達(dá)拉非尼|T1903

1篇文獻(xiàn)

價(jià)格	￥541	￥697	￥995
包裝	5mg	10mg	25mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2025-03-12

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產(chǎn)品詳情

中文名稱:達(dá)拉非尼	英文名稱:Dabrafenib
CAS:1195765-45-7	品牌: TargetMol
產(chǎn)地: 美國	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: 99.83%	產(chǎn)品類別: 抑制劑
貨號(hào): T1903

Product Introduction

Bioactivity

名稱	Dabrafenib
描述	Dabrafenib (GSK2118436A) is a Raf inhibitor that inhibits C-Raf and B-RafV600E (IC50=5/0.6 nM) and is ATP-competitive. Dabrafenib exhibits antitumor activity for the treatment of B-RafV600E-mutated melanoma.
細(xì)胞實(shí)驗(yàn)	A375P-F11 assay: A375P cells were plated in 96-well plates by limiting dilution and single cell-derived clones were harvested and tested for sensitivity to B-Raf inhibitors. The F11 clone was selected for future studies and was named A375P-F11. Cellular pSmad Assay to Measure Anti-TGF-β Activity: Activity of compounds was tested in a mechanistic assay in HepG2 cells. Cells were seeded in 12-well plates at a density of 500,000 cells/well and allowed to adhere overnight at 37℃/5% CO2. Media (BME+10% serum) was removed and compound in serum-free media was added to the cells for 45 minutes at 37℃/5% CO2. Cells were stimulated with 1 ng/ml TGF-β for 60 minutes. Cells were lysed in buffer (25 mM Tris-HCl ph: 7.5, 2 mM EDTA, 2 mM EGTA,1% Triton X-100, 0.1 % SDS, 50 mM sodium-β-glycerophosphate, 2 mM sodium orthovanadate, 12.5 mM sodium pyrophosphate, protease and phosphatase inhibitor cocktails) for 30 minutes, scraped, collected, clarified by centrifugation and prepared for western blots in LDS/reducing reagent. Samples were resolved on 4-12% Bis-Tris gels, transferred to PVDF, and probed for total and phospho-Smad2 using antibodies. Gels were imaged using the odyssey blot scanner and quantified. Phospho:total Smad2 ratios were determined and the IC50 was defined as the concentration of compound which decreased the phospho:total ratio by 50% [1].
動(dòng)物實(shí)驗(yàn)	Cells were implanted in nude mice and grown as tumor xenografts. Dosing began when tumors achieved ~150-200mm^3 volume. GSK2118436 was administered by oral gavage at a dose volume of 0.2 mL/20 gram body weight in 0.5% hydroxypropylmethylcellulose and 0.2% Tween-80 in distilled water pH 8.0. Dosing was daily for duration stipulated. Results are reported as mean tumor volume for n=7-8 mice/group. Tumors were measured twice weekly with Vernier calipers, and tumor volume was estimated from two-dimensional measurements using a prolate ellipsoid equation (Tumor volume mm^3 = (length x width^2) x 0.5). Complete tumor regression was defined as a >93% decrease in an individual tumor volume for at least 1 week [1].
體外活性	方法：195 種腫瘤細(xì)胞用 Dabrafenib 處理 72 h，使用 CellTiter-Glo Assay 檢測(cè)細(xì)胞生長(zhǎng)。結(jié)果：編碼 BRAFV600E 的 20 個(gè)細(xì)胞系中有 16 個(gè)對(duì) Dabrafenib 敏感 (gIC50<200 nM)。其他 5 個(gè)突變 BRAF 細(xì)胞系中的 3 個(gè)對(duì) Dabrafenib 敏感 (gIC50<30nM)，包括 WM-115(BRAFV600D) 和 YUMAC(BRAFV600K)。152 個(gè) RAS/RAF 野生型中的133個(gè)和所有 18 個(gè)突變 RAS 細(xì)胞系對(duì) Dabrafenib 不敏感 (gIC50>10μM)。[1] 方法：黑色素瘤細(xì)胞株 LCP(BRAFV600R)、WM266 (BRAFV600D) 和 M257 (BRAFWT) 用 Dabrafenib (3-100 nM) 處理 72 h，使用 Western Blot 檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：與具有野生型 BRAF 的對(duì)照細(xì)胞相比，具有 BRAFV600D/R 突變的細(xì)胞系對(duì)磷酸化 ERK 表現(xiàn)出更快更強(qiáng)的抑制作用。[2]
體內(nèi)活性	方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Dabrafenib (3-100 mg/kg，0.5% hydroxypropylmethylcellulose+0.2% Tween 80 in pH 8.0 distilled water) 灌胃給藥給攜帶人結(jié)直腸癌腫瘤 Colo 205 (BRAFV600E) 的 CD1 nu/nu 小鼠，每天一次，持續(xù)十四天。結(jié)果：Dabrafenib 顯示出劑量依賴性的腫瘤生長(zhǎng)抑制作用，8 只小鼠中有 4 只在 100 mg/kg 劑量下顯示出部分消退。[1] 方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Dabrafenib (0.1-100 mg/kg，0.5% hydroxypropylmethylcellulose+0.2% Tween 80 in pH 8.0 distilled water) 灌胃給藥給攜帶人惡性黑色素瘤 A375P F11 (BRAFV600E) 的 CD1 nu/nu 小鼠，每天一次，持續(xù)十四天。結(jié)果：Dabrafenib 可顯著減少攜帶 B-RafV600E 人類黑色素瘤腫瘤的小鼠的腫瘤生長(zhǎng)。100 mg/kg 組中，50% 的治療動(dòng)物觀察到腫瘤完全消退。[3]
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	Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2.8 mg/mL (5.39 mM), Please add co-solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. DMSO : 55 mg/mL (105.86 mM)
關(guān)鍵字	GSK-2118436 \| inhibit \| Dabrafenib \| Raf kinases \| GSK 2118436 \| Inhibitor \| Raf
相關(guān)產(chǎn)品	Pelitinib \| Doramapimod \| Vemurafenib \| Sorafenib tosylate \| Exarafenib \| PLX-4720 \| Regorafenib \| Sorafenib \| GW 441756 \| Regorafenib monohydrate \| Sulindac sulfide \| LY3009120
相關(guān)庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 已知活性化合物庫 \| EMA 上市藥物庫 \| 激酶抑制劑庫 \| 疼痛相關(guān)化合物庫 \| 酪氨酸激酶分子庫 \| FDA 上市激酶抑制劑庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字：達(dá)拉非尼|||GSK2118436A|||GSK2118436|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國波士頓、德國慕尼黑的同事一起，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)過在中國市場(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	566.2651萬人民幣
員工人數(shù)	100-500人	年?duì)I業(yè)額	￥ 1億以上
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公司成立：12年
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