Trilaciclib产品描述：Trilaciclib is a CDK4/6 inhibitor with IC₅₀s of 1 nM and 4 nM for CDK4 and CDK6, respectively.IC50 & Target: IC50: 1 nM (CDK4), 4 nM (CDK6)^[1]In Vitro: 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^[1].In Vivo: 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^[1].
产品链接：www.medchemexpress.com/Trilaciclib.html

研究领域：Cell Cycle/DNA Damage

靶点：CDK

相关产品：LY2835219  |  Dinaciclib  |  LEE011  |  THZ1  |  Roscovitine  |  Ro-3306  |  Flavopiridol  |  1-NM-PP1  |  THZ2  |  AZD-5438  |  BAY-1143572  |  BIO  |  BS-181  |  SNS-032  |  LDC000067  |  



公司介绍：MedChemExpress(MCE)专注于各种抑制剂、激动剂、API及化合物库，总部位于美国新泽西，分别在瑞典和上海设有欧洲区子公司和亚洲区总代理，营销网点遍及全球20多个国家地区。MCE经过多年努力已成为全球生物活性小分子领域的一流供应商， 产品涵盖癌症、神经科学、抗感染、表观遗传学等20个热门研究领域，PI3K、MAPK等近千个细分靶点，超过4000个活性小分子化合物现货，以及GPCR、API、离子通道等超过20种不同类型的化合物库，同时提供从毫克到千克的专业定制合成服务。
MCE 对每批产品都进行严格的LCMS和NMR检验，其产品已被全球近万名客户广泛使用并发表大量文章、；
MCE 定期增加各领域热门抑制剂、激动剂，不断扩增已有化合物库，以满足*新的科研需求；
数千种产品在上海有充足备货，24-48小时内送达客户；
大量产品提供免费试用装；已为全球多个知名企业、院校构建各种定制型化合物库。

更新时间：2024/1/2 10:10:55