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簡(jiǎn)要描述：Ponatinib 943319-70-8Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively.
產(chǎn)品型號(hào)：abs47028015廠商性質(zhì)：生產(chǎn)廠家更新時(shí)間：2026-01-13訪 問(wèn) 量：655產(chǎn)品分類
Product Category詳細(xì)介紹
| 品牌 | absin | CAS | 943319-70-8 |
|---|---|---|---|
| 分子式 | C29H27F3N6O | 純度 | 98% |
| 分子量 | 532.56 | 貨號(hào) | abs47028015 |
| 規(guī)格 | 10mg | 供貨周期 | 現(xiàn)貨 |
| 主要用途 | is a novel, potent multi-target inhibit | 應(yīng)用領(lǐng)域 | 化工,生物產(chǎn)業(yè),農(nóng)林牧漁,制藥/生物制藥,綜合 |
Ponatinib 943319-70-8
| 產(chǎn)品描述 | |
| 描述 | Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM, respectively. |
| 純度 | 98% |
| 儲(chǔ)存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 別名 | 普納替尼；帕納替尼; AP24534 |
| 外觀 | Yellow powder |
| 可溶性/溶解性 | DMSO : 16.67 mg/mL (31.3 mM) Ethanol : 26.6 mg/mL (50 mM) |
| 生物活性 | |
| 靶點(diǎn) | Abl ,PDGFRα ,VEGFR2 ,FGFR1 ,c-Src |
| In vitro(體外研究) | AP24534 potently inhibits native Abl, AblT315I, and other clinically important Abl kinase domain mutants with IC50 of 0.30 nM–2 nM. AP24534 doesn't inhibit Aurora kinase family members, nor does it inhibit insulin receptor or CDK2/cyclin E. AP24534 inhibits proliferation of Ba/F3 cells expressing Bcr-Abl with IC50 of 0.5 nM, as well as Ba/F3 cells expressing a range of Bcr-Abl mutants with IC50 of 0.5 nM–36 nM. The inhibition of proliferation by AP24534 is correlated with induction of apoptosis. In leukemic cell lines containing activated forms of FLT3, KIT, FGFR1, and PDGFRα receptors, AP24534 potently inhibits receptor phosphorylation and cellular proliferation with IC50 of 0.3 nM to 20 nM. In MV4-11 (FLT3-ITD(+/+)) but not RS4;11 (FLT3-ITD(–/–)) AML cells, AP24534 inhibits FLT3 signaling and induced apoptosis at less than 10 nM. AP24534 inhibits viability of primary leukemic blasts from a FLT3-ITD positive AML patient with IC50 of 4 nM but not those from patients with AML expressing native FLT3. In Ba/F3 cells engineered to express activated FGFR1-4, AP24534 potently inhibits FGFR-mediated signaling and viability with IC50 lower than 40 nM. In cell lines representing multiple tumor types (endometrial, bladder, gastric, breast, lung, and colon), and containing FGFRs dysregulated by a variety of mechanisms, AP24534 inhibits FGFR-mediated signaling with IC50 less than 40 nM and inhibits cell growth with IC50 of 7 nM–181 nM. |
| In vivo(體內(nèi)研究) | In a mouse xenograft model of Ba/F3 cells expressing native Bcr-Abl, AP24534 (2.5 mg/kg and 5 mg/kg) prolongs mice median survival. In the xenograft model of Ba/F3 Bcr-AblT315I, AP24534 (10 mg/kg–50 mg/kg) significantly suppresses tumor growth. AP24534 (30 mg/kg) decreases the phosphorylated Bcr-Abl and phosphorylated CrkL levels in the tumors. |
| 研究領(lǐng)域 | |
| 研究領(lǐng)域 | CancerCancer MetabolismResponse to hypoxia CancerOncoproteins/suppressorsOncoproteinsGrowth factor receptors CardiovascularAngiogenesisEndothelial Cell Markers CardiovascularCardiovascular MarkersCell MarkersEndothelial Cells MetabolismTypes of diseaseCancer MetabolismPathways and ProcessesMetabolism processesHypoxia MicrobiologyInterspecies InteractionHost Virus Interaction NeuroscienceDevelopment NeuroscienceProcesses Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases Stem CellsEndothelial ProgenitorsEndothelial Markers Stem CellsHematopoietic ProgenitorsSurface Molecules Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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