Cirtociclib

Cirtociclib (BLU-222) is an orally active and highly selective CDK2 inhibitor. Cirtociclib disrupts Rb signaling and causes G1 arrest and apoptosis in CCNE1-amplified endometrial cancer cells[1][2][3].

Product Specifications

CAS Number

[2888704-84-3]

Product Name Alternative

BLU-222

UNSPSC

12352005

Target

Apoptosis; CDK

Type

Reference compound

Related Pathways

Apoptosis; Cell Cycle/DNA Damage

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/blu-222.html

Concentration

10mM

Purity

99.02

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

FC(OC1=CC(NC2=NC3=C(C=NN3CC4CCOCC4)N=C2)=NN1)F

Molecular Formula

C15H17F2N7O2

Molecular Weight

365.34

References & Citations

[1]Talbot T, et al. Amplified therapeutic targets in high-grade serous ovarian carcinoma - a review of the literature with quantitative appraisal. Cancer Gene Ther. 2023 Jul;30 (7) :955-963.|[2]House N, et al. BLU-222, a potent and highly selective CDK2 inhibitor, demonstrated antitumor activity as monotherapy and as combination treatment in CCNE1-aberrant endometrial cancer models[J]. Cancer Research, 2024, 84 (6_Supplement) : 1959-1959.|[3]Luo L, et al. Abstract PO1-18-05: Combination treatment with CDK2 inhibitor (BLU-222) and either palbociclib or ribociclib is synergistic in pre-clinical models of CDK4/6 inhibitor-resistant breast cancer[J]. Cancer Research, 2024, 84 (9_Supplement) : PO1-18-05-PO1-18-05.