| Identification | Back Directory | [Name]
N-(5-(difluoromethoxy)-1H-pyrazol-3-yl)-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-pyrazolo[3,4-b]pyrazin-6-amine | [CAS]
2888704-84-3 | [Synonyms]
N-(5-(difluoromethoxy)-1H-pyrazol-3-yl)-1-((tetrahydro-2H-pyran-4-yl)methyl)-1H-pyrazolo[3,4-b]pyrazin-6-amine
1H-Pyrazolo[3,4-b]pyrazin-6-amine, N-[5-(difluoromethoxy)-1H-pyrazol-3-yl]-1-[(tetrahydro-2H-pyran-4-yl)methyl]- | [Molecular Formula]
C15H17F2N7O2 | [MOL File]
2888704-84-3.mol | [Molecular Weight]
365.34 |
| Chemical Properties | Back Directory | [Boiling point ]
581.6±50.0 °C(predicted) | [density ]
1.67±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | [form ]
Solid | [pka]
10.67±0.10(predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Cirtociclib (BLU-222) (60 mg/kg; twice daily) shows significant anti-tumor activity in both endometrial cancer PDX models[3]. | [References]
[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. DOI:10.1038/s41417-023-00589-z
[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. |
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