| Identification | Back Directory | [Name]
8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one | [CAS]
1607837-31-9 | [Synonyms]
CCT-251921
LM-3860,CCT251921
CCT-251921;CCT 251921
8-[2-amino-3-chloro-5-(1-methylindazol-5-yl)pyridin-4-yl]-2,8-diazaspiro[4.5]decan-1-one
8-[2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)-4-pyridinyl]-2,8-Diazaspiro[4.5]decan-1-one
8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one
2,8-Diazaspiro[4.5]decan-1-one, 8-[2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)-4-pyridinyl]- | [Molecular Formula]
C21H23ClN6O | [MDL Number]
MFCD30502895 | [MOL File]
1607837-31-9.mol | [Molecular Weight]
410.9 |
| Chemical Properties | Back Directory | [Boiling point ]
696.4±55.0 °C(Predicted) | [density ]
1.51±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 28 mg/mL (68.14 mM) | [form ]
Solid | [pka]
15.81±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
CCT251921 is a potent, selective, and orally bioavailable small-molecule modulators of the mediator complex-associated kinases CDK8 and CDK19. (IC50 data: CDK8:=2.3 nM; CDK19 = 2.6 nM). CCT251921 showed the optimal compromise of in vitro biochemical, pharmacokinetic, and physicochemical properties and is suitable for progression to animal models of cancer. The Mediator complex-associated cyclin-dependent kinase CDK8 has been implicated in human disease, particularly in colorectal cancer where it has been reported as a putative oncogene. | [Uses]
CCT-251921 is a potent, selective, and orally bioavailable CDK8 inhibitor with an IC50 of 2.3 nM. | [in vivo]
CCT-251921 shows improved oral pharmacokinetics and pharmaceutical properties in order to facilitate further evaluation of CDK8/19 pharmacology and progression into preclinical efficacy and safety studies. In APC-mutant SW620 human colorectal carcinoma xenograft model, CCT-251921 treatment reduces mice tumor weight (54.2%) at day 15. The inhibition of STAT1SER727 phosphorylation is maintained for more than 6 h after the last dose[1]. | [IC 50]
CDK8: 2.3 nM (IC50); CDK19: 2.6 nM (IC50) | [References]
[1] Mallinger A, et al. Discovery of Potent, Selective, and Orally Bioavailable Small-Molecule Modulators of the Mediator Complex-Associated Kinases CDK8 and CDK19. J Med Chem. 2016 Feb 11;59(3):1078-101. DOI:10.1021/acs.jmedchem.5b01685 |
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| Company Name: |
BOC Sciences
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| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
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