CT52923

Alias: CT52923; CT-52923; CT 52923; KN734; KN-734; KN 734;
Cat No.:V56768 Purity: ≥98%
CT52923, also known as KN734, is a platelet-derived growth factor receptor (PDGFR) inhibitor.
CT52923 Chemical Structure CAS No.: 205256-55-9
Product category: Others 11
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
Other Sizes
Official Supplier of:
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Product Description
CT52923, also known as KN734, is a platelet-derived growth factor receptor (PDGFR) inhibitor. CT52923 showed significant specificity when tested against other kinases such as all members of the closely related PDGFR family. PDGFR and stem cell factor receptor blocker/inhibitory IC(50) ranged from 100 to 200 nM, whereas 45- to >200-fold higher concentrations of CT52923 were required to inhibit fms-like tyrosine kinase 3 and colony-stimulating factor. 1 receptor respectively. In addition, CT52923 showed specificity in inhibiting cellular responses.
Biological Activity I Assay Protocols (From Reference)
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].
ln Vivo
CT52923 (cervical; 5, 15, 30 and 50 mg/kg; twice daily) significantly inhibits intimal neogenesis after carotid artery injury [1].
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].
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.
References
[1]. J C Yu, et al. Efficacy of the novel selective platelet-derived growth factor receptor antagonist CT52923 on cellular proliferation, migration, and suppression of neointima following vascular injury. J Pharmacol Exp Ther. 2001 Sep;298(3):1172-8.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C23H25N5O4S
Molecular Weight
467.544
Exact Mass
467.16
Elemental Analysis
C, 59.09; H, 5.39; N, 14.98; O, 13.69; S, 6.86
CAS #
205256-55-9
SMILES
S=C(N1CCN(CC1)C2=C3C=C(OC)C(OC)=CC3=NC=N2)NCC4=CC=C5OCOC5=C4
InChi Key
ORRFUYVNMZSYIC-UHFFFAOYSA-N
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)
Chemical Name
N-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carbothioamide
Synonyms
CT52923; CT-52923; CT 52923; KN734; KN-734; KN 734;
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~50 mg/mL (~106.94 mM)
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.

Calculator

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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