環(huán)巴胺|T2825|TargetMol

價(jià)格	￥484	￥753	￥1380
包裝	5mg	10mg	25mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:環(huán)巴胺	英文名稱:Cyclopamine
CAS:4449-51-8	品牌: TargetMol
產(chǎn)地: 美國(guó)	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 99.66%	產(chǎn)品類別: 抑制劑
貨號(hào): T2825

Product Introduction

Bioactivity

名稱	Cyclopamine
描述	Cyclopamine (11-Deoxojervine), a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids.
細(xì)胞實(shí)驗(yàn)	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].
激酶實(shí)驗(yàn)	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].
動(dòng)物實(shí)驗(yàn)	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].
體外活性	將雞胚胎暴露于cyclopamine后，觀察到顯著的外部缺陷，包括單眼、小眼、象鼻形成、無(wú)肢、胸椎前凸和體積減小[2]。與tomatidine對(duì)照組相比，cyclopamine處理使來(lái)自食道、胃、膽道和胰腺的腫瘤細(xì)胞系的生長(zhǎng)降低了75-95%[3]。在胰腺癌細(xì)胞系中，使用cyclopamine進(jìn)行Hh抑制，導(dǎo)致snail的下調(diào)和E-細(xì)胞黏附分子的上調(diào)，與上皮-間質(zhì)轉(zhuǎn)變的抑制一致，并且通過(guò)體外侵襲能力的顯著降低得到反映(P < 0.0001)[4]。
體內(nèi)活性	為了考察Cyclopamine治療在活體內(nèi)的效果，首先在無(wú)胸腺小鼠中建立了來(lái)自HUCCT1細(xì)胞的皮下異種移植物，這些細(xì)胞來(lái)自于具有轉(zhuǎn)移性的膽管癌細(xì)胞系。在Cyclopamine處理的動(dòng)物中，腫瘤在12天內(nèi)完全消退[3]。在延遲治療模型中，對(duì)比未治療的對(duì)照組，使用Cyclopamine(1.2 mg)處理的BxPC3-SMOlow腫瘤在重量上沒(méi)有差異。相反，Panc 05.04和L3.6sl來(lái)源的腫瘤質(zhì)量分別觀察到了50-60%的減少（見(jiàn)圖5b, c）—并且，在同時(shí)治療模型中，L3.6sl來(lái)源的腫瘤質(zhì)量減少了84%，顯示了更顯著的效果[5]。
存儲(chǔ)條件	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.
關(guān)鍵字	Endogenous Metabolite \| Hedgehog \| Smoothened \| inhibit \| Cyclopamine \| Smo \| Inhibitor
相關(guān)產(chǎn)品	Oleamide \| p-Hydroxybenzaldehyde \| Guanidine hydrochloride \| Naringin \| Daidzein \| Glycerol \| Sucrose \| Oxalic acid dihydrate \| Ferulic Acid \| 3-Indoleacetic acid \| Thymidine \| Fumaric acid
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗癌活性化合物庫(kù) \| 植物來(lái)源化合物庫(kù) \| 古代經(jīng)典名方目錄分子庫(kù) \| 生物堿類天然產(chǎn)物庫(kù) \| 藥食同源庫(kù) \| 天然產(chǎn)物庫(kù) \| 中藥單體化合物庫(kù) \| GPCR靶點(diǎn)分子庫(kù) \| 膜蛋白靶向化合物庫(kù)

關(guān)鍵字：環(huán)巴胺|||11-Deoxojervine|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)慕尼黑的同事一起，為北美、歐洲和亞洲從事藥物研發(fā)和生物學(xué)研究的科學(xué)家提供優(yōu)質(zhì)的產(chǎn)品和專業(yè)的服務(wù)。公司下設(shè)篩選事業(yè)部，化學(xué)事業(yè)部，生物事業(yè)部和新材料部。從虛擬篩選到實(shí)體化合物分子供應(yīng)；從商業(yè)化產(chǎn)品銷售到個(gè)性化定制合成；從對(duì)明確靶點(diǎn)的分子篩選到對(duì)明確分子的多靶點(diǎn)篩選，從高通量篩選到化學(xué)結(jié)構(gòu)優(yōu)化，我們都可以滿足您的科研用品及技術(shù)服務(wù)的需求。經(jīng)過(guò)在中國(guó)市場(chǎng)五年的精心耕耘，我們已成為篩選化合物領(lǐng)域優(yōu)秀的供應(yīng)商，為超過(guò)五百家學(xué)校和各類企業(yè)提供了品質(zhì)卓越的小分子化合物和藥物篩

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.2651萬(wàn)人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

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公司成立：12年
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