吉列替尼|T4409|TargetMol

價(jià)格	￥358	￥519	￥828
包裝	1mg	2mg	5mg

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:吉列替尼	英文名稱:Gilteritinib
CAS:1254053-43-4	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): T4409

Product Introduction

Bioactivity

名稱	Gilteritinib
描述	Gilteritinib (ASP2215) is a FLT3 inhibitor (IC50=0.29 nM) and an AXL inhibitor (IC50=0.73 nM) with ATP-competitive, selective, and oral activity. Gilteritinib exhibits antitumor activity and can be used to treat FLT3 mutation-positive AML.
細(xì)胞實(shí)驗(yàn)	Gilteritinib is dissolved in DMSO and stored, and then diluted with appropriate media before use.The effect of Gilteritinib on MV4-11 and MOLM-13 cells is assessed using the CellTiter-Glo Luminescent Cell Viability Assay. Subsequent studies are conducted to examine the effect of Gilteritinib and Quizartinib on Ba/F3 cells expressing either FLT3-ITD, FLT3-D835Y, FLT3-ITD-D835Y, FLT3-ITD-F691 L, or FLT3-ITD-F691I. MV4-11 and MOLM-13 cells are treated with DMSO or increasing concentrations of Gilteritinib (0.01, 0.1, 1, 10, and 100 nM) for 5 days, and cell viability is measured using CellTiter-Glo
激酶實(shí)驗(yàn)	The kinase inhibitory activity of Gilteritinib is tested against a panel of 78 tested kinases using ATP concentrations that are approximately equal to the Km value for each kinase in a TK-ELISA or off-chip mobility shift assay. Initially, two concentrations of Gilteritinib (1 nM and 5 nM) are tested to assess each compound's inhibitory effect on TK activity. Further studies are then conducted using a dose range of Gilteritinib to determine IC50 values for kinases in which activity is inhibited by >50% with 1 nM Gilteritinib as well as for c-KIT. TK-ELISA and MSA assays are used to conduct IC50 studies for FLT3, LTK, AXL, and c-KIT; the HTRF KinEASE-TK assay is performed to assess the IC50 value of echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK)
動(dòng)物實(shí)驗(yàn)	MiceAntitumor activity is evaluated in nude mice transplanted with MV4-11 AML cells. The pharmacokinetics in xenografted mice is also investigated. MV4-11 xenografted-mice are treated with oral administration of Gilteritinib at 10 mg/kg for 4 days. Treatment of Gilteritinib for 28 days results in dose-dependent inhibition of MV4-11 tumor growth and induces complete tumor regression at more than 6 mg/kg
體外活性	方法：人急性髓細(xì)胞白血病細(xì)胞 MV4-11 和 MOLM-13 用 Gilteritinib (0.01-100 nM) 處理 5 天，使用 CellTiter-Glo 檢測(cè)細(xì)胞增殖。結(jié)果：Gilteritinib 抑制 MV4-11 和 MOLM-13 細(xì)胞的生長(zhǎng)，平均 IC50 值分別為 0.92 nM 和 2.9 nM。[1] 方法：人急性髓細(xì)胞白血病細(xì)胞 Molm14 用 Gilteritinib (5-20 nM) 處理 1-24 h，使用 Western Blot 檢測(cè)靶點(diǎn)蛋白表達(dá)水平。結(jié)果：當(dāng)與 Molm14 細(xì)胞孵育 1 h 時(shí)，Gilteritinib 有效地抑制了 FLT3 及其下游信號(hào)通路的活性。但是到 24? h，盡管 FLT3 持續(xù)受到抑制，但 ERK 信號(hào)傳導(dǎo)反彈，如 pERK 上調(diào)。[2]
體內(nèi)活性	方法：為測(cè)試體內(nèi)抗腫瘤活性，將 Gilteritinib (1-10 mg/kg) 口服給藥給攜帶人急性髓細(xì)胞白血病腫瘤 MV4-11 的 Nude 小鼠，每天一次，持續(xù)二十八天。結(jié)果：在 1 mg/kg/天 (63%)和 3 mg/kg/天 (80%) 劑量下觀察到 MV4-11 腫瘤的顯著生長(zhǎng)抑制。并且在 6 mg/kg/天 (93%) 和 10 mg/kg/天 (100%) 劑量下觀察到腫瘤幾乎完全消退。[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 : 1 mg/mL Ethanol : 4 mg/mL (7.2 mM) H2O : Insoluble 10% DMSO+90% Saline : 0.2 mg/mL (0.36 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	FLT3 \| TAM Receptor \| CD135 \| Axl \| inhibit \| Gilteritinib \| Mer \| ASP-2215 \| Tyro3 \| Fms like tyrosine kinase 3 \| Cluster of differentiation antigen 135 \| ASP 2215 \| Inhibitor
相關(guān)產(chǎn)品	Sorafenib
相關(guān)庫(kù)	抑制劑庫(kù) \| 經(jīng)典已知活性庫(kù) \| 激酶抑制劑庫(kù) \| FDA 上市藥物庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字：吉列替尼|||ASP2215|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)

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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