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雷度替尼,Radotinib

雷度替尼|T2328|TargetMol

價(jià)格 258 413 622
包裝 2mg 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(chēng):雷度替尼英文名稱(chēng):Radotinib
CAS:926037-48-1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: 99.97%產(chǎn)品類(lèi)別: 抑制劑
貨號(hào): T2328
2024-12-12 雷度替尼 Radotinib 2mg/258RMB;5mg/413RMB;10mg/622RMB 258 TargetMol 美國(guó) Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. 99.97% 抑制劑

Product Introduction

Bioactivity

名稱(chēng)Radotinib
描述Radotinib (IY-5511), and sometimes referred to by its investigational name IY5511, is a drug for the treatment of different types of Y, most notably Philadelphia chromosome-positive (Ph+) chronic myeloid leukemia (CML) with resistance or intolerance of other tyrosine kinase Bcr-Abl inhibitors
細(xì)胞實(shí)驗(yàn)Cells are seeded in 96-well plates at a density of 2×104 cells/ml with 100 μL of medium per well and then incubated with various concentrations of radotinib (0, 1, 10, and 100 μM) for 72 h at 37°C. The CellTiter 96 solution (20 μL) is added directly to each well and plates are incubated for 4 h in a humidified 5% CO2 atmosphere at 37°C. Absorbance is measured with a PowerWave XS2 Microplate Spectrophotometer at 490 nm and the results are expressed as percentage changes from the basal condition using four to five culture wells for each experimental treatment. In some experiments, HL60 cells are cultured with 100 nM ATRA and 1 μM dasatinib for 4 days, and 10 μM radotinib is added to each group according to the planned schedule(Only for Reference)
激酶實(shí)驗(yàn)Autophosphorylation of EGFR in cells: For experiments using cells in culture, A431 cells are treated with various concentrations of Pelitinib for 2.75 hours before co-incubation with 100 ng/mL EGF for 0.25 hour. Cells are washed twice with cold phosphate-buffered saline (PBS) before adding to lysis buffer (10 mM Tris, pH 7.5, 5 mM ethylenediamine tetra-acetic acid (EDTA), 150 mM NaCl, 1% Triton X-100, 1% Sodium deoxycholate, 0.1 % SDS, 1 mM PMSF, 10 mg/mL pepstatin A, 10 mg/mL leupeptin, 20 KIU/mL aprotinin, 2 mM sodium orthovanadate, and 100 mM sodium fluoride) for 20 minutes on ice, before immunoprecipitation and SDS-PAGE-immunoblotting. For immunoprecipitation, cultured cells are placed in cold lysis buffer and immediately homogenized on ice with a polytron with several pulses. The homogenate is first centrifuged at 2500 rpm (20 minutes, 4 °C) and then again at 14,000 rpm in a microcentrifuge (10 minutes, 4 °C). Supernatants (1000 μg protein) are incubated for 2 hours at 4 °C with 15 mL of EGFR polyclonal antibody. After 2 hours, 50 μL of protein G plus/protein A agarose beads is added and incubated with constant rotation for 2 hours at 4 °C. After washing with lysis buffer, beads are boiled for 2 minutes in Laemmli sample buffer. Proteins are then resolved by SDS-PAGE, transferred to immobilon membrane and probed overnight with an anti-phosphotyrosine antibody conjugated with horseradish peroxidase (HRP). Membranes are developed using the ECL reagent. Total EGFR protein is determined by stripping membranes and re-probing with receptor-specific antibodies. Quantitation of bands is done by densitometry, using ImageQuant software with a Molecular Dynamics laser transmittance scanner.
體外活性體外實(shí)驗(yàn)中,Radotinib結(jié)合BCR-ABL1并減少了其目標(biāo)蛋白CrkL的磷酸化。Radotinib還有效抑制了BCR-ABL1常見(jiàn)突變克隆的增殖,T315I突變除外。[1] 在A(yíng)ML細(xì)胞中,Radotinib顯著降低了細(xì)胞活性,促進(jìn)了分化,并誘導(dǎo)了CD11b表達(dá)和凋亡。在NB4、THP-1和Kasumi-1細(xì)胞中,Radotinib也誘導(dǎo)CD11b表達(dá),并降低了細(xì)胞的活性。[2]
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 : 5.3 mg/mL (10 mM)
關(guān)鍵字IY5511 | IY 5511 | Radotinib
相關(guān)產(chǎn)品Ponatinib | Pivanex | Imatinib | Bosutinib hydrate | KW-2449 | Masitinib | Nilotinib monohydrochloride monohydrate | Bosutinib | GNF-5 | Dasatinib | Imatinib Mesylate | Nilotinib
相關(guān)庫(kù)經(jīng)典已知活性庫(kù) | 抗癌活性化合物庫(kù) | 激酶抑制劑庫(kù) | FDA 上市激酶抑制劑庫(kù) | 酪氨酸激酶分子庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌藥物庫(kù)
關(guān)鍵字: 雷度替尼|||Supect|||IY-5511|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(zhuān)業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶(hù)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(mǎn)足不同需求的化合物庫(kù),以及多種類(lèi)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(lèi)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(mǎn)足客戶(hù)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(zhuān)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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