1. Cell Cycle/DNA Damage
  2. CDK
  3. Trilaciclib hydrochloride

Trilaciclib hydrochloride (Synonyms: G1T28 hydrochloride)

目录号: HY-101467A 纯度: 99.24%
产品使用指南

Trilaciclib hydrochloride (G1T28 hydrochloride) 是 CDK4/6 的抑制剂,对 CDK4 和 CDK6 的 IC50 值分别为 1 nM 和 4 nM。

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Trilaciclib hydrochloride Chemical Structure

Trilaciclib hydrochloride Chemical Structure

CAS No. : 1977495-97-8

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Trilaciclib hydrochloride (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively[1].

IC50 & Target

Cdk4/cyclin D1

1 nM (IC50)

cdk6/cyclin D3

4 nM (IC50)

体外研究
(In Vitro)

Incubation with Trilaciclib hydrochloride (G1T28) for 24 hours induces a robust G1 cell-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 G1 arrest. A transient Trilaciclib hydrochloride-mediated G1 cell-cycle arrest in CDK4/6-sensitive cells decreases the in vitro toxicity of a variety of commonly used cytotoxic chemotherapy agents associated with myelosuppression[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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 manner in 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 apoptosis in 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
分子量

519.47

Formula

C24H32Cl2N8O

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9250 mL 9.6252 mL 19.2504 mL
5 mM 0.3850 mL 1.9250 mL 3.8501 mL
10 mM 0.1925 mL 0.9625 mL 1.9250 mL
*

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
Kinase Assay
[1]

HS68, WM2664, and A2058 cells are treated with 300 nM Trilaciclib hydrochloride (G1T28) or DMSO (0.1%), for 4, 8, 16, or 24 hours. Whole cell extracts are prepared using 1× radioimmunoprecipitation assay buffer containing 1× HALT protease and phosphatase inhibitors. Total protein concentration is determined by using the kit, according to the manufacturer's instructions. For Western blot analysis, protein is processed as described previously. Antibodies to total RB and β-tubulin run as a loading control are assessed[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

HS68 cells are treated for 24 hours with Trilaciclib hydrochloride (G1T28) at 10, 30, 100, 300, 1,000, or 3,000 nM final concentration. Cells are harvested and fixed in ice-cold methanol. Fixed cells are stained with 20 μg propidium iodide, 50 μg RNAse A in PBS-CMF (calcium magnesium free) +1% BSA, Fraction V. Samples are processed on Cyan ADP Analyzer, and cell-cycle analysis is completed using software[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Female athymic nude mice are implanted with H69 cells and monitored until treatment initiation. Once tumors reach an acceptable size (150 mm3), mice are dosed in various combinations of Trilaciclib hydrochloride (G1T28) and topotecan for 5 days per week for 4 weeks. Tumors are measured for up to 60 days after treatment. All mice that reach excessive tumor burden before 60 days are humanely euthanized. Topotecan and Trilaciclib hydrochloride levels in blood plasma from the mice treated with Trilaciclib hydrochloride and/or topotecan are processed and analyzed using established methods[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

纯度: 99.24%

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× = ×
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产品名称:
Trilaciclib hydrochloride
目录号:
HY-101467A
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