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Trilaciclib
CAS No. : 1374743-00-6
MCE 国际站:Trilaciclib
产品活性:Trilaciclib (G1T28) 是一种口服有效的 CDK4/6 的抑制剂,对于 CDK4 和 CDK6 的 IC50 值分别为 1 nM 和 4 nM。Trilaciclib 能够有效抑制肿瘤细胞增殖,并减轻化疗产生的血液毒性。Trilaciclib 可减轻 5FU (HY-90006) 化疗引起的细胞凋亡和骨髓抑制。
作用靶点:CDK
In Vitro: Trilaciclib (10-1000 nM; 24 h) reversibly modulates the proliferation of mouse and canine bone marrow hematopoietic stem and progenitor cells.
Trilaciclib (10-1000 nM; 24 h) can arrest the cell cycle of CDK4/6-dependent cells in the G1 phase, with an EC50 of 30 nM for HS68.
Trilaciclib (300 nM; 16 or 48 h) protects CDK4/6 dependent cells (HS68, WM2664) from chemotherapy-induced damage, and attenuates chemotherapy-induced-apoptosis.
In Vivo: Trilaciclib (50-150 mg/kg; po; single dose) protects mouse bone marrow cells from chemotherapy-induced apoptosis and attenuates chemotherapy-induced myelosuppression in vivo. Trilaciclib at 150 mg/kg reduces HSPC damage induced by 5FU (HY-90006) (150 mg/kg; ip) chemotherapy, thereby accelerating blood count recovery after chemotherapy.
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