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| | CCT251545 Basic information |
| Product Name: | CCT251545 | | Synonyms: | CCT251545;8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one;LM-3773,CCT251545;8-(3-chloro-5-(4-(1-methyl-1H-pyrazol-4-yl)phenyl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one;2,8-Diazaspiro[4.5]decan-1-one, 8-[3-chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl]-;CCT-251545;CCT 251545;CS-2537;inhibit,Wnt,CCT251545,Inhibitor,CCT-251545,CCT 251545 | | CAS: | 1661839-45-7 | | MF: | C23H24ClN5O | | MW: | 421.92 | | EINECS: | | | Product Categories: | | | Mol File: | 1661839-45-7.mol |  |
| | CCT251545 Chemical Properties |
| Boiling point | 709.7±60.0 °C(Predicted) | | density | 1.37±0.1 g/cm3(Predicted) | | storage temp. | Inert atmosphere,Store in freezer, under -20°C | | solubility | ≥42.2 mg/mL in DMSO; insoluble in H2O; ≥2.33 mg/mL in EtOH with ultrasonic | | form | solid | | pka | 15.81±0.20(Predicted) |
| | CCT251545 Usage And Synthesis |
| Description | CCT251545 is an orally bioavailable inhibitor of Wnt signaling (IC50 = 5 nM). It is a potent and selective inhibitor of the human mediator complex-associated protein kinases Cdk8 and Cdk19. Through its effects on Cdk8 and Cdk19, CCT251545 alters Wnt pathway-regulated gene expression. It reduces tumor growth in COLO 205 human colon cancer xenografts after oral dosing (70 mg/kg bid) and in Wnt-dependent tumors. | | Uses | CCT251545 is a potent inhibitor of WNT signaling with good oral pharmacokinetics. | | Definition | ChEBI: CCT251545 is a chloropyridine that is 3-chloropyridine substituted by a 1-oxo-2,8-diazaspiro[4.5]decan-8-yl group and a 4-(1-methyl-1H-pyrazol-4-yl)phenyl group at positions 4 and 5, respectively. It is an orally bioavailable inhibitor of Wnt signaling (IC50 = 5 nM) and a potent and selective chemical probe for cyclin-dependent kinases CDK8 and CDK19. It has a role as a Wnt signalling inhibitor, an antineoplastic agent and an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor. It is a chloropyridine, a member of pyrazoles and an azaspiro compound. | | references | [1]. mallinger a, crumpler s, pichowicz m, et al. discovery of potent, orally bioavailable, small-molecule inhibitors of wnt signaling from a cell-based pathway screen. j med chem, 2015, 58(4): 1717-1735.
[2]. dale t, clarke pa, esdar c, et al. a selective chemical probe for exploring the role of cdk8 and cdk19 in human disease. nat chem biol, 2015, 11(12): 973-980. |
| | CCT251545 Preparation Products And Raw materials |
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