化合物 PD158780|T5410|TargetMol

價(jià)格	￥239	￥540	￥930
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-29

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產(chǎn)品詳情

中文名稱:化合物 PD158780	英文名稱:PD158780
CAS:171179-06-9	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: 98.81%	產(chǎn)品類別: 抑制劑
貨號(hào): T5410

Product Introduction

Bioactivity

名稱	PD158780
描述	PD 158780 reversibly inhibits auto and transphosphorylation of all four members of the ErbB receptor superfamily: EGFR, ErbB2, ErbB3, and ErbB4 (IC50s: 8μM, 49 nM, 52 nM, and 52 nM in cell assay).
細(xì)胞實(shí)驗(yàn)	All cell lines were maintained as monolayers in dMEM/F12, 50:50 containing 10% fetal bovine serum. For growth inhibition assays, dilutions of the designated compound in 10 μL were placed in 24-well Linbro plates (1.7 x 1.6 cm, flat bottom) followed by the addition of cells (2 × 10^4) in 2 mL of medium. The plates were incubated for 72 hr at 37 °C in a humidified atmosphere containing 5% CO 2 in air. Cell growth was determined by counting cells with a Coulter model AM electronic cell counter. For clone formation in soft agar, cells were trypsinized, and 10,000 cells/mL were seeded into DMEM/F12 medium containing 10% fetal bovine serum, 0.4% agarose, and the designated concentration of compound. One milliliter of this solution was placed over a bottom layer of the same medium containing 0.8% agarose in a 35-mm Petri dish and incubated at 37 °C in a humidified atmosphere containing 5% CO 2 in air. After 3 weeks, colonies were stained with p-iodonitrotetrazolium violet (INT) and quantitated with an image analyzer using the software NIH Image version 1.55. Incorporation of radiolabeled thymidine into cellular DNA was monitored by exposing compound-treated or control cells to [methyl)H]thymidine at a concentration of 1 μM and specific activity of 1 μCi/nmol. After 2 hr the cells were trypsinized and injected into 2 mL of ice-cold 15% trichloroacetic acid (TCA). The resulting precipitate was collected on glass fiber filters, washed five times with 2-mL aliquots of ice-cold 15% TCA, dried, and placed in scintillation vials plus 10 mL Ready gel [1].
激酶實(shí)驗(yàn)	Epidermal growth factor receptor was prepared from human A431 carcinoma cell shed membrane vesicles by immunoaffinity chromatography as previously described, and the assays were carried out as reported previously. The substrate used was based on a portion of phospholipase Cγ1, having the sequence Lys-His-Lys-Lys-LeuAla-Glu-Gly-Ser-Ala-Tyr472-Glu-Glu-Val. The reaction was allowed to proceed for 10 min at room temperature and then was stopped by the addition of 2 mL of 75 mM phosphoric acid. The solution was then passed through a 2.5 cm phosphocellulose disk which bound the peptide. This filter was washed with 75 mM phosphoric acid (5×), and the incorporated label was assessed by scintillation counting in an aqueous fluor. Control activity (no drug) gave a count of approximately 100 000 cpm. At least two independent dose-response curves were done and the IC50 values computed. The reported values are averages; variation was generally ±15% [1].
體外活性	PD158780在A431人類表皮樣癌細(xì)胞中抑制了EGF受體的自磷酸化作用，IC50值為13 nM。PD158780對(duì)EGF受體具有很高的特異性，在Swiss 3T3成纖維細(xì)胞中，以低納摩爾濃度抑制了依賴EGF的受體自磷酸化和胸腺嘧啶的摻入。PD158780還抑制了SK-BR-3和MDA-MB-453乳腺癌細(xì)胞中由heregulin刺激的磷酸化作用，IC50值分別為49 nM和52 nM [1]。
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 : 8 mg/mL (24.23 mM) DMSO : 30 mg/mL (90.86 mM)
關(guān)鍵字	Inhibitor \| PD158780 \| PD 158780 \| Epidermal growth factor receptor \| inhibit \| PD-158780 \| HER1 \| EGFR \| ErbB-1
相關(guān)產(chǎn)品	Lapatinib \| Neratinib \| Chalcone \| Gefitinib \| Erlotinib \| Osimertinib \| Erlotinib hydrochloride \| Afatinib Dimaleate \| Lidocaine Hydrochloride hydrate \| Genistein \| Khellin \| Osimertinib mesylate
相關(guān)庫(kù)	抑制劑庫(kù) \| 血管生成庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| 抗結(jié)直腸癌化合物庫(kù) \| 激酶抑制劑庫(kù) \| JAK-STAT 化合物庫(kù) \| 抗卵巢癌化合物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(kù)

關(guān)鍵字： PD158780|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。

成立日期	2013-04-18 （12年）	注冊(cè)資本	566.265100萬(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)	天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù)	經(jīng)營(yíng)模式	貿(mào)易,工廠,試劑,定制,服務(wù)

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公司成立：12年
注冊(cè)資本：566.265100萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
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公司地址：靜安區(qū)江場(chǎng)三路238號(hào)8樓

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