BLU-222

• UNSPSC Description:

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

• Target Antigen:

  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

• Solubility:

  DMSO : 100 mg/mL (ultrasonic)

• Smiles:

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

• 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.

• Shipping Conditions:

  Room Temperature

• Clinical Information:

  Phase 2

• CAS Number:

  2888704-84-3