| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| A408044-1ml |
1ml |
现货  |
|
| 别名 | 甲磺酸阿帕替尼 (YN968D1) |
|---|---|
| 英文别名 | Rivoceranib mesylate | N-[4-(1-cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide |
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | Apatinib (YN968D1) mesylate |
| 生化机理 | 甲磺酸阿帕替尼（YN968D1，Rivoceranib）是一种强效的血管内皮生长因子信号通路抑制剂，对血管内皮生长因子受体-2、Ret（c-Ret）、c-Kit 和 c-Src 的 IC50 值分别为 1 nM、13 nM、429 nM 和 530 nM。甲磺酸阿帕替尼可诱导自噬和细胞凋亡。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 血管内皮生长因子受体 2 抑制剂 |
| 产品介绍 |
Apatinib(YN-968D1) is an orally bioavailable, selective VEGFR2 inhibitor with IC50 of 1 nM. Information Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis Apatinib (YN968D1) is a novel, orally bioavailable, selective inhibitor with potential antiangiogenic and antineoplastic activities. Apatinib selectively binds to and inhibits VEGFR2. Apatinib 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. Apatinib inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ. Apatinib significantly inhibits proliferation stimulated by 20 ng/mL VEGF (IC50 = 0.17μM). Apatinib effectively inhibits proliferation, migration and tube formation of human umbilical vein endothelial cells induced by FBS, and blocked the budding of rat aortic ring. Apatinib 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. Apatinib 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, apatinib significantly inhibited the photoaffinity labeling of both ABCB1 and ABCG2 with [125I]iodoarylazidoprazosin in a concentration-dependent manner. In vivo Apatinib inhibits the growth of a broad range of human tumor xenografts in a significant dose-dependent manner. Apatinib reverses ABCB1-mediated MDR in the nude mouse xenograft model. Apatinib significantly enhances the antitumor activity of doxorubicin in nude mice bearing K562/ADR xenografts. cell lines：A375 cells Concentrations：~25 μM Incubation Time：72 h Powder Purity:≥99% |
| IC50 | VEGFR2, IC50: 1 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| 分子量 | 493.58 |
| 溶解性 | Solubility (25°C) In vitro DMSO: Insoluble; Water: Insoluble; Ethanol: Insoluble; |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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