奎扎替尼|T2066|TargetMol

價(jià)格	￥297	￥727	￥1080
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-02

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產(chǎn)品詳情

中文名稱:奎扎替尼	英文名稱:Quizartinib
CAS:950769-58-1	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: 99.42%	產(chǎn)品類別: 抑制劑
貨號(hào): T2066

Product Introduction

Bioactivity

名稱	Quizartinib
描述	Quizartinib (AC220) is a second-generation type II FLT3 tyrosine kinase inhibitor that is orally active and highly selective, inhibiting the autophosphorylation of FLT3-WT and FLT3-ITD (IC50=4.1/1.1 nM). Quizartinib induces apoptosis in tumor cells.
細(xì)胞實(shí)驗(yàn)	MV4-11 and RS4;11 cells were cultured in Iscove media with 10% fetal bovine serum (FBS) and RPMI complete with 10% FBS, respectively. For proliferation assays, cells were cultured overnight in low serum media (0.5% FBS), then seeded in a 96-well plate at 40 000 cells per well. Inhibitors were added to the cells and incubated at 37°C for 72 hours. Cell viability was measured using the Cell Titer-Blue Cell Viability Assay. To measure inhibition of FLT3 autophosphorylation, cells were cultured in low serum media (0.5% FBS) overnight and seeded at a density of 400 000 cells per well in a 96-well plate the following day. The cells were incubated with inhibitors for 2 hours at 37°C. To induce FLT3 autophosphorylation in RS4;11 cells, 100 ng/mL FLT3 ligand was added for 15 minutes after the 2-hour compound incubation. Cell lysates were prepared and incubated in 96-well plates pre-coated with a total FLT3 capture antibody. The coated plates were incubated with either a biotinylated antibody against FLT3 to detect total FLT3 or an antibody against phosphotyrosines to detect FLT3 autophosphorylation. In both cases, a SULFO-tagged streptavidin secondary antibody was used for electrochemiluminescence detection on the Meso Scale Discovery platform [1].
激酶實(shí)驗(yàn)	KinomeScan kinase binding assays were performed as previously described. For the FLT3 assay, we used a kinase construct that spanned the catalytic domain only (amino acids 592 to 969 in NP_004110.2). This construct does not include the juxtamembrane domain and is designed to measure the intrinsic binding affinity of the open FLT3 active site for inhibitors [1].
動(dòng)物實(shí)驗(yàn)	The model was performed according to published procedures.20 For intravenous bone marrow engraftment, nonobese diabetic/severe combined immunodeficient mice were acclimated for 2 weeks before pretreatment with 150 mg/kg cyclophosphamide delivered intraperitoneally once a day for 2 days. After a 48-hour rest period, animals were given an intravenous injection of 5 × 10^6 MV4-11 cells into the tail vein. AC220 was formulated and delivered as described for pharmacokinetic studies [1].
體外活性	方法：人白血病細(xì)胞系 MV4-11 和人惡性黑色素瘤細(xì)胞系 A375 用 Quizartinib 處理 72 h，使用 Cell Titer-Blue Cell Viability Assay 檢測(cè)細(xì)胞活力。結(jié)果：Quizartinib 抑制 MV4-11 細(xì)胞生長(zhǎng)，IC50 為 0.56 ?nM。Quizartinib 不影響 A375 細(xì)胞的增殖，IC50 大于 10000 nM。[1] 方法：AML 細(xì)胞系 MV4-11 用 Quizartinib (0.0625-8 nM) 處理 2 h，使用 Western Blot 檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：Quizartinib 對(duì) MV4-11 細(xì)胞中的 FLT3 信號(hào)通路具有濃度依賴性抑制活性。Quizartinib 有效抑制 FLT3 磷酸化 (IC50=0.50 nM)。Quizartinib 抑制下游分子 SHP-2、STAT5、MEK1/2、ERK1/2 和 AKT的磷酸化。[2]
體內(nèi)活性	方法：為檢測(cè)體內(nèi)抗腫瘤活性，將 Quizartinib (10 mg/kg，22% hydroxypropyl-β-cyclodextrin, CEP-701 was formulated in 20% gelucire 44/14 in water (vol/vol)) 口服給藥給攜帶 MV4-11 異種移植物的 NU/NU 小鼠，每天一次，持續(xù) 28 天。結(jié)果：用 10 mg/kg 的 Quizartinib 治療導(dǎo)致所有動(dòng)物的腫瘤快速完全消退，并且在治療后 60 天的觀察期內(nèi)沒(méi)有觀察到腫瘤再生。[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	DMSO : 16.67 mg/mL (29.73 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.32 mg/mL (5.92 mM), Suspension. 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	AC-220 \| Inhibitor \| myeloid \| FLT3-ITD \| Apoptosis \| oral \| Autophagy \| Fms like tyrosine kinase 3 \| Target Protein-binding Moiety \| mutation \| inhibit \| Quizartinib \| CD135 \| AML \| leukemia \| Ligands for Target Protein for PROTAC \| acute \| AC 220 \| Cluster of differentiation antigen 135 \| FLT3 \| selective
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相關(guān)庫(kù)	抗癌上市藥物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 已知活性化合物庫(kù) \| EMA 上市藥物庫(kù) \| 抗衰老化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字：奎扎替尼|||AC220|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(guò)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(guò)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(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)	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)

TargetMol中國(guó)（陶術(shù)生物）

VIP 12年

公司成立：12年
注冊(cè)資本：566.2651萬(wàn)人民幣
企業(yè)類型：有限責(zé)任公司(自然人投資或控股)
主營(yíng)產(chǎn)品：小分子抑制劑，藥物篩選化合物庫(kù)，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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