XL092

XL092 is a multi-kinase inhibitor. It selectively inhibits the receptor tyrosine kinases (RTKs) MET, VEGFR2, Axl, and Mer (IC50s = 3, 15, 5.8, and 0.6 nM, respectively) over serine/threonine kinases for which it has no activity, but does inhibit 28 other RTKs with IC50 values ranging from 3 to 54 nM, as well as additional kinases by greater than 70% at 1 µM. XL092 inhibits the proliferation of SNU-5 human gastric carcinoma cells (IC50 = 98.9 nM), which highly express MET, and human umbilical vein endothelial cells (HUVECs, IC50 = 10.4 nM). It reduces tumor volume and intratumoral MET phosphorylation in NCI H441 human lung cancer and SNU-5 mouse xenograft models when administered at doses of 3 and 10 mg/kg. XL092 (30 mg/kg) increases the number of peripheral B cells and CD4+ T cells, and decreases the number of peripheral myeloid cells, in an MC-38 syngeneic mouse model of colon carcinoma, indicating a conversion to an immune-permissive tumor microenvironment.Formal Name: N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-1,1-cyclopropanedicarboxamide. CAS Number: 2367004-54-2. Synonyms: Zanzalintinib. Molecular Formula: C29H25FN4O5. Formula Weight: 528.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: O=C(C1=CC2=C(OC3=CC=C(NC(C4(CC4)C(NC5=CC=C(C=C5)F)=O)=O)C=C3)C=CN=C2C=C1OC)NC. InChi Code: 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). InChi Key: JSPCKALGNNVYOO-UHFFFAOYSA-N.