货号	规格	价格	上海	北京	珠海	重庆	武汉
T27103-5mg买3赠1	99.50%	￥620.00 T27103-5mg ￥620.00 现货（买3赠1）	6 6	-	-	-	-
T27103-10mg买3赠1	99.50%	￥930.00 T27103-10mg ￥930.00 现货（买3赠1）	5 5	-	-	-	-
T27103-25mg买3赠1	99.50%	￥1720.00 T27103-25mg ￥1720.00 现货（买3赠1）	4 4	-	-	-	-
T27103-100mg	≥98%	￥4350.00 T27103-100mg ￥4350.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Trilaciclib 是 CDK4/6 的抑制剂，对于 CDK4 和 CDK6 的 IC50 值分别为 1 nM 和 4 nM。

靶点：

IC50: 1 nM (CDK4), 4 nM (CDK6);CDK

体外研究：

Incubation with Trilaciclib (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 causes a transient, and reversible G1 arrest. A transient Trilaciclib-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.

体内研究：

Trilaciclib (G1T28) treatment results in a robust and dose-dependent suppression of proliferation in HSPCs at 12 hours, with 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 can produce reversible cell-cycle arrest in HSPCs in a dose-dependent manner in vivo. Mice given 100 mg/kg Trilaciclib 30 minutes prior to etoposide treatment, exhibits only background levels of caspase-3/7 activity. These data demonstrate that Trilaciclib can protect the bone marrow from chemotherapy-induced apoptosis in vivo. The data demonstrate that treatment with Trilaciclib prior to 5-FU likely decreases 5-FU-induced damage by chemotherapy in HSPCs, thus accelerating blood count recovery after chemotherapy.

参考文献：

1.Bisi JE, et al. Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93.

溶解性：

soluble in DMSO

保存条件：

-20°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.239 ml	11.197 ml	22.394 ml
5 mM	0.448 ml	2.239 ml	4.479 ml
10 mM	0.224 ml	1.12 ml	2.239 ml
50 mM	0.045 ml	0.224 ml	0.448 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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