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| Targets |
Ansornitinib targets PDGFR and VEGFR2, two receptor tyrosine kinases involved in cell proliferation, migration, and angiogenesis. PDGFR signaling is critical for the activation of fibroblasts and the development of fibrosis, while VEGFR2 mediates angiogenesis. By inhibiting both kinases, Ansornitinib reduces fibrosis and pathological angiogenesis, making it a potential therapeutic agent for fibrotic diseases.
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| ln Vitro |
Ansornitinib (Compound I) (0.1 nM-10 μM, 2 h) has the ability to notably prevent the phosphorylation of KDR in human umbilical vein endothelial cells (HUVEC) and PDGFRβ in human hepatic stellate cells [1]. Compound I (ansonitinib) (0.1–13 μM, 48 hours) causes a reduction in the production of numerous markers associated with inflammation, including fibrosis, soluble interleukin-8, and macrophage colony-stimulating factor (M-CSF). N-calmodulin, α-SMA, and other related indicators exhibit dosage dependence [1].
In vitro, Ansornitinib inhibits PDGFR and VEGFR2 kinase activity. Specific IC50 values for these targets are not provided in the available sources. Its activity is characterized in kinase inhibition assays measuring the phosphorylation of substrates. |
| ln Vivo |
Ansornitinib (Compound I) (25 mg/kg, PO, twice daily, 4 weeks) decreases fibrosis in TGFβ-positive female mice [1]. Ansornitinib (Compound I) (5-45 mg/kg orally twice daily for 4 days) decreases inflammatory bowel disease (IBD) in male CD-1 mice with TNBS-induced IBD/acute colitis [1].
In vivo, Ansornitinib (5-45 mg/kg orally twice daily for 4 days) decreases inflammatory bowel disease in male CD-1 mice with TNBS-induced IBD/acute colitis. This demonstrates its in vivo efficacy in a model of intestinal inflammation and fibrosis. The compound is being studied for its potential in cancer therapy. |
| Enzyme Assay |
A cell-free assay for Ansornitinib would involve measuring its inhibition of PDGFR and VEGFR2 kinase activity. Recombinant PDGFR or VEGFR2 is incubated with a peptide substrate and ATP in the presence of varying concentrations of the compound. The incorporation of phosphate into the substrate is measured, and IC50 values are calculated. Specific IC50 values are not provided.
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| Cell Assay |
Cellular assays for Ansornitinib would typically involve assessing its effects on PDGFR and VEGFR2 signaling in cells expressing these receptors. Cells are treated with the compound, and the phosphorylation of the receptors and downstream signaling molecules is measured. The compound's ability to inhibit cell proliferation and migration can also be assessed.
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| Animal Protocol |
Animal/Disease Models: 8-10 weeks TGFβ-positive female mice [1]
Doses: 25 mg/kg Route of Administration: Oral; twice (two times) daily; 4-week Experimental Results: Pulmonary fibrosis score, lung hydroxyproline level and αSMA (early Pulmonary fibrosis markers) diminished. Animal/Disease Models: TNBS-induced IBD/acute colitis male CD-1 mice [1] Doses: 5, 15, 45 mg/kg Route of Administration: oral; Route of Administration: oral. twice (two times) daily; 4-day Experimental Results: Colonic histology improved and TNBS-induced goblet cell loss was Dramatically diminished at the 15 mg/kg and 45 mg/kg doses. 5 mg/kg and 15 mg/kg Dramatically diminished the expression level of myeloperoxidase (MPO), while 45 mg/kg had no statistical difference. Animal/Disease Models: Male Sprague Dawley rat [1] Doses: 30 mg/kg Route of Administration: intravenous (iv) (iv)injection; Experimental Results: pharmacokinetic/PK/PK parameters of ansonitinib (Compound I) Parameters Ansonitinib (Compound I) t1 /2 4.1 h Tmax 0.518 h Cmax 7860 ng/mL Clearance 173 mL/kg/min Steady-state volume 18.2 L/kg AUC0-last 3180 ng/mL*h AUC0-in In vivo animal experiments with Ansornitinib were conducted in male CD-1 mice with TNBS-induced IBD/acute colitis. The compound was administered orally at 5-45 mg/kg twice daily for 4 days. The compound decreased inflammatory bowel disease in this model. Specific outcome measures are not detailed. |
| ADME/Pharmacokinetics |
Ansornitinib is an orally bioactive compound. It has a molecular formula of C30H32N6O4 and a molecular weight of 540.61 g/mol. Specific pharmacokinetic parameters, such as half-life and bioavailability, are not provided in the available sources. It is being studied for its potential in cancer therapy.
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| Toxicity/Toxicokinetics |
Toxicity data for Ansornitinib are not provided in the available sources. As a research compound, it is intended for research use only and not for human consumption. Standard laboratory safety precautions should be observed when handling this compound.
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| References | |
| Additional Infomation |
Ansornitinib (CAS: 1448874-96-1) is an orally bioactive dual-kinase inhibitor targeting PDGFR and VEGFR2. It is also known as ANG-3070. The compound has anti-fibrotic activity and is used to study fibrotic diseases. Its molecular formula is C30H32N6O4 and its molecular weight is 540.61 g/mol. It is not an approved drug and is strictly for research purposes.
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| Molecular Formula |
C30H32N6O4
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| Molecular Weight |
540.61
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| Exact Mass |
540.248
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| CAS # |
1448874-96-1
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| Related CAS # |
1448874-96-1;2757115-29-8 (HCl);
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| PubChem CID |
136234633
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
40
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| Complexity |
895
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1C=CC=CC=1)(=C1\C(NC2=NC(C(=O)OC)=CC=C\12)=O)\NC1C=CC(N(C)C(=O)CN2CCN(C)CC2)=CC=1
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| InChi Key |
CIBINADBMIHXHZ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C30H32N6O4/c1-34-15-17-36(18-16-34)19-25(37)35(2)22-11-9-21(10-12-22)31-27(20-7-5-4-6-8-20)26-23-13-14-24(30(39)40-3)32-28(23)33-29(26)38/h4-14,38H,15-19H2,1-3H3,(H,32,33)
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| Chemical Name |
methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-pyrrolo[2,3-b]pyridine-6-carboxylate
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| Synonyms |
Ansornitinib; 1448874-96-1; Ansornitinib [INN]; LHC4W5LJH4; UNII-LHC4W5LJH4; ANG-3070; ANG3070
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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 |
| 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: ~40 mg/mL (74.0 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8498 mL | 9.2488 mL | 18.4976 mL | |
| 5 mM | 0.3700 mL | 1.8498 mL | 3.6995 mL | |
| 10 mM | 0.1850 mL | 0.9249 mL | 1.8498 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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