Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
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 |
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 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (127.93 mM)
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 |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
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。
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