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.

Physicochemical Properties

Molecular Formula	C23H25N5O4S
Molecular Weight	467.54070353508
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
PubChem CID	9890746
Appearance	White to off-white to be determined
LogP	2.9
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	8
Rotatable Bond Count	5
Heavy Atom Count	33
Complexity	667
Defined Atom Stereocenter Count	0
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;
HS Tariff Code	2934.99.9001
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)

Biological Activity

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]. 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.

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.