2803837-13-8

2803837-13-8 structure
2803837-13-8 structure
  • Name: CDK2/4/6-IN-1
  • Chemical Name: CDK2/4/6-IN-1
  • CAS Number: 2803837-13-8
  • Molecular Formula: C22H22N4O4S
  • Molecular Weight: 438.50
  • Catalog: Signaling Pathways Cell Cycle/DNA Damage CDK
  • Create Date: 2022-12-06 16:24:18
  • Modify Date: 2024-01-13 18:25:38
  • CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research[1].

Name CDK2/4/6-IN-1
Description CDK2/4/6-IN-1(example 29) is a CDK2/4/6 inhibitor with IC50 values of 2.5, 23.7 and 44.3 nM for CDK2, CDK4 and CDK6, respectively. CDK2/4/6-IN-1 can be used in cancer research[1].
Related Catalog
Target

CDK2:2.5 nM (IC50)

CDK4:23.7 nM (IC50)

CDK6:44.3 nM (IC50)

In Vitro CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits the proliferation of OVCAR3 and MCF7 cells with the IC50 values of 14.6 and 117.8 nM, respectively[1]. CDK2/4/6-IN-1(example 29) (0-600 nM, 24 h) inhibits phosphorylation of Rb protein in OVCAR3 and MCF7 cells with the IC50 values of 18 and 581 nM, respectively[1].
In Vivo CDK2/4/6-IN-1(example 29) (25 mg/kg or 50 mg/kg, once a day, orally) has a significant inhibitory effect on tumor growth[1]. The pharmacokinetic parameters of example 29 in BALB/c mice (10 mg/kg, p.o.) Parameters Cmax(ng/mL) Tmax(hr) AUClast(hr*ng/mL) T1/2(hr) PO 4050 0.5 10050 4.8The pharmacokinetic parameters of example 29 in BALB/c mice (3 mg/kg, i.v.) Parameters C0(ng/mL) T1/2(hr) AUClast(hr*ng/mL) Vss(L/Kg) IV 4407 0.7 3245 0.9
References

[1]. ZHANG YAN, et al. Cdk2/4/6 inhibitor, preparation method therefor, and application thereof. WO2022152259 A1.

Molecular Formula C22H22N4O4S
Molecular Weight 438.50