化合物 Palomid 529|T2706|TargetMol

價(jià)格	￥186	￥413	￥662
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 Palomid 529	英文名稱:Palomid 529
CAS:914913-88-5	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: 99.03%	產(chǎn)品類別: 抑制劑
貨號(hào): T2706

Product Introduction

Bioactivity

名稱	Palomid 529
描述	Palomid 529 (SG 00529) has been used in trials studying the treatment of Age-Related Macular Degeneration.
細(xì)胞實(shí)驗(yàn)	Human umbilical vascular endothelial cells (HUVEC) are used. The proliferation assay is carried out by seeding the HUVECs in 96-well plates at a density of 1,000 per well in complete medium. Following a 24-hour plating period, the cells are starved for 24 hours in 0.5% serum before being treated with Palomid 529 in the presence of 10 ng/mL basic fibroblast growth factor (bFGF) or VEGF in complete medium. After 48 hours, cell number is determined using a colorimetric method. The results are expressed as the percentage of the maximal bFGF or VEGF response in the absence of Palomid 529. Nonproliferating endothelial cells are assayed by growing HUVECs to quiescence in 96-well plates and treating with Palomid 529 for 48 hours. Initially, 5,000 cells per well are seeded and confluence is achieved the next day. The plates are incubated for another 24 hours to ensure growth arrest before treatment with Palomid 529. (Only for Reference)
激酶實(shí)驗(yàn)	Estrogen receptor binding assays: The proteins are produced with rabbit reticulocyte lysates. The amount of template used in each reaction is determined empirically and expression is monitored in parallel reactions where [35S]methionine is incorporated into the receptor followed by gel electrophoresis and exposure to film. Binding reactions of the estrogen receptors (ER) and Palomid 529 are carried out in 100 mL final volumes in TEG buffer [10 mM Tris (pH 7.5), 1.5 mM EDTA, 10% glycerol]. In vitro transcribed-translated receptor (5 μL) is used in each binding reaction in the presence of 0.5 nM [3H]estradiol (E2). Palomid 529 is routinely tested from 10?11 to 10?6 M and diluted in ethanol. The reactions are incubated at 4 °C overnight and bound E2 is quantified by adding 200 mL dextran-coated charcoal. After a 15-minutes rotation at 4 °C, the tubes are centrifuged for 10 minutes and 150 mL of the supernatant are added to 5 mL scintillation mixture for determination of cpm by liquid scintillation counting. The maximum binding is determined by competing bound E2 with only the ethanol vehicle. Controls for background are included in each experiment using 5 mL unprogrammed rabbit reticulocyte lysate. This value, typically 10% to 15% of the maximal counts, is subtracted from all values. The data are plotted and Ki values are calculated. Experiments are conducted at least thrice in duplicate.
體外活性	Palomid 529抑制腫瘤生長(zhǎng),血管生成和血管通透性.在兔視網(wǎng)膜脫離模型中,Palomid 529可有效抑制Müller細(xì)胞增殖,神經(jīng)膠質(zhì)瘢痕形成和感光細(xì)胞死亡.Palomid 529劑量依賴性抑制Ad-VEGF-A驅(qū)動(dòng)的血管生成,裸鼠灌胃Palomid 529可抑制C6V10膠質(zhì)瘤生長(zhǎng).與對(duì)照組相比,Palomid 529處理PC-3腫瘤小鼠可減少57.1%的腫瘤生長(zhǎng).Palomid 529明顯抑制小鼠Brca1缺失腫瘤生長(zhǎng)模型中Akt和 mTOR信號(hào)通路.
體內(nèi)活性	Palomid529不僅降低缺血性視網(wǎng)膜的增殖,而且能改善血管形成的組織和結(jié)構(gòu)。Palomid 529抑制VEGF介導(dǎo)和bFGF介導(dǎo)的內(nèi)皮細(xì)胞增殖,IC 50分別為20 nM 和30 nM。Palomid 529可誘導(dǎo)內(nèi)皮細(xì)胞凋亡,降低血管內(nèi)皮生長(zhǎng)因子VEGF-A誘導(dǎo)的pAktS473,pGSK3βS9和pS6磷酸化。在肺癌NCI- 60細(xì)胞系中,Palomid 529顯示高效的抗增殖活性,GI50< 35 μM。此外,Palomid 529可顯著增強(qiáng)輻射對(duì)前列腺癌細(xì)胞（PC-3）的抗增殖作用。Palomid 529對(duì)PC-3細(xì)胞產(chǎn)生濃度依賴性生長(zhǎng)抑制。Palomid 529抑制PC-3中輻射誘導(dǎo)的p-Akt激活,并降低Bcl-2/Bax的比例。
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) DMSO : 50 mg/mL (123.02 mM), Sonication is recommended.
關(guān)鍵字	mTOR \| Apoptosis \| P-529 \| Palomid-529 \| Inhibitor \| Palomid529 \| P 529 \| SG00529 \| Mammalian target of Rapamycin \| Palomid 529 \| SG-00529 \| inhibit
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相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 抗癌活性化合物庫(kù) \| 已知活性化合物庫(kù) \| 激酶抑制劑庫(kù) \| 抗衰老化合物庫(kù) \| 藥物功能重定位化合物庫(kù) \| 抗癌臨床化合物庫(kù) \| 神經(jīng)元分化化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字： SG 00529|||P529|TargetMol

公司簡(jiǎn)介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)國(guó)家和地區(qū)，已發(fā)展成為全球知名的化合物庫(kù)和小分子化合物研究供應(yīng)商。 TargetMol?可提供160多種滿足不同需求的化合物庫(kù)，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學(xué)試劑盒等，此外，我們還建設(shè)有CADD（計(jì)算機(jī)輔助藥物設(shè)計(jì)）研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺(tái)三大技術(shù)中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結(jié)果。

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