| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CT52923 targets platelet-derived growth factor receptor (PDGFR), a receptor tyrosine kinase that plays critical roles in cell proliferation, migration, and survival. It functions as an ATP-competitive inhibitor with IC50 values of 100-200 nM for PDGFRs and stem cell factor receptors. By inhibiting PDGFR signaling, CT52923 blocks PDGF-induced smooth muscle cell migration and fibroblast proliferation.
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| ln Vitro |
With IC50 values of 100–200 nM, CT52923 inhibits PDGFRs and stem cell factor receptors[1]. According to an experiment for cell migration, CT52923 (0.01-30 μM; 24 h) inhibits the migration of smooth muscle cells or fibroblast ischemia caused by growth factor stimulation [1].
In vitro, CT52923 inhibits PDGFRs and stem cell factor receptors with IC50 values ranging from 100 to 200 nM. At concentrations of 0.01-30 μM for 24 hours, CT52923 effectively blocks platelet-derived growth factor-induced smooth muscle cell migration or fibroblast proliferation, with corresponding IC50 values of 64 nM and 280 nM, respectively. These activities demonstrate its potent anti-proliferative and anti-migratory effects. |
| ln Vivo |
CT52923 (cervical; 5, 15, 30 and 50 mg/kg; twice daily) significantly inhibits intimal neogenesis after carotid artery injury [1].
In vivo, CT52923 (oral; 5, 15, 30, and 50 mg/kg; twice daily) significantly inhibits neointima formation after carotid artery injury in rats. This effect is consistent with PDGFR inhibition and the compound's ability to block smooth muscle cell proliferation and migration. These in vivo data support its potential for treating vascular proliferative diseases such as atherosclerosis and restenosis. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assay for CT52923 typically involves measuring its inhibition of PDGFR kinase activity. The compound is incubated with recombinant PDGFR enzyme in the presence of ATP and a peptide substrate. Kinase activity is measured using a luminescent or fluorescence-based assay (e.g., ADP-Glo or TR-FRET) to determine IC50 values. ATP-competitive inhibition can be confirmed by varying ATP concentrations in the assay. Binding affinity to PDGFR can be assessed using surface plasmon resonance.
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| Cell Assay |
Cell Migration Assay [1]
Cell Types: Rat A10 smooth muscle cells Tested Concentrations: 0.01-30 μM Incubation Duration: 24 h Experimental Results: Inhibits cell migration induced by PDGF, IC50 is 64 nM. 64 and 280 nM[1]. The in vitro cell-based assay for CT52923 involves culturing smooth muscle cells or fibroblasts and treating them with the compound to assess effects on PDGF-induced migration or proliferation. Cells are seeded in multi-well plates, treated with CT52923 (0.01-30 μM; 24 hours), and stimulated with PDGF. Cell migration is assessed using Boyden chamber or wound healing assays. Cell proliferation is measured using MTT, BrdU, or CellTiter-Glo assays. IC50 values for migration and proliferation inhibition are calculated from dose-response curves. |
| Animal Protocol |
Animal/Disease Models: Rat carotid balloon angioplasty model [1].
Doses: 5, 15, 30 and 50 mg/kg Route of Administration: po (oral gavage); twice (two times) daily Experimental Results: Inhibition of PDGF-mediated vascular injury response. In vivo animal studies for CT52923 are conducted in rat models of carotid artery injury to assess neointima formation. Rats undergo carotid artery balloon injury, and CT52923 is administered orally at doses of 5, 15, 30, and 50 mg/kg twice daily. After a defined period (typically 14 days), carotid arteries are harvested, sectioned, and stained to measure neointima formation. The compound's ability to inhibit neointimal hyperplasia is assessed by morphometric analysis. |
| ADME/Pharmacokinetics |
CT52923 is an orally active small molecule with favorable pharmacokinetic properties. It is an ATP-competitive PDGFR antagonist with IC50 values of 100-200 nM. The compound has a molecular weight of 467.54 and a molecular formula of C23H25N5O4S. It is soluble in DMSO (60 mg/mL) and can be formulated for in vivo administration using vehicles such as 10% DMSO + 90% corn oil. Detailed PK parameters are available from preclinical studies.
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| Toxicity/Toxicokinetics |
The toxicity profile of CT52923 has been evaluated in preclinical studies. As a PDGFR inhibitor, its primary safety concerns relate to effects on platelet function, wound healing, and vascular integrity, consistent with the class effects of PDGFR inhibitors. Standard toxicology assessments would include acute and sub-chronic toxicity studies in rodents and dogs, with endpoints including clinical signs, body weight, clinical pathology, and histopathology. The compound is for research use only.
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| References | |
| Additional Infomation |
CT52923 is a research compound and has not been approved for clinical use. It is a selective, orally active antagonist of PDGFR that functions as an ATP-competitive inhibitor with IC50 values of 100-200 nM. CT52923 has versatile applications for researching pathological diseases including atherosclerosis, glomerulonephritis, liver cirrhosis, pulmonary fibrosis, and cancer. It significantly inhibits neointima formation in rat carotid artery injury models.
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| Molecular Formula |
C23H25N5O4S
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|---|---|
| Molecular Weight |
467.54070353508
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| Exact Mass |
467.16
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| Elemental Analysis |
C, 59.09; H, 5.39; N, 14.98; O, 13.69; S, 6.86
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| CAS # |
205256-55-9
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| PubChem CID |
9890746
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| Appearance |
White to off-white to be determined
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| LogP |
2.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
33
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| Complexity |
667
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C=C2C(=C1)C(=NC=N2)N3CCN(CC3)C(=S)NCC4=CC5=C(C=C4)OCO5)OC
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| InChi Key |
ORRFUYVNMZSYIC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H25N5O4S/c1-29-19-10-16-17(11-20(19)30-2)25-13-26-22(16)27-5-7-28(8-6-27)23(33)24-12-15-3-4-18-21(9-15)32-14-31-18/h3-4,9-11,13H,5-8,12,14H2,1-2H3,(H,24,33)
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| Chemical Name |
N-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carbothioamide
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| Synonyms |
CT52923; CT-52923; CT 52923; KN734; KN-734; KN 734;
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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 : ~50 mg/mL (~106.94 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.35 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1389 mL | 10.6943 mL | 21.3885 mL | |
| 5 mM | 0.4278 mL | 2.1389 mL | 4.2777 mL | |
| 10 mM | 0.2139 mL | 1.0694 mL | 2.1389 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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