維莫德吉|T2590

價(jià)格	￥575	￥897	￥2260
包裝	5mg	10mg	50mg

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:維莫德吉	英文名稱:Vismodegib
CAS:879085-55-9	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: 99.99%	產(chǎn)品類別: 抑制劑
貨號(hào): T2590

Product Introduction

Bioactivity

名稱	Vismodegib
描述	Vismodegib (GDC-0449) is a hedgehog pathway inhibitor (IC50: 3 nM). It also inhibits P-gp (IC50: 3.0 μM), ABCG2 (IC50: 1.4 μM).
細(xì)胞實(shí)驗(yàn)	MDCKII cells were plated into 24-well plates at a density of 3 x 10^5 cells per well and were allowed to attach. The medium was then changed to that containing different drugs (50 μM VP, 50 μM indomethacin, or 20 μM Vismodegib) in DMSO or DMSO alone as control, and nonfluorescent calcein-AM was added to a final concentration of 1.0 μM and incubated at 37°C for 2 hours. Cells were then washed twice with Ca2+, Mg2+-containing Hank's balanced salt solution buffer and lysed by shaking in 0.01% Triton X-100 in PBS buffer for 1 hour at room temperature or overnight at 4°C. The lysate was then transferred into 96-well plates, and the fluorescence signal caused by the cell-derived calcein was quantified spectrophotometrically with a SpectraMax M5 Multi-Detection Reader using an excitation wavelength of 495 nm and an emission wavelength of 515 nm. All manipulations were performed in the dark. All readings are expressed as mean ± SEM normalized to the control [2].
動(dòng)物實(shí)驗(yàn)	Female CD-1 nude mice (weighing 25–28 g) were administered oral doses of 5, 15, 50, and 100 mg/kg (free base equivalent) of vismodegib hydrochloride salt in 0.5% methylcellulose/0.2% Tween 80 (MCT). Blood samples (～1 mL) were collected up to 24 hours postdose via cardiac puncture (terminal collection) into tubes containing potassium ethylenediaminetetraacetic acid (K2EDTA) anticoagulant. Immediately on the collection, the blood was mixed with K2EDTA and stored on ice. Within 30 minutes, blood samples were centrifuged at approximately 1000 to 1500 × g for 5 minutes at 4°C, and plasma was harvested. The plasma samples were stored at ?80°C until analysis. Concentrations of vismodegib were determined by LC/MS/MS as described previously [4].
體外活性	Vismodegib (GDC-0449) 是針對(duì)兩種ABC轉(zhuǎn)運(yùn)蛋白，ABCG2/BCRP 和 ABCB1/Pgp 的強(qiáng)效抑制劑，并對(duì) ABCC1/MRP1 表現(xiàn)出溫和的抑制作用。在過(guò)表達(dá)ABCG2 的HEK293細(xì)胞中，Vismodegib 增加了熒光ABCG2底物BODIPY-prazosin的保留，并使這些細(xì)胞重新對(duì)抗腫瘤藥物mitoxantrone敏感。此外，Vismodegib 還使過(guò)表達(dá)ABCG2的人類非小細(xì)胞肺癌細(xì)胞 NCI-H460/par 和 NCI-H460/MX20 對(duì)mitoxantrone、topotecan 或 SN-38 重新敏感。Vismodegib 抑制ABCG2 和 Pgp 的IC(50) 值分別約為1.4 μM 和約3.0 μM [2]。在對(duì)順鉑敏感和耐藥的細(xì)胞中，GDC-0449 均抑制了細(xì)胞生長(zhǎng)。在這兩種細(xì)胞類型中，GDC-0449 增加了[Ca(2+)](cyto) 并減少了內(nèi)質(zhì)網(wǎng)中的[Ca(2+)](ER) [3]。
體內(nèi)活性	經(jīng)口給予vismodegib在Ptch(+/-)同種異體移植的小腦髓質(zhì)瘤模型中，當(dāng)劑量≥25 mg/kg時(shí)可引起腫瘤退縮。在兩種配體依賴的CRC模型D5123和1040830中，vismodegib劑量高達(dá)92 mg/kg并每日兩次給藥時(shí)可抑制腫瘤生長(zhǎng)。通過(guò)分析Hh通路活性和PK/PD建模顯示，vismodegib在這兩種模型中抑制Gli1的IC(50)相似（分別為0.165 μmol/L ±11.5%和0.267 μmol/L ±4.83%）。該路徑調(diào)控與療效的關(guān)聯(lián)通過(guò)一個(gè)整合的PK/PD模型揭示，其中vismodegib活性> 50%與Hh路徑>80%的抑制呈陡峭關(guān)系[4]。
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 : 50 mg/mL (118.68 mM) Ethanol : Insoluble H2O : Insoluble
關(guān)鍵字	GDC0449 \| Hedgehog \| Inhibitor \| RG3616 \| Vismodegib \| inhibit \| RG-3616 \| Autophagy \| GDC 0449
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Naringin \| Valproic Acid \| Taurine \| Gefitinib \| Aceglutamide \| Hydroxychloroquine \| Curcumin \| Stavudine \| Salicylic acid \| Paeonol \| Sodium 4-phenylbutyrate
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗癌上市藥物庫(kù) \| EMA 上市藥物庫(kù) \| 抗衰老化合物庫(kù) \| 離子通道庫(kù) \| FDA 上市藥物庫(kù) \| 抗癌臨床化合物庫(kù)

關(guān)鍵字：維莫德吉|||RG 3616|||GDC-0449|||Erivedge|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)

TargetMol中國(guó)（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊(cè)資本：566.2651萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓

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