WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H556162
CAS#: 205256-55-9
Description: CT52923, also known as KN734, is a platelet-derived growth factor receptor (PDGFR) inhibitor. CT52923 exhibited remarkable specificity when tested against other kinases, including all members of the closely related PDGFR family. The PDGFRs and stem cell factor receptor were inhibited with an IC(50) of 100 to 200 nM, while 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 also demonstrated specificity for inhibition of cellular responses.
Hodoodo Cat#: H556162
Name: CT52923
CAS#: 205256-55-9
Chemical Formula: C23H25N5O4S
Exact Mass: 467.1627
Molecular Weight: 467.544
Elemental Analysis: C, 59.09; H, 5.39; N, 14.98; O, 13.69; S, 6.86
Synonym: CT52923; CT-52923; CT 52923; KN734; KN-734; KN 734;
IUPAC/Chemical Name: N-(benzo[d][1,3]dioxol-5-ylmethyl)-4-(6,7-dimethoxyquinazolin-4-yl)piperazine-1-carbothioamide
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)
SMILES Code: S=C(N1CCN(CC1)C2=C3C=C(OC)C(OC)=CC3=NC=N2)NCC4=CC=C5OCOC5=C4
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 467.544 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
1: Ma D, Nutt CL, Shanehsaz P, Peng X, Louis DN, Kaetzel DM. Autocrine platelet- derived growth factor-dependent gene expression in glioblastoma cells is mediated largely by activation of the transcription factor sterol regulatory element binding protein and is associated with altered genotype and patient survival in human brain tumors. Cancer Res. 2005 Jul 1;65(13):5523-34. doi: 10.1158/0008-5472.CAN-04-2582. PMID: 15994924.
2: Kozaki K, Kaminski WE, Tang J, Hollenbach S, Lindahl P, Sullivan C, Yu JC, Abe K, Martin PJ, Ross R, Betsholtz C, Giese NA, Raines EW. Blockade of platelet-derived growth factor or its receptors transiently delays but does not prevent fibrous cap formation in ApoE null mice. Am J Pathol. 2002 Oct;161(4):1395-407. doi: 10.1016/S0002-9440(10)64415-X. PMID: 12368212; PMCID: PMC1867295.
3: Matsuno K, Nakajima T, Ichimura M, Giese NA, Yu JC, Lokker NA, Ushiki J, Ide S, Oda S, Nomoto Y. Potent and selective inhibitors of PDGF receptor phosphorylation. 2. Synthesis, structure activity relationship, improvement of aqueous solubility, and biological effects of 4-[4-(N-substituted (thio)carbamoyl)-1-piperazinyl]-6,7-dimethoxyquinazoline derivatives. J Med Chem. 2002 Sep 26;45(20):4513-23. doi: 10.1021/jm0201114. PMID: 12238930.
4: Lokker NA, Sullivan CM, Hollenbach SJ, Israel MA, Giese NA. Platelet-derived growth factor (PDGF) autocrine signaling regulates survival and mitogenic pathways in glioblastoma cells: evidence that the novel PDGF-C and PDGF-D ligands may play a role in the development of brain tumors. Cancer Res. 2002 Jul 1;62(13):3729-35. PMID: 12097282.
5: Yu JC, Lokker NA, Hollenbach S, Apatira M, Li J, Betz A, Sedlock D, Oda S, Nomoto Y, Matsuno K, Ide S, Tsukuda E, Giese NA. 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. PMID: 11504817.
