Trilaciclib

Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC₅₀ values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy^[1]. IC50 & Target:IC50: 1 nM (CDK4), 4 nM (CDK6)^[1] In Vitro:Trilaciclib (10-1000 nM; 24 h) reversibly modulates the proliferation of mouse and canine bone marrow hematopoietic stem and progenitor cells^[1].
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^[1].
Trilaciclib (300 nM; 16 or 48 h) protects CDK4/6 dependent cells (HS68, WM2664) from chemotherapy-induced damage, and attenuates chemotherapy-induced-apoptosis^[1].
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^[1].