ChemicalBook > CAS DataBase List > 8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-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)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one

Product 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 No.
1607837-31-9
Chemical Name
8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one
Synonyms
CCT-251921;LM-3860,CCT251921;CCT-251921;CCT 251921;CCT-251921, 10 mM in DMSO;CCT-251921,Cyclin dependent kinase,Inhibitor,CDK,CCT251921,CCT 251921,inhibit;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]-
CBNumber
CB43133466
Molecular Formula
C21H23ClN6O
Formula Weight
410.9
MOL File
1607837-31-9.mol
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8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one Property

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)
pka
15.81±0.20(Predicted)
form 
Solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

ChemScene
Product number
CS-5521
Product name
CCT-251921
Purity
99.77%
Packaging
1mg
Price
$108
Updated
2021/12/16
ChemScene
Product number
CS-5521
Product name
CCT-251921
Purity
99.77%
Packaging
10mg
Price
$420
Updated
2021/12/16
ChemScene
Product number
CS-5521
Product name
CCT-251921
Purity
99.77%
Packaging
25mg
Price
$840
Updated
2021/12/16
ChemScene
Product number
CS-5521
Product name
CCT-251921
Purity
99.77%
Packaging
50mg
Price
$1140
Updated
2021/12/16
Crysdot
Product number
CD00008621
Product name
CCT251921
Purity
97%
Packaging
50mg
Price
$1496
Updated
2021/12/16
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8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one Chemical Properties,Usage,Production

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

8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one Preparation Products And Raw materials

Raw materials

Preparation Products

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8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one Suppliers

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1607837-31-9, 8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-oneRelated Search:


  • 8-(2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)pyridin-4-yl)-2,8-diazaspiro[4.5]decan-1-one
  • CCT-251921
  • LM-3860,CCT251921
  • 8-[2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)-4-pyridinyl]-2,8-Diazaspiro[4.5]decan-1-one
  • 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
  • 2,8-Diazaspiro[4.5]decan-1-one, 8-[2-amino-3-chloro-5-(1-methyl-1H-indazol-5-yl)-4-pyridinyl]-
  • CCT-251921,Cyclin dependent kinase,Inhibitor,CDK,CCT251921,CCT 251921,inhibit
  • CCT-251921, 10 mM in DMSO
  • 1607837-31-9