitor
相关产品	Formamide \| Oleamide \| Guanidine hydrochloride \| Naringin \| Daidzein \| Glycerol \| Sucrose \| Ferulic Acid \| Thymidine \| Fumaric acid
相关库	抑制剂库 \| 抗癌活性化合物库 \| 植物来源化合物库 \| 古代经典名方目录分子库 \| 生物碱类天然产物库 \| 药食同源库 \| 天然产物库 \| 中药单体化合物库 \| GPCR靶点分子库 \| 膜蛋白靶向化合物库

环巴胺|||11-Deoxojervine|TargetMol

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期	(12年)
注册资本	566.2651万人民币
员工人数	100-500人
年营业额	￥ 1亿以上
经营模式	贸易,试剂,定制,服务
主营行业	化学试剂,生物活性小分子