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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
Chiauranib targets multiple kinases including VEGFR, PDGFR, c-Kit, and other receptor tyrosine kinases involved in angiogenesis and tumor growth. By inhibiting these kinases, chiauranib blocks angiogenesis (formation of new blood vessels) and directly inhibits tumor cell proliferation. The compound's multi-targeted mechanism of action may provide advantages over single-target inhibitors by addressing multiple pathways involved in cancer progression.
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| 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].
In vitro, chiauranib demonstrates potent inhibitory activity against multiple kinases including VEGFR, PDGFR, and c-Kit. It inhibits angiogenesis in endothelial cell assays and shows antiproliferative activity against various cancer cell lines. Specific IC₅₀ values for kinase inhibition and cell growth inhibition are documented in the literature. The compound shows activity against a broad range of cancer cell types. |
| 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].
In vivo, chiauranib has been studied in animal models of cancer, showing significant antitumor activity. It inhibits tumor growth in various xenograft models through inhibition of angiogenesis and direct antiproliferative effects. The compound has been evaluated in clinical trials for the treatment of non-small cell lung cancer, ovarian cancer, and other solid tumors. Clinical studies have demonstrated promising efficacy and acceptable safety profiles. |
| Enzyme Assay |
Kinase inhibition assays are performed using purified kinase enzymes and ATP. Kinase activity is measured by phosphorylation of peptide substrates using radiolabeled ATP or fluorescence-based detection. Chiauranib is tested at various concentrations, and IC₅₀ values are calculated for each target kinase. Selectivity profiling is performed against a panel of kinases to assess off-target activity. Binding affinity is determined using surface plasmon resonance or other biophysical methods.
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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. In vitro cellular assays use various cancer cell lines and endothelial cells. Cells are treated with chiauranib at various concentrations. Antiproliferative activity is measured by MTT assay. Anti-angiogenic activity is assessed using endothelial cell tube formation assays and migration assays. Apoptosis is evaluated by Annexin V staining or caspase activity assays. Signaling pathway inhibition is assessed by Western blot analysis of phospho-kinase targets. The compound is dissolved in DMSO for stock solutions. |
| 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. In vivo efficacy is evaluated in murine xenograft models using various cancer cell lines. Chiauranib is administered orally or intraperitoneally. Tumor growth is monitored by caliper measurements. Endpoints include tumor volume, tumor weight, survival, and histopathological analysis. Angiogenesis is assessed by CD31 staining or other vascular markers. Pharmacokinetic studies are conducted to determine plasma concentrations and tissue distribution. Clinical trials have been conducted to evaluate safety and efficacy in patients. |
| ADME/Pharmacokinetics |
Chiauranib is a multi-targeted kinase inhibitor. Specific chemical properties including molecular weight, molecular formula, and CAS number are documented in the literature. The compound is typically stored at -20°C and protected from light. It is soluble in DMSO and other organic solvents. Specific pharmacokinetic parameters are documented in the literature from clinical studies. It is metabolized in the liver and excreted primarily in urine and feces.
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| Toxicity/Toxicokinetics |
Specific toxicity data for chiauranib are documented in preclinical and clinical studies. Common adverse effects may include hypertension, proteinuria, fatigue, gastrointestinal disturbances, and hematological effects. These are consistent with the known effects of VEGFR inhibitors. The compound should be used with caution in patients with cardiovascular disease or bleeding risk. Monitoring of blood pressure, renal function, and hematological parameters is recommended during therapy.
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| References | |
| Additional Infomation |
Chiauranib is being investigated in the clinical trial NCT03974243 (Chiauranib in combination with Chidamide for the treatment of patients with relapsed/refractory non-Hodgkin's lymphoma). Ibcasertib is an oral small molecule inhibitor that inhibits multiple serine/threonine kinases, including Aurora B, vascular endothelial growth factor receptor (VEGFR), c-kit, and platelet-derived growth factor receptor (PDGFR), exhibiting potential antitumor activity. After oral administration, ibcasertib binds to and inhibits the activity of Aurora B, VEGFR, c-kit, and PDGFR, potentially leading to reduced proliferation of tumor cells overexpressing these kinases. Overexpression of these kinases is observed in various cancer cell types.
Chiauranib is a novel multi-targeted anticancer agent that inhibits angiogenesis and tumor cell proliferation through inhibition of VEGFR, PDGFR, c-Kit, and other kinases. It has been studied in clinical trials for the treatment of various cancers including non-small cell lung cancer, ovarian cancer, and other solid tumors. The compound's multi-targeted mechanism of action may provide advantages over single-target inhibitors. It represents a promising approach to cancer therapy through simultaneous inhibition of angiogenesis and tumor cell proliferation. |
| 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.
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