艾力替尼|T6331|TargetMol

價(jià)格	￥463	￥1160	￥1860
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:艾力替尼	英文名稱:Allitinib tosylate
CAS:1050500-29-2	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: 98.52%	產(chǎn)品類別: 抑制劑
貨號(hào): T6331

Product Introduction

Bioactivity

名稱	Allitinib tosylate
描述	Allitinib tosylate (AST-1306) is a novel irreversible inhibitor of EGFR and ErbB2 with IC50 of 0.5 nM and 3 nM, respectively.
細(xì)胞實(shí)驗(yàn)	Cell (including Calu-3, A-549 cell line et al.) proliferation is evaluated using the SRB (Sulforhodamine B) assay. Briefly, cells are seeded into 96-well plates and grown for 24 hours. The cells are then treated with increasing concentrations of AST-1306 and grown for a further 72 hours. The medium remains unchanged until the completion of the experiment. The cells are then fixed with 10% precooled trichloroacetic acid (TCA) for 1 hour at 4 °C and stained for 15 min at room temperature with 100 μL of 4 mg/mL SRB solution in 1% acetic acid. The SRB is then removed, and the cells are quickly rinsed five times with 1% acetic acid. After cells are air-dried, protein-bound dye is dissolved in 150 μL of 10 mM Tris base for 5 min and measured at 515 nm using a multiwell spectrophotometer. The inhibition rate on cell proliferation is calculated as (1 - A515 treated/A515 control) × 100%. The IC50 value is obtained by the Logit method and is determined from the results of at least 3 independent tests.(Only for Reference)
激酶實(shí)驗(yàn)	Tyrosine kinase assays: The tyrosine kinase activities are determined in 96-well ELISA plates precoated with 20 μg/mL Poly (Glu,Tyr)4:1. First, 80 μL of 5 μM ATP solution diluted in kinase reaction buffer (50 mM HEPES pH 7.4, 20 mM MgCl2, 0.1 mM MnCl2, 0.2 mM Na3VO4, 1 mM DTT) is added to each well. Various concentrations of AST-1306 diluted in 10 μL of 1% DMSO (v/v) are then added to each reaction well, with 1% DMSO (v/v) used as the negative control. Subsequently, the kinase reaction is initiated by the addition of purified tyrosine kinase proteins diluted in 10 μL of kinase reaction buffer solution. Experiments at each concentration are performed in duplicate. After incubation for 60 min at 37 °C, the plate is washed three times with phosphate buffered saline (PBS) containing 0.1% Tween 20 (T-PBS). Next, 100 μL anti-phosphotyrosine antibody (PY99, 1:500 dilution) diluted in T-PBS containing 5 mg/mL BSA is added. After 30 min incubation at 37 °C, the plate is washed three times as before. Horseradish peroxidase-conjugated goat anti-mouse IgG (100 μL) diluted 1:2000 in T-PBS containing 5 mg/mL BSA is added. The plate is reincubated at 37 °C for 30 min, and then washed with PBS. Finally, 100 μL of a solution containing 0.03 % Water2 and 2 mg/mL o-phenylenediamine in 0.1 M citrate buffer, pH 5.5, is added and samples are incubated at room temperature until color emerged. The reaction is terminated by the addition of 50 μL of 2 M H2SO4, and the plate is read using a multi-well spectrophotometer at 490 nm. The inhibition rate (%) is calculated using the following equation: [1-(A490 treated /A490 control)] ×100%. IC50 values are determined from the results of at least three independent tests and calculated by Logit method.
體外活性	Allitinib同時(shí)針對(duì) ErB2 和 EGFR T790M/L858R 雙突變體。 Allitinib的活性大約是 lapatinib 的 500 倍，并且針對(duì) ErbB 家族激酶相較于其他激酶家族（包括 PDGFR、KDR 和 c-Met）的選擇性超過 3000 倍。 Allitinib可能與 EGFR 和 ErbB2 的特定氨基酸殘基形成共價(jià)結(jié)合。 Allitinib以濃度依賴的方式顯著抑制 HIH3T3-EGFR T790M/L858R 細(xì)胞的生長(zhǎng)，并有效抑制這些細(xì)胞中 EGFR 的磷酸化。此外， Allitinib在濃度依賴的方式中阻斷帶有 EGFR T790M/L858R 突變的 NCI-H1975 細(xì)胞的生長(zhǎng)，并阻斷 EGFR 及其下游途徑的磷酸化。同時(shí)， Allitinib以劑量依賴的方式明顯抑制 A549 細(xì)胞中 EGF 誘導(dǎo)的 EGFR 磷酸化。 Allitinib抑制 EGFR 和 ErbB2 的磷酸化及包括 A549 細(xì)胞、Calu-3 細(xì)胞和 SK-OV-3 細(xì)胞在內(nèi)的人類癌癥細(xì)胞的下游信號(hào)傳導(dǎo)。[1]
體內(nèi)活性	每日兩次口服AST-1306能顯著防止SK-OV-3和Calu-3異種移植模型中的腫瘤生長(zhǎng)。在SK-OV-3模型中，經(jīng)過7天的AST-1306治療，腫瘤幾乎消失。相反，在HO-8910和A549異種移植模型中，AST-1306僅輕微抑制腫瘤生長(zhǎng)。因此，AST-1306在過表達(dá)ErbB2的腫瘤模型中的抗腫瘤效能大于在低表達(dá)ErbB2的模型中。AST-1306具有良好的耐受性。雖然Lapatinib在這些過表達(dá)ErbB2的腫瘤模型中顯示出抗腫瘤活性，但與Lapatinib相比，AST-1306在相同劑量和計(jì)劃下治療SK-OV-3異種移植腫瘤模型時(shí)更加有效。此外，每日兩次口服AST-1306連續(xù)3周顯著抑制了FVB-2/Nneu模型中的腫瘤生長(zhǎng)。治療11天后，腫瘤幾乎完全消失。治療期間，小鼠體重減少不到20%。[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	H2O : < 1 mg/mL (insoluble or slightly soluble) Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 114 mg/mL (183.6 mM)
關(guān)鍵字	inhibit \| AST1306 \| Epidermal growth factor receptor \| EGFR \| ErbB-1 \| Allitinib Tosylate \| Inhibitor \| Irreversible \| AST 6 \| AST 1306 \| Allitinib tosylate \| TsOH \| HER1 \| anilino-quinazoline \| AST6 \| anti-cancer
相關(guān)產(chǎn)品	Lapatinib \| Neratinib \| Chalcone \| Gefitinib \| Erlotinib \| Osimertinib \| Erlotinib hydrochloride \| Gilteritinib \| Lidocaine Hydrochloride hydrate \| Genistein \| Nintedanib \| Sorafenib
相關(guān)庫	抑制劑庫 \| 抗癌活性化合物庫 \| 經(jīng)典已知活性庫 \| 激酶抑制劑庫 \| 高選擇性抑制劑庫 \| 膜蛋白靶向化合物庫 \| 酪氨酸激酶分子庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關(guān)鍵字：艾力替尼|||AST-6|||AST-1306 TsOH|||AST-1306 (TsOH)|||AST-1306|||Allitinib|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)國家和地區(qū)，已發(fā)展成為全球知名的化合物庫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，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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