普納替尼|T2372|TargetMol

價(jià)格	￥669	￥1900	￥2683
包裝	10mg	50mg	100mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-09-23

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產(chǎn)品詳情

中文名稱:普納替尼	英文名稱:Ponatinib
CAS:943319-70-8	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: 99.74%	產(chǎn)品類別: 抑制劑
貨號(hào): T2372

Product Introduction

Bioactivity

名稱	Ponatinib
描述	Ponatinib (AP24534) is a multi-targeted kinase inhibitor with oral activity that inhibits Abl, PDGFRα, VEGFR2, FGFR1, and Src (IC50=0.37/1.1/1.5/2.2/5.4 nM). Ponatinib has antitumor activity for the treatment of chronic granulocytic leukemia in adults. leukemia.
細(xì)胞實(shí)驗(yàn)	Ba/F3 cell lines were distributed in 96-well plates (4 × 10^3 cells/well) and incubated with escalating concentrations of AP24534 for 72 hr. The inhibitor ranges used were: 0–625 nM for cells expressing BCR-ABL and 0–10,000 nM for BCR-ABL negative cells. Proliferation was measured using an MTS-based viability assay. IC50 values are reported as the mean of three independent experiments performed in quadruplicate. For cell proliferation experiments with CML or normal primary cells, mononuclear cells were plated in 96-well plates (5 × 10^4 cells/well) over graded concentrations of AP24534 (0–1000 nM) in RPMI supplemented with 10% FBS, L-glutamine, penicillin/streptomycin, and 100 μM β-mercaptoethanol. Following a 72 hr incubation, cell viability was assessed by subjecting cells to an MTS assay. All values were normalized to the control wells with no drug [1].
激酶實(shí)驗(yàn)	AP24534 was profiled against >100 kinases by Reaction Biology Corporation using the Kinase Hotspot assay, which utilizes 10 μM [33P]-ATP, recombinant kinase domain, peptide substrate, and a range of 10 concentrations of inhibitor to establish an IC50 value [1].
動(dòng)物實(shí)驗(yàn)	Briefly, tumor xenografts were established by the subcutaneous implantation of MV4-11 cells (1 × 10^7 in 50% Matrigel) into the right flank of female CB.17 severe combined immunodeficient mice and dosing was initiated when the average tumor volume reached approximately 200 mm^3. Ponatinib was formulated in aqueous 25 mmol/L citrate buffer (pH = 2.75) and mice were dosed orally once daily for 4 weeks. The tumors were measured in 2 dimensions (length and width) with a caliper in millimeters. Tumor volume (mm3) was calculated with the following formula: tumor volume = (length × width^2)/2. Tumor growth inhibition (TGI) was calculated as follows: TGI = (1 ? ΔT/ΔC) × 100, where ΔT stands for mean tumor volume change of each treatment group and ΔC for mean tumor volume change of control group. The tumor volume data were collected and analyzed with a 1-way ANOVA test to determine the overall difference among groups. Each ponatinib treatment group was further compared to the vehicle control group for statistical significance using Dunnett's Multiple Comparison Test. A P-value less than 0.05 was considered to be statistically significant and a P-value less than 0.01 to be highly statistically significant [3].
體外活性	方法：親本 Ba/F3 細(xì)胞和表達(dá)天然或突變 BCR-ABL Ba/F3 細(xì)胞的用 Ponatinib (0-10000 nM) 處理 72 h，使用 MTS assay 檢測(cè)細(xì)胞活力。結(jié)果：Ponatinib 有效地抑制表達(dá)天然 BCR-ABL 的 Ba/F3 細(xì)胞的增殖 (IC50=0.5 nM)。所有測(cè)試的 BCR-ABL 突變體對(duì) Ponatinib 保持敏感 (IC50=0.5-36 nM)，包括 BCR-ABLT315I (IC50=11 nM)。親本 Ba/F3 細(xì)胞的生長(zhǎng)僅在顯著更高的 IC50 (1713 nM) 下受到抑制，表明對(duì) BCR-ABL 陽性細(xì)胞的抑制具有顯著的差異選擇性。[1] 方法：AML 細(xì)胞系 MV4-11、Kasumi-1、KG1 和 EOL1 用 Ponatinib (0.03-100 nmol/L) 處理 1 h，使用 Western Blot 檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：Ponatinib 以劑量依賴的方式抑制所有 4 種 RTK (FLT3、KIT、FGFR1 和 PDGFRα) 的磷酸化，IC50 值在 0.3-20 nmol/L 之間。[2]
體內(nèi)活性	方法：為測(cè)試體內(nèi)抗腫瘤活性，將 Ponatinib (2.5-50 mg/kg in 0.5% CMC) 灌胃給藥給注射 Ba/F3: BCR-ABLT315I 細(xì)胞的 SCID 小鼠，每天一次，持續(xù)十九天。結(jié)果：Ponatinib 的治療以劑量依賴的方式抑制腫瘤生長(zhǎng)，延長(zhǎng)了生存期。[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 : 26.6 mg/mL (50 mM) DMSO : 16.67 mg/mL (31.3 mM) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 5.33 mg/mL (10.01 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.
關(guān)鍵字	Src \| Ponatinib \| Platelet-derived growth factor receptor \| Bcr-Abl \| orally \| inhibit \| multi-targeted \| VEGFR2 \| Fibroblast growth factor receptor \| Abl \| VEGFR \| active \| PDGFR \| AP 24534 \| FGFR \| Inhibitor \| AP-24534 \| PDGFRα \| kinase \| FGFR1 \| Autophagy \| Vascular endothelial growth factor receptor
相關(guān)產(chǎn)品	Guanidine hydrochloride \| Hydroxychloroquine \| Ferulic Acid
相關(guān)庫	抗癌上市藥物庫 \| 抗癌活性化合物庫 \| EMA 上市藥物庫 \| 抗衰老化合物庫 \| 膜蛋白靶向化合物庫 \| 藥物功能重定位化合物庫 \| FDA 上市激酶抑制劑庫 \| 抗癌臨床化合物庫

關(guān)鍵字：普納替尼|||帕納替尼|||AP24534|TargetMol

公司簡(jiǎn)介

上海陶術(shù)生物科技有限公司為美國(guó)Target Molecule Corp. ( Target Mol ) 在上海建立的全資子公司。我們與美國(guó)波士頓、德國(guó)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(guó)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
主營(yíng)行業(yè)	化學(xué)試劑,生物活性小分子	經(jīng)營(yíng)模式	貿(mào)易,試劑,定制,服務(wù)

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VIP 12年

公司成立：12年
注冊(cè)資本：566.2651萬人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫，天然產(chǎn)物，活性分子化合物等
公司地址：上海市閘北區(qū)江場(chǎng)三路28號(hào)4樓

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