| Identification | Back Directory | [Name]
CCT251545 | [CAS]
1661839-45-7 | [Synonyms]
CS-2537
CCT251545
LM-3773,CCT251545
CCT-251545;CCT 251545
8-(3-chloro-5-(4-(1-methyl-1H-pyrazol-4-yl)phenyl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one
8-[3-Chloro-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]-4-pyridinyl]-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]- | [Molecular Formula]
C23H24ClN5O | [MDL Number]
MFCD29472582 | [MOL File]
1661839-45-7.mol | [Molecular Weight]
421.92 |
| Chemical Properties | Back Directory | [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) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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. | [in vivo]
CCT251545 (70mg/kg; p.o.; twice daily) causes an inhibition of tumor growth in NCr athymic mice bearing established SW620 human colorectal cancer xenografts[2].
| Animal Model: | 6-8 weeks female NCr athymic mice bearing established SW620 xenografts[2] | | Dosage: | 70mg/kg | | Administration: | Oral administration; twice daily; from days 0-7 and days 10-14 | | Result: | Caused an inhibition of tumor growth with a 70% reduction in final tumor weight relative to control. |
| [storage]
Store at -20°C | [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. |
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| Company Name: |
Spectrum Chemical Manufacturing Corp.
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| Telephone: |
021-021-021-67601398-809-809-809 15221380277 |
| Website: |
www.spectrumchemical.com/oa_html/index.jsp?minisite=10020&respid=22372&language=us |
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