| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| ln Vivo |
Significant inhibition of tumor growth was observed in xenograft studies with zanzolintinib (10 mg/kg/day; sidewall) administered for 14 days. P-MET and PEGFR2 are 82% and 96%, respectively, inhibited by zuzanilintinib [1]. T1/2 for zanzolintinib (Compound 8; 3 mg/kg; IV) was 5.4 hours, and CL was 43 mL/hr·kg. T1/2 of 7.1 hours, Cmax were deposited by zanzolintinib (3 mg/kg; lateral).
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|---|---|
| Animal Protocol |
Animal/Disease Models: Rat [1]
Doses: 3 mg/kg (pharmacokinetic/PK/PK analysis) Route of Administration: IV Experimental Results: T1/2 is 5.4 hrs (hrs (hours)), CL is 43 mL/hr·kg. is 11.4 μM[2]. |
| References | |
| Additional Infomation |
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.
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| Molecular Formula |
C29H25FN4O5
|
|---|---|
| Molecular Weight |
528.5310
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| Exact Mass |
528.18
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| Elemental Analysis |
C, 65.90; H, 4.77; F, 3.59; N, 10.60; O, 15.14
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| CAS # |
2367004-54-2
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| Related CAS # |
2367004-54-2
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| PubChem CID |
139350422
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| Appearance |
Off-white to light brown solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
39
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| Complexity |
885
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JSPCKALGNNVYOO-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
1-N'-(4-fluorophenyl)-1-N-[4-[7-methoxy-6-(methylcarbamoyl)quinolin-4-yl]oxyphenyl]cyclopropane-1,1-dicarboxamide
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| Synonyms |
XL-092; XL092; X L092; JUN-04542; JUN04542; JUN 04542
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 16.7~100 mg/mL (31.5~189.2 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.73 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (3.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8920 mL | 9.4602 mL | 18.9204 mL | |
| 5 mM | 0.3784 mL | 1.8920 mL | 3.7841 mL | |
| 10 mM | 0.1892 mL | 0.9460 mL | 1.8920 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03845166 | Active Recruiting |
Drug: XL092 Drug: Atezolizumab |
Neoplasm Malignant Renal Cell Carcinoma |
Exelixis | March 20, 2019 | Phase 1 |
| NCT05678673 | Recruiting | Drug: XL092 Drug: Nivolumab |
Non-Clear Cell Renal Cell Carcinoma |
Exelixis | January 1, 2023 | Phase 3 |
| NCT05425940 | Recruiting | Drug: XL092 Drug: Atezolizumab |
Colorectal Cancer | Exelixis | September 7, 2022 | Phase 3 |
| NCT05176483 | Recruiting | Drug: XL092 Drug: Nivolumab |
Renal Cell Carcinoma Solid Tumor |
Exelixis | December 14, 2021 | Phase 1 |
| NCT06082167 | Not yet recruiting | Drug: Zanzalintinib Biological: Pembrolizumab |
Head and Neck Squamous Cell Carcinoma |
Exelixis | November 2023 | Phase 2 Phase 3 |
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