WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 555990
Description: XL092 is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values in cell-based assays of 15, 1.6, 3.4, and 7.2 nM respectively. In xenograft studies, XL092 caused substantial tumor growth inhibition following 10 mg/kg daily oral dosing for 14 days. XL092 has good oral bioavailability and a significantly shorter half-life than cabozantinib.
MedKoo Cat#: 555990
Chemical Formula: C29H25FN4O5
Exact Mass: 528.1809
Molecular Weight: 528.5404
Elemental Analysis: C, 65.90; H, 4.77; F, 3.59; N, 10.60; O, 15.14
Synonym: JUN04542; JUN-04542; JUN 04542; XL092; XL-092; X L092;
IUPAC/Chemical Name: 1,1-Cyclopropanedicarboxamide, N-(4-fluorophenyl)-N'-[4-[[7-methoxy-6-[(methylamino)carbonyl]-4-quinolinyl]oxy]phenyl]-
InChi Key: JSPCKALGNNVYOO-UHFFFAOYSA-N
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)
SMILES Code: O=C(C1(C(NC2=CC=C(OC3=CC=NC4=CC(OC)=C(C(NC)=O)C=C34)C=C2)=O)CC1)NC5=CC=C(F)C=C5
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 528.5404 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
XL092 retains the target inhibition profile of the clinically active drug cabozantinib, simultaneously targeting MET, VEGFR2, AXL and MER. In preclinical studies XL092 showed potent pharmacodynamic inhibition of MET and VEGFR2 phosphorylation, which was associated with significant anti-tumor activity. PK data from the Phase 1 trial of XL092 shows a significantly shorter terminal half-life compared to cabozantinib, consistent with the desired profile.