MedKoo Cat#: 555990 | Name: XL092
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

XL092
XL092
CAS#2367004-54-2

Theoretical Analysis

MedKoo Cat#: 555990

Name: XL092

CAS#: 2367004-54-2

Chemical Formula: C29H25FN4O5

Exact Mass: 528.1809

Molecular Weight: 528.54

Elemental Analysis: C, 65.90; H, 4.77; F, 3.59; N, 10.60; O, 15.14

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,850.00 Ready to ship
1g USD 4,250.00 Ready to ship
2g USD 7,650.00 Ready to ship
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Related CAS #
No Data
Synonym
JUN04542; JUN-04542; JUN 04542; XL092; XL-092; X L092; Zanzalintinib
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
More Info
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.
Biological target:
XL092 is a potent inhibitor of the activity of Axl, Mer and C-Met kinase.
In vitro activity:
TBD
In vivo activity:
TBD

Preparing Stock Solutions

The following data is based on the product molecular weight 528.54 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.

Recalculate based on batch purity %
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
Formulation protocol:
TBD
In vitro protocol:
TBD
In vivo protocol:
TBD
1: Yu J, Park R, Tojjari A, Sadeghipour A, Saeed A, Saeed A. Zanzalintinib (XL092): a next-generation tyrosine kinase inhibitor-comprehensive review of early safety & efficacy data. Expert Opin Investig Drugs. 2024 Sep;33(9):887-895. doi: 10.1080/13543784.2024.2388571. Epub 2024 Aug 7. PMID: 39099411. 2: Saeed A, Tabernero J, Parikh A, Van den Eynde M, Karthaus M, Gerlinger M, Wang Z, Wang G, Smith R, Hecht JR. STELLAR-303: randomized phase III study of zanzalintinib + atezolizumab in previously treated metastatic colorectal cancer. Future Oncol. 2024;20(24):1733-1743. doi: 10.1080/14796694.2024.2352276. Epub 2024 Jul 23. PMID: 39041200; PMCID: PMC11485978.