For research use only. Not for therapeutic Use.
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[1][2].
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[1].
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[2].
| Catalog Number | I038431 |
| CAS Number | 2367004-54-2 |
| Synonyms | 1-N’-(4-fluorophenyl)-1-N-[4-[7-methoxy-6-(methylcarbamoyl)quinolin-4-yl]oxyphenyl]cyclopropane-1,1-dicarboxamide |
| Molecular Formula | C29H25FN4O5 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H25FN4O5/c1-31-26(35)22-15-21-23(16-25(22)38-2)32-14-11-24(21)39-20-9-7-19(8-10-20)34-28(37)29(12-13-29)27(36)33-18-5-3-17(30)4-6-18/h3-11,14-16H,12-13H2,1-2H3,(H,31,35)(H,33,36)(H,34,37) |
| InChIKey | JSPCKALGNNVYOO-UHFFFAOYSA-N |
| SMILES | CNC(=O)C1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F |
| Reference | [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. |
