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LDC-4297 HCl (1453834-21-3(free base))

LDC-4297 HCl (1453834-21-3(free base))

产品编号 T4417   CAS T4417

LDC-4297 HCl (1453834-21-3(free base)) 是一种有效的选择性 CDK7 抑制剂,IC50 为 0.13 nM。

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LDC-4297 HCl (1453834-21-3(free base)) Chemical Structure
LDC-4297 HCl (1453834-21-3(free base)), CAS T4417
规格 价格/CNY 货期 数量
1 mg ¥ 525 现货
2 mg ¥ 749 现货
5 mg ¥ 987 现货
10 mg ¥ 1,690 现货
25 mg ¥ 3,490 现货
50 mg ¥ 4,960 现货
100 mg ¥ 7,190 现货
1 mL * 10 mM (in DMSO) ¥ 987 现货
其他形式的 LDC-4297 HCl (1453834-21-3(free base)):
千万补贴 助力科研
BCA蛋白浓度测定试剂盒限时半价
重组蛋白限时优惠
产品目录号及名称: LDC-4297 HCl (1453834-21-3(free base)) (T4417)
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纯度: 99.81%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 LDC4297 is a potent and selective CDK7 inhibitor with an IC50 of 0.13 nM.
靶点活性 CDK7:0.13 nM
体外活性 The affinity of LDC4297 for CDK7 proves to be extremely high. Kinase assays performed for CDK1, CDK2, CDK4, CDK6, CDK7, and CDK9 confirms the selective inhibitory activity of LDC4297 for CDK7 in the nano-picomolar range (IC50, 0.13±0.06 nM for CDK7 versus IC50s between 10 nM and 10,000 nM for all other analyzed CDKs). LDC4297 exerts anticytomegaloviral activity. Human cytomegalovirus (HCMV) replication is inhibited by LDC4297 in a concentration-dependent manner with an EC50 value of 24.5±1.3 nM. Inhibition is statistically significant and morphological signs of cytotoxicity only occurrs at concentrations of 3.3 μM or higher. Anti-HCMV activity of LDC4297 is exerted through a multifaceted mode of action that involves an interference with virus-induced Rb phosphorylation. Virus replication is broadly blocked by LDC4297, whereby the antiviral efficacies varied between the viruses used, i.e., strong efficacy for HSV-1 and VZV (EC50s = 0.02 and 0.06 μM, respectively) and intermediate to low efficacy for HSV-2 and EBV (EC50s = 0.27 and 1.21 μM, respectively
体内活性 An analysis of the PK parameters in CD1 mice reveals positive characteristics after oral administration, as demonstrated for a single-dose treatment (100 mg/kg of LDC4297). The half-life (t1/2z) is determined to be 1.6 h, and a time (Tmax) to a mean peak plasma concentration of 1,297.6 ng/mL is reached 0.5 h after administration, with a continued presence of LDC4297 plasma levels for at least 8 h and a bioavailability of 97.7%
细胞实验 A trypan blue exclusion assay is performed with cultured cells seeded in 24-well plates and incubated with increasing concentrations of antiviral compound LDC4297 (range, 0.1 to 50 μM) for the durations indicated. Cell staining is achieved with 0.1% trypan blue for 10 min at room temperature before the percentage of viable cells is determined by microscopic counting
分子量 469.02
分子式 C23H29ClN8O
CAS No. T4417

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 60 mg/mL (127.93 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1321 mL 10.6605 mL 21.3211 mL 53.3026 mL
5 mM 0.4264 mL 2.1321 mL 4.2642 mL 10.6605 mL
10 mM 0.2132 mL 1.0661 mL 2.1321 mL 5.3303 mL
20 mM 0.1066 mL 0.533 mL 1.0661 mL 2.6651 mL
50 mM 0.0426 mL 0.2132 mL 0.4264 mL 1.0661 mL
100 mM 0.0213 mL 0.1066 mL 0.2132 mL 0.533 mL

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TargetMol Library Books参考文献

1. Hutterer C,etal. A novel CDK7 inhibitor of the Pyrazolotriazine class exerts broad-spectrum antiviral activity at nanomolar concentrations.Antimicrob Agents Chemother. 2015 Apr;59(4):2062-71.
CDK12-IN-2 CDK-IN-2 CDK8-IN-13 GSK-3 inhibitor 4 AZD4573 ZCL278 CDK4-IN-1 SU9516

相关化合物库

该产品包含在如下化合物库中:
抑制剂库 已知活性化合物库 表型筛选靶点鉴定库 细胞周期化合物库 抗胰腺癌化合物库 抗乳腺癌化合物库 抗癌化合物库 NO PAINS 化合物库 激酶抑制剂库 经典已知活性库

TargetMol Calculator剂量换算

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TargetMol Calculator 体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

LDC-4297 HCl (1453834-21-3(free base)) T4417 Cell Cycle/Checkpoint CDK LDC4297 HCl (1453834213(free base)) LDC 4297 HCl (1453834 21 3(free base)) Inhibitor inhibitor inhibit

 

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