2397678-18-9
Chemical Structure
Tibremciclib
Synonym(s): BPI-16350
- CAS No.: 2397678-18-9
- Formula:C28H32F2N8
- Molecular Weight:518.60
InChIKey: XOJPAVACYRFOBK-GOSISDBHSA-N
SMILES: C[C@H]1N2C3=CC(C4=NC(NC5=CC=C(C=N5)CN6CCN(CC6)CC)=NC=C4F)=CC(F)=C3N=C2CCC1
Biological Activity: Tibremciclib (BPI-16350) is an orally active CDK4/6 inhibitor. Tibremciclib selectively inhibits CDK4/cyclin D1 and CDK6/cyclin D1 with IC50 values of 2.21 nM and 0.407 nM, respectively. Tibremciclib blocks Rb phosphorylation and cell cycle progression, and induces G1 phase arrest in Rb-positive tumor cells, exhibiting broad-spectrum anti-tumor cell proliferation activity. Tibremciclib inhibits MATE1 and MATE2-K. Tibremciclib dose-dependently inhibits tumor growth in xenograft models, and shows synergistic effects when combined with Fulvestrant (HY-13636). Tibremciclib can be used for research related to breast cancer[1][2][3].
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Tibremciclib | Tibremciclib (BPI-16350) is an orally active CDK4/6 inhibitor. Tibremciclib selectively inhibits CDK4/cyclin D1 and CDK6/cyclin D1 with IC50 values of 2.21 nM and 0.407 nM, respectively. Tibremciclib blocks Rb phosphorylation and cell cycle progression, and induces G1 phase arrest in Rb-positive tumor cells, exhibiting broad-spectrum anti-tumor cell proliferation activity. Tibremciclib inhibits MATE1 and MATE2-K. Tibremciclib dose-dependently inhibits tumor growth in xenograft models, and shows synergistic effects when combined with Fulvestrant (HY-13636). Tibremciclib can be used for research related to breast cancer. | |||||||||||||||||||||
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References
- [1]. Gao S, et al. A novel potent CDK4/6 inhibitor BPI-16350 in preclinical cancer models[J]. 2022.
- [2]. Zhang J, et al. A phase I dose-escalation and dose-expansion study of tibremciclib, a novel CDK4/6 inhibitor, monotherapy and in combination with fulvestrant in HR-positive/HER2-negative advanced breast cancer. ESMO open. 2025 Jun 1;10(6):105121.
- [3]. Shu L, et al. CDK4/6 inhibitor-associated vortex keratopathy: a case report. BMC Ophthalmology. 2025 Apr 14;25(1):206.
