| Identification | Back Directory | [Name]
1-Piperidinecarboxylic acid, 4-[[2-methyl-8-(1-methylethyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl]amino]-, (3S)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]-3-pyrrolidinyl ester | [CAS]
2654003-64-0 | [Synonyms]
CDK7-IN-8
1-Piperidinecarboxylic acid, 4-[[2-methyl-8-(1-methylethyl)pyrazolo[1,5-a]-1,3,5-triazin-4-yl]amino]-, (3S)-1-[(2E)-4-(dimethylamino)-1-oxo-2-buten-1-yl]-3-pyrrolidinyl ester | [Molecular Formula]
C25H38N8O3 | [MOL File]
2654003-64-0.mol | [Molecular Weight]
498.62 |
| Hazard Information | Back Directory | [Uses]
CDK7-IN-8 is a potent CDK7 inhibitor with IC50 of 54.29 nM. CDK7-IN-8 has inhibitory effect on certain cancer cells and in vivo tumor models[1]. | [in vivo]
CDK7-IN-8 (20 or 40 mg/kg; i.g., single) has good advantages Pharmacokinetic properties[1].
CDK7-IN-8 (25 mg/kg; p.o., qd, for 21 days) effectively inhibits tumor proliferation with tumor growth inhibition (TGI) value of 81.9%[1].
Pharmacokinetic Parameters of CDK7-IN-8 in male ICR mice[1].
| IG (20 mg/kg) | IG (40 mg/kg) | | T1/2 (h) | 1.48 | 2.99 | | Tmax (h) | 0.50 | 4.67 | | Cmax (ng/mL) | 3379.92 | 783.01 | | AUC0-t (h*ng/mL) | 6258.34 | 7828.87 | | AUC0-∞ (h*ng/mL) | 6375.00 | 7879.45 |
| Animal Model: | Male ICR mice [1] | | Dosage: | 20 or 40 mg/kg | | Administration: | i.g., single (pharmacokinetic analysis) | | Result: | Showed good advantages Pharmacokinetic properties. |
| Animal Model: | Male BALB/c nude mice (injected with HCT116 tumor cells)[1] | | Dosage: | 25 mg/kg | | Administration: | p.o., qd, for 21 days | | Result: | Effectively inhibited tumor proliferation with tumor growth inhibition (TGI) value of 81.9%. |
| [IC 50]
CDK7: 54.29 nM (IC50) | [References]
[1] Hu Yonghan, et al. Heterocyclic compound, and pharmaceutical composition thereof, preparation method therefor, intermediate thereof and application thereof. WO2021121390 |
|
|