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)

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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: 10mg
Price: $515
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 STAT1^SER727 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