| 产品描述： | Zanzalintinib (XL092) is an orally active, ATP-competitive inhibitor of multiple receptor tyrosine kinases (RTKs) including MET, VEGFR2, AXL and MER, with IC50s in cell-based assays of 15 nM, 1.6 nM, 3.4 nM, 7.2 nM respectively. Zanzalintinib exhibits anti-tumor activity. Zanzalintinib has the potential for kinase-dependent diseases and conditions research |
| 靶点： |
VEGFR2:1.6 nM (IC50);AXL:3.4 nM (IC50);MER:7.2 nM (IC50) |
| 体内研究： |
Zanzalintinib (10 mg/kg/day; oral; for 14 days) causes substantial tumor growth inhibition in xenograft studies. Zanzalintinib shows 82% and 96% inhibition on p-MET and p-VEGFR2, respectively. Zanzalintinib (compound 8; 3 mg/kg; iv) has a T1/2 of 5.4 hours, a CL of 43 mL/hr?kg. Zanzalintinib (3 mg/kg; po) has a T1/2 of 7.1 hours and a Cmax of 11.4 μM for rats. Animal Model: Rat Dosage: 3 mg/kg (Pharmacokinetic Analysis) Administration: IV Result: Had a T1/2 of 5.4 hours, a CL of 43 mL/hr•kg. |
| 参考文献： |
1. J. Hsu, et al. XL092, a multi-targeted inhibitor of MET, VEGFR2, AXL and MER with an optimized pharmacokinetic profile. European Journal of Cancer, Volume 138, Supplement 2, October 2020, Page S16. 2. Lynne Canne Bannen, et al. Compounds for the treatment of kinase-dependent disorders. WO2019148044A1. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
-80℃（运输条件：冰袋低温运输） |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
1.892 ml |
9.46 ml |
18.92 ml |
| 5 mM |
0.378 ml |
1.892 ml |
3.784 ml |
| 10 mM |
0.189 ml |
0.946 ml |
1.892 ml |
| 50 mM |
0.038 ml |
0.189 ml |
0.378 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京