XL092

Chemical Information
Zanzalintinib is an orally bioavailable inhibitor of the receptor tyrosine kinases (RTKs) hepatocyte growth factor receptor (c-Met; HGFR), vascular endothelial growth factor receptor type 2 (VEGFR2), AXL and MER, with potential anti-angiogenesis and antineoplastic activities. Upon oral administration, zanzalintinib targets and binds to c-Met, VEGFR2, AXL and MER, and prevents their RTK activity. This blocks c-Met/VEGFR2/AXL/MER-mediated signal transduction pathways, and inhibits the proliferation and migration of c-Met-, VEGFR2-, AXL- and MER-overexpressing tumor cells. c-Met, overexpressed in many tumor cell types, plays a critical role in tumor formation, proliferation, invasion and metastasis, and contributes to tumor resistance. VEGFR2, overexpressed in certain tumor types, plays an essential role in angiogenesis and the proliferation, survival, migration and differentiation of endothelial cells. AXL and MER, both members of the TAM (Tyro3, Axl and Mer) family of RTKs, are overexpressed by many tumor cell types. They play key roles in tumor cell proliferation, survival, invasion, angiogenesis and metastasis, and their expression is associated with enhanced immunosuppression, drug resistance and poor prognosis.
| CAS Number | 2367004-54-2 |
| PubChem CID | 139350422 |
| IUPAC Name | 1-N'-(4-fluorophenyl)-1-N-[4-[7-methoxy-6-(methylcarbamoyl)quinolin-4-yl]oxyphenyl]cyclopropane-1,1-dicarboxamide |
| Molecular Formula | C29H25FN4O5 |
| Molecular Weight | 528.5 |
| XLogP | 4.7 |
| Topological Polar Surface Area | 119 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 8 |
| Heavy Atom Count | 39 |
| Formal Charge | 0 |
| Complexity | 885 |
| Property | Value |
|---|---|
| Molecular Weight | 528.5 |
| XLogP3 | 4.7 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 7 |
| Rotatable Bond Count | 8 |
| Exact Mass | 528.18089807 |
| Monoisotopic Mass | 528.18089807 |
| Topological Polar Surface Area | 119 Ų |
| Heavy Atom Count | 39 |
| Formal Charge | 0 |
| Complexity | 885 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Covalently-Bonded Unit Count | 1 |
| Compound Is Canonicalized | Yes |
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