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| 品牌 | absin | CAS | 252916-29-3 |
|---|---|---|---|
| 分子式 | C18H18N2O3 | 纯度 | ＞98% |
| 分子量 | 310.35 | 货号 | abs810477 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | has greatest potency against PDGFR auto | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
TSU-68 252916-29-3
| 产品描述 | |
| 描述 | TSU-68 has greatest potency against PDGFR autophosphorylation with Ki of 8 nM, but also strongly inhibits Flk-1 and FGFR1 trans-phosphorylation, little activity against IGF-1R, Met, Src, Lck, Zap70, Abl and CDK2; does not inhibit EGFR. |
| 纯度 | >98% |
| 储存/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 | |
| 别名 | Orantinib；SU6668；SU 6668 |
| 外观 | red to orange Powder |
| 可溶性/溶解性 | DMSO : ≥ 28 mg/mL (90.22 mM) |
| 生物活性 | |
| 靶点 | PDGFRβ；FGFR1；Flt-1 |
| In vitro(体外研究) | Orantinib (SU6668; 0.03-10 μM) shows inhibitory activity against tyrosine phosphorylation of KDR in VEGF stimulated HUVECs, and also blocks PDGF-stimulated PDGFRβ tyrosine phosphorylation in NIH-3T3 cells overexpressing PDGFRβ. Orantinib (≥10 μM) inhibits acidic FGF-induced phosphorylation of the FGFR1 substrate 2. However, Orantinib (up to 100 μM) has no effect on EGF-stimulated EGFR tyrosine phosphorylation in NIH-3T3 cells overexpressing EGFR. Furthermore, Orantinib inhibits VEGF-driven and FGF-driven mitogenesis of HUVECs with mean IC50 of 0.34 μM and 9.6 μM, respectively. In human myeloid leukemia MO7E cells, Orantinib (SU6668) inhibits the tyrosine autophosphorylation of stem cell factor (SCF) receptor, c-kit, with IC50 of 0.1-1 μM, as well as ERK1/2 phosphorylation. In addition, Orantinib suppresses SCF-induced proliferation of MO7E cells with an IC50 of 0.29 μM, and induces apoptosis. |
| In vivo(体内研究) | Orantinib (SU6668; 75-200 mg/kg) causes tumor growth inhibition on several tumor types in xenograft models in athymic mice, such as A375, Colo205, H460, Calu-6, C6, SF763T, and SKOV3TP5 cells. Orantinib (75 mg/kg) also inhibits tumor angiogenesis of C6 glioma xenografts. In a tumor model of HT29 human colon carcinoma, Orantinib (200 mg/kg) decreases the average vessel permeability and average fractional plasma volume in the tumor rim and core. Orantinib enhances abnormal stromal development at the periphery of carcinomas[3]. Moreover, Orantinib (TSU-68; 200 mg/kg) augments the effect of chemotherapeutic infusion in a rabbit VX2 liver tumor model. |
| 研究领域 | |
| 研究领域 | NeuroscienceDevelopment NeuroscienceNeurology processNeurogenesis Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases MicrobiologyOrganismVirusRNA VirusssRNA positive strand virusSARS Coronavirus Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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