索凡替尼|T4075|TargetMol

價(jià)格	￥479	￥1090	￥1730
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:索凡替尼	英文名稱:Sulfatinib
CAS:1308672-74-3	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: 98.93%	產(chǎn)品類別: 抑制劑
貨號(hào): T4075

Product Introduction

Bioactivity

名稱	Sulfatinib
描述	Sulfatinib (KDR-IN-1) (HMPL-012) is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC 50 s ranging from 1 to 24 nM.
細(xì)胞實(shí)驗(yàn)	A CHO cellline stably transfected with hEGR cDNA and expressing hERG channels is used for the study.Whole-cell recording are performed using a 700B. Test compound is prepared as a 10 mM DMSO stock solution in a glass vial and is diluted using External Solution, the dilution is prepared no longer than 30 minutes before use. After achieving whole-cell configuration, the cells are monitored for 90 seconds to assess stability and washed with external solution for 66 sec. External solution containing 0.1% DMSO (vehicle) is applied to the cells to establish the baseline. After allowing the current to stabilize for 3 min, the test compound is applied. The test solution is added in 4 steps and the cells are kept in the test solution until the compound is effect reached a steady state or for a maximum of 6 min. Subsequently, the positive control (10 nM cisapride) is added. Washout with external solution is performed until the recovery of the current reached a steady state[1].
激酶實(shí)驗(yàn)	The KDR kinase inhibition activity is tested using the the Z-lyte assay kit. Tyr1 peptide is used to test the KDR kinase inhibitory activity of N-(2-(dimethylamino)-ethyl)-1-(3-((4-((2-methyl-1H-indol-5-yl)oxy)pyrimidin-2-yl)amino)phenyl)methanesulfonamide. The testing system contains 300ng/ml of recombinant human KDR catalytic domain, 10 μM of ATP, 1 μM of substrate peptide, and a test compound at a series of different concentrations in 384-well plate; total volume is 10 μL. The enzyme inhibition proceeds at room temperature (25°C), for 1 hour at room temperature on the shaker. 5ul of stop solution is added to stop the reaction. The KDR Kinase inhibition activity of a test compound is calculated based on the method recommended by the manufacturer. The IC50 values of the KDR kinase inhibition activity are calculated using XLfit software[1].
動(dòng)物實(shí)驗(yàn)	The phamacokinetics of the test componds are studied with male ICR mice (n=6 for each group, weight 20-30 g) after a single intraveneous and oral dosing at 2.5 and 10 mg/kg, respectively. For i.v. dosing formulation, the test compound is dissolved in DMSO (0.25%)-solutol(10%)-ethanol(10%)-physiological saline(79.75%) at the concentration of 0.25 mg/mL. And the p.o. Dosing formulation (1 mg/mL) is prepared with 0.5% CMC-Na. After i.v. Or p.o. Dosing, blood samples are collected via the ophthalmic vein at 0 (pre-close), 5, 15, 30 min and 1, 1.5, 2, 4, 8, 24 h, anti-coagulated with heparin-Na. After centrifugation, plasma samples are seprated and protein precipitated with acetonitrilel containing internal standard.\
體外活性	Sulfatinib抑制VEGFR1、2和3、FGFR1及CSF1R激酶，其IC 50值在1至24 nM范圍內(nèi)。Sulfatinib在HEK293KDR細(xì)胞中顯著阻斷由VEGF誘導(dǎo)的VEGFR2磷酸化，以及在RAW264.7細(xì)胞中由CSF1刺激的CSF1R磷酸化，其IC 50分別為2和79 nM。同時(shí)，Sulfatinib能夠減弱VEGF或FGF刺激的HUVEC細(xì)胞增殖，IC 50< 50 nM [1]。此外，它也是一種hERG抑制劑，在CHO細(xì)胞中的IC 50為6.8 μM [2]。
體內(nèi)活性	通過(guò)單次口服給藥，Sulfatinib 在動(dòng)物研究中依賴于暴露量抑制裸鼠肺組織中 VEGF 刺激的 VEGFR2 磷酸化。此外，在服藥后 24 小時(shí)，血漿中 FGF23 水平的提高表明抑制了 FGFR 信號(hào)傳導(dǎo)。Sulfatinib 在多個(gè)人源異種移植模型中展現(xiàn)出強(qiáng)大的腫瘤生長(zhǎng)抑制能力，并顯著降低 CD31 表達(dá)，表明通過(guò) VEGFR 和 FGFR 信號(hào)傳導(dǎo)強(qiáng)烈抑制血管生成。在同源小鼠結(jié)腸癌模型 CT-26 中，Sulfatinib 經(jīng)單藥治療展現(xiàn)出適度的腫瘤生長(zhǎng)抑制 [1]?？诜o藥 10 mg/kg 后，在小鼠體內(nèi)的 AUC 和 C max 分別為 397 ng/mL 和 138ng/mL [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 : 55 mg/mL (114.45 mM)
關(guān)鍵字	Sulfatinib
相關(guān)產(chǎn)品	Neratinib \| Amlexanox \| Ribociclib \| Formononetin \| Axitinib \| Lenvatinib mesylate \| Ferulic Acid \| Regorafenib \| Pazopanib \| Nintedanib \| Sorafenib \| Regorafenib monohydrate
相關(guān)庫(kù)	抑制劑庫(kù) \| 抗癌活性化合物庫(kù) \| 經(jīng)典已知活性庫(kù) \| 激酶抑制劑庫(kù) \| 膜蛋白靶向化合物庫(kù) \| 酪氨酸激酶分子庫(kù) \| 抗癌臨床化合物庫(kù) \| 抗癌藥物庫(kù)

關(guān)鍵字：索凡替尼|||KDR-IN-1|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(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多種滿足不同需求的化合物庫(kù)，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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