Trilaciclib hydrochloride (G1T28 hydrochloride) is aCDK4/6inhibitor withIC₅₀s of 1 nM and 4 nM forCDK4andCDK6, respectively^[1].

Incubation with Trilaciclib hydrochloride (G1T28) for 24 hours induces a robust G₁cell-cycle arrest (time=0). By 16 hours after Trilaciclib hydrochloride washout, cells have reentered the cell cycle and demonstrate cell-cycle kinetics similar to untreated control cells. These results demonstrate that Trilaciclib hydrochloride causes a transient, and reversible G₁arrest. A transient Trilaciclib hydrochloride-mediated G₁cell-cycle arrest in CDK4/6-sensitive cells decreases thein vitrotoxicity of a variety of commonly used cytotoxic chemotherapy agents associated with myelosuppression^[1].

Trilaciclib hydrochloride (G1T28) treatment results in a robust and dose-dependent suppression of proliferation in HSPCs at 12 hours, with 5-ethynyl-2′-deoxyuridine (EdU) incorporation returning near baseline levels in a dose-dependent manner by 24 hours after administration. These data demonstrate that a single oral dose of Trilaciclib hydrochloride can produce reversible cell-cycle arrest in HSPCs in a dose-dependent mannerin vivo. Mice given 100 mg/kg Trilaciclib hydrochloride 30 minutes prior to etoposide treatment, exhibits only background levels of caspase-3/7 activity. These data demonstrate that Trilaciclib hydrochloride can protect the bone marrow from chemotherapy-induced apoptosisin vivo. The data demonstrate that treatment with Trilaciclib hydrochloride prior to 5-fluorouracil (5-FU) likely decreases 5-FU-induced damage by chemotherapy in HSPCs, thus accelerating blood count recovery after chemotherapy^[1].

519.47

Solid

C₂₄H₃₂Cl₂N₈O

1977495-97-8

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

H₂O : 25.64 mg/mL(49.36 mM;ultrasonic and adjust pH to 2 with HCl)

DMSO : 1.1 mg/mL(2.12 mM;Need ultrasonic)

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。