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5mg |
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10mg |
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25mg |
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50mg |
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Chiauranib (CS-2164) is a novel, oral and potent inhibitor of multiple tyrosine and serine-threonine kinases with anticancer activity. Chiauranib simultaneously inhibits the angiogenesis-related kinases (VEGFR2, VEGFR1, VEGFR3, PDGFRa and c-Kit), mitosis-related kinase Aurora B and chronic inflammationrelated kinase CSF-1R in a high potency manner with the IC50 at a single-digit nanomolar range. In particular, Chiauranib showed very high selectivity in the kinase inhibition profile with little activity on off-target non-receptor kinases, proteins, GPCR and ion channels, indicative of a better drug safety profile in terms of clinical relevance.
ln Vitro |
Chiauranib (CS2164; 3 μM; 24 hours) induces G2/M cell cycle arrest and inhibits cell proliferation in tumor tissues by inhibiting Aurora B-mediated H3 phosphorylation [1]. In HUVEC and PDGFRβ phosphorylation in PDGFRβ-overexpressing NIH3T3 cells, Chiauranib (CS2164; 0.03-3 μM) inhibits VEGFR/PDGFR phosphorylation, inhibits ligand-dependent cell proliferation and capillary formation, and prevents vasculature formation. Displays anti-angiogenic activity in tumor tissues [1]. .Chiauranib (CS2164) inhibits CSF-1R phosphorylation, thereby inhibiting ligand-stimulated monocyte differentiation into macrophages and reducing CSF-1R+ cells in tumor tissue [1].
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ln Vivo |
In various human tumor xenograft models, chiauranib (CS2164; 0.5–40 mg/kg; oral; once daily; for 33 or 43 days) therapy induced considerable regression or total tumor development at well-tolerated oral doses. In vivo, chiauranib demonstrates extensive and strong anticancer activity [1].
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Cell Assay |
Cell cycle analysis [1]
Cell Types: Molt-4 Cell Tested Concentrations: 3 μM Incubation Duration: 24 hrs (hours) Experimental Results: 3 μM induced cell cycle to obviously arrest in the G2/M phase. Western Blot Analysis[1] Cell Types: Molt-4 Cells Tested Concentrations: 1.5 μM, 3 μM, 6 μM Incubation Duration: 24 hrs (hours) Experimental Results: p-H3 levels were Dramatically diminished in Molt-4 cells in a concentration-dependent fashion. |
Animal Protocol |
Animal/Disease Models: Female BALB/c athymic (nu+/nu+) mice (6 weeks old) [1]
Doses: 2.5 mg/kg, 5 mg /kg, 10 mg/kg, 20 mg/kg, 40 mg/kg Dosing: Oral; one time/day; for 33 days or 43 days Experimental Results: Induced significant regression or complete suppression in several human tumor xenograft models Tumor growth. |
References | |
Additional Infomation |
Chiauranib is under investigation in clinical trial NCT03974243 (Chiauranib in Combination With Chidamide in Patients With Relapsed/refractory Non-hodgkin's Lymphoma).
Ibcasertib is an orally available, small molecule inhibitor of select serine-threonine kinases, including aurora kinase B (aurora B), vascular endothelial growth factor receptors (VEGFRs), stem cell factor receptor (c-KIT), and platelet-derived growth factor receptors (PDGFRs), with potential antineoplastic activity. Upon oral administration, ibcasertib binds to and inhibits the activity of aurora B, VEGFRs, c-kit and PDGFRs, which may result in a decrease in the proliferation of tumor cells that overexpress these kinases. These kinases are overexpressed by a variety of cancer cell types. |
Molecular Formula |
C27H21N3O3
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Molecular Weight |
435.483
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Exact Mass |
435.158
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CAS # |
1256349-48-0
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PubChem CID |
49779393
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Appearance |
White to light brown solid powder
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Density |
1.333±0.06 g/cm3(Predicted)
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Boiling Point |
604.6±50.0 °C(Predicted)
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LogP |
5.1
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Hydrogen Bond Donor Count |
2
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Hydrogen Bond Acceptor Count |
5
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Rotatable Bond Count |
5
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Heavy Atom Count |
33
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Complexity |
661
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Defined Atom Stereocenter Count |
0
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InChi Key |
BRKWREZNORONDU-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C27H21N3O3/c1-32-18-9-12-22-25(16-18)29-14-13-26(22)33-19-10-11-20-17(15-19)5-4-6-21(20)27(31)30-24-8-3-2-7-23(24)28/h2-16H,28H2,1H3,(H,30,31)
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Chemical Name |
N-(2-aminophenyl)-6-(7-methoxyquinolin-4-yl)oxynaphthalene-1-carboxamide
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Synonyms |
CS-2164 CS2164 Chiauranib
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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 : ~62.5 mg/mL (~143.52 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.78 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2963 mL | 11.4816 mL | 22.9632 mL | |
5 mM | 0.4593 mL | 2.2963 mL | 4.5926 mL | |
10 mM | 0.2296 mL | 1.1482 mL | 2.2963 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.