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ChemicalBook >> CAS DataBase List >>8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one

8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one

8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one Structure
8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one structure
CAS No.
2613307-67-6
Chemical Name:
8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one
Synonyms
CDK8-IN-12;CDK8-IN-12, 10 mM in DMSO;8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one
CBNumber:
CB913461570
Molecular Formula:
C21H20ClN3O2
Molecular Weight:
381.86
MDL Number:
MOL File:
2613307-67-6.mol
Last updated:2025-04-18 09:53:00
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8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one Properties

Boiling point 631.4±55.0 °C(Predicted)
Density 1.39±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)
form Solid
pka 15.81±0.20(Predicted)
color Off-white to light yellow

8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one Chemical Properties,Uses,Production

Uses

CDK8-IN-12 is an orally active, potent CDK8 inhibitor with a Ki of 14 nM. CDK8-IN-12 has off-target kinase inhibition on GSK-3α, GSK-3β, PCK-θ with Kis of 13 nM, 4 nM, 109 nM, respectively. CDK8-IN-12 shows potent anti-proliferative effects selectively on MV4-11 cell. CDK8-IN-12 is an anti-cancer agent[1].

in vivo

CDK8-IN-12 (compound 38; IV; 5 mg/kg for rat and 2 mg/kg for mouse) has a T1/2 of 0.9 hours and 0.34 hours for rat and mouse, respectively[1].
Pharmacokinetic Parameters of CDK8-IN-12 [1].

IV (Rat 5 mg/kg)PO (Rat 20 mg/kg)IV (Mouse 2 mg/kg)PO (Mouse 10 mg/kg)
Tmax (h)0.042.750.040.42
Cmax (μM)14.42.773.445.01
AUC0-24 (μM?h)9.714.61.392.30
T1/2 (ng/mL)0.92.240.341.11
CL (L/h?kg)1.393.78
Vss (L/kg)1.111.99
F (%)3833

IC 50

CDK8: 14 nM (Ki); GSK-3α: 13 nM (Ki); GSK-3β: 4 nM (Ki); PKCθ: 109 nM (Ki)

References

[1] Mingfeng Yu, et al. Potent and orally bioavailable CDK8 inhibitors: Design, synthesis, structure-activity relationship analysis and biological evaluation. Eur J Med Chem. 2021 Mar 15;214:113248. DOI:10.1016/j.ejmech.2021.113248

8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one Preparation Products And Raw materials

Raw materials

Preparation Products

8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one Suppliers

Global( 8)Suppliers
Supplier Tel Email Country ProdList Advantage
Shanghai Beckham Medical Technology Co., Ltd 021-13816613772 13816613772 huahero21@sina.com China 998 55
Tianjin Kailiqi Biotechnology Co., Ltd. 15076683720 klq@cw-bio.com China 6439 55
Shanghai Chaolan Chemical Technology Center 021-QQ：65489617 15618227136 Sales@ATKchemical.com China 9342 58
Shanghai Yifei Biotechnology Co. , Ltd. 021-65675885 18964387627 customer_service@efebio.com China 11973 58
TargetMol Chemicals Inc. 15002134094 marketing@targetmol.cn China 20004 58
Sangon Biotech (Shanghai) Co.,Ltd. 400-821-026 Sales@sangon.com China 55710 58
Supplier Advantage
Shanghai Beckham Medical Technology Co., Ltd 55
Tianjin Kailiqi Biotechnology Co., Ltd. 55
Shanghai Chaolan Chemical Technology Center 58
Shanghai Yifei Biotechnology Co. , Ltd. 58
TargetMol Chemicals Inc. 58
Sangon Biotech (Shanghai) Co.,Ltd. 58
8-[3-(2-Benzofuranyl)-5-chloro-4-pyridinyl]-2,8-diazaspiro[4.5]decan-1-one CDK8-IN-12 CDK8-IN-12, 10 mM in DMSO 2613307-67-6