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| 品牌 | absin | CAS | 1218779-75-9 |
|---|---|---|---|
| 分子式 | C25H27N5O4S | 纯度 | 99% |
| 分子量 | 493.58 | 货号 | abs814025 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is an orally bioavailable | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
YN968D1 1218779-75-9
| 产品描述 | |
| 描述 | Apatini (YN968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM. |
| 纯度 | 99% |
| 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 | YN968D1 |
| 外观 | Powder |
| 可溶性/溶解性 | DMSO：22 mg/mL (44.57 mM) |
| 生物活性 | |
| 靶点 | VEGFR2 ,RET |
| In vitro(体外研究) | Apatini (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatini selectively binds to and inhibits VEGFR2. Apatini can also potently suppress the activities of Ret, c-kit and c-src with IC50 of 0.013 μM, 0.429 μM and 0.53 μM, respectively. Apatini inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatini significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17μM). Apatini effectively inhibits proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. Apatini reverses ABCB1- and ABCG2-mediated MDR by inhibiting their transport function, but not by blocking the AKT or ERK1/2 pathway or downregulating ABCB1 or ABCG2 expression. Apatini significantly potentiates the cytotoxicity of established ABCB1 and ABCG2 substrates and increased the accumulation of DOX and Rho 123 in ABCB1- or ABCG2-overexpressing cells. Furthermore, apatini significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with iodoarylazidoprazosin in a concentration-dependent manner. |
| In vivo(体内研究) | Apatini inhibits the growth of a broad range of human tumor xenografts in a significant dose-dependent manner. Apatini reverses ABCB1-mediated MDR in the nude mouse xenograft model. Apatini significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts. |
| 参考文献 | |
| 参考文献 | 1] Tian S, et al. Cancer Sci, 2011, 102(7), 1374-1380. [2] Mi YJ, et al. Cancer Res, 2010, 70(20), 7981-7991. [3] Tong XZ, et al. Biochem Pharmacol, 2012, 83(5), 586-597. |
| 研究领域 | |
| 研究领域 | Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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