| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T409225-1ml |
1ml |
现货  |
|
| 别名 | 替沃扎尼（AV-951） |
|---|---|
| 英文别名 | KRN-951 | 1-(2-chloro-4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-3-(5-methylisoxazol-3-yl)urea |
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Tivozanib (AV-951) |
| 生化机理 | Tivozanib（AV-951，KRN-951）是一种强效的选择性血管内皮生长因子受体（VEGFR）抑制剂，对 VEGFR1/2/3 的 IC50 为 30 nM/6.5 nM/15 nM，还能抑制 PDGFR 和 c-Kit，对 FGFR-1、Flt3、c-Met、EGFR 和 IGF-1R 的活性较低。第 3 阶段 |
| 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抑制剂 |
| 产品介绍 |
Tivozanib (AV-951)是VEGFR抑制剂，对VEGFR1，2和3的IC50分别为30 nM，6.5 nM和15 nM，还能抑制PDGFR和c-Kit，对FGFR-1，Flt3，c-Met，EGFR和IGF-1R的抑制性较低。 Information Tivozanib (AV-951, KRN-951) is a potent and selectiveVEGFRinhibitor forVEGFR1/2/3with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3. AV-951 is a novel quinoline-urea derivative. AV-951 blocks VEGF-dependent activation of mitogen-activated protein kinases and proliferation of endothelial cells. In vivo In vivo studies show that AV-951 also decreases the micro vessel density and suppresses VEGFR2 phosphorylation levels in tumor xenografts, especially at a concentration of 1mg/kg (p.o. administration). AV-951 shows almost complete inhibition of tumor xenografts growth (TGI>85%) in athymic rats. Another study in rat peritoneal disseminated tumor model shows that AV-951 could prolong the survival of the tumor-bearing rats with the MST of 53.5 days. AV-951 displays antitumor activity against many human tumor xenografts including lung, breast, colon, ovarian, pancreas and prostate cancer. cell lines： Concentrations：1 μM Incubation Time：15 minutes Powder Purity:≥95% |
| IC50 | VEGFR1, IC50: 30 nM |
|---|
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | COC1=CC2=C(C=C1OC)C(=CC=N2)OC3=CC=C(NC(=O)NC4=NOC(=C4)C)C(=C3)Cl |
| 分子量 | 454.86 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 50 mg/mL (198.23 mM); Water: 17 mg/mL (67.4 mM); Ethanol: Insoluble; |
|---|
| Concentration(Compounding value) | 9.0-11.0(mmol/L) |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
| Record the entire process by video | Conform |
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