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Lerociclib

产品编号 T11345 CAS 1628256-23-4

别名: G1T38

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 2nM, 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively. 在相同实验条件下，摩尔浓度相同的化合物盐形式与游离态具有相同的生物活性，但盐形式 Lerociclib dihydrochloride 的水溶性和稳定性通常比游离态更好。

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Lerociclib, CAS 1628256-23-4

规格	价格/CNY		货期	数量
5 mg	￥ 1,250		5日内发货

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Lerociclib 的其他形式现货产品:

Lerociclib dihydrochloride

其他形式的 Lerociclib:

Lerociclib dihydrochloride
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 2nM, 1 nM for CDK6/CyclinD3 and CDK4/CyclinD1, respectively.
靶点活性	CDK6-CyclinD3:2 nM, CDK5-p35:0.832 μM, CDK2-CyclinA:1.5 μM, CDK5-p25:1.2 μM, CDK1-CyclinB1:2.4 μM, CDK2-CyclinE:3.6 μM, CDK4-CyclinD1:1 nM, CDK9-CyclinT:28 nM, CDK7-CyclinH-MAT1:2.4 μM
体外活性	Lerociclib produces a robust and sustained G1 arrest in CDK4/6 dependent cells with an EC50 of ~20 nM.?A dose dependent increase of cells in the G1 phase of the cell cycle is observed when CDK4/6 dependent WM2664 cells are treated with Lerociclib for 24 hours.?This arrest is maintained through 300 nM, more than 300x the biochemical IC50.?WM2664 cells treated with 30-1000 nM of Lerociclib for 24 hours exhibits a complete inhibition of RB phosphorylation compared to vehicle controls.?Treatment with Lerociclib reduces RB phosphorylation within 1 hour post-treatment and generates near complete inhibition of RB phosphorylation by 16 hours post-treatment.?Lerociclib produces a robust inhibition of proliferation in a diverse array of tumor cell lines including breast, melanoma, leukemia and lymphoma with EC50 concentrations as low as 23 nM.Within the CDK family, Lerociclib is least selective against CDK9/cyclin T, ~30 fold between CDK4/cyclin D1 and CDK9/ cyclin T at the biochemical IC50.
体内活性	In this HER2+ breast cancer model, Mice treated with Lerociclib elicits 8% tumor regression after 21 days of treatment while control animals have a 577% increase in tumor burden over the same treatment period.?Compared to the vehicle-treated mice, daily treatment with 100 mg/kg of Lerocyclib or palbociclib shows tumor regression within 10 days in the MCF7 xenograft model.?After 27 days of treatment, tumor growth inhibition is observed in the 10, 50, and 100 mg/kg Lerociclib cohorts (approximately 12%, 74%, and 90% inhibition, respectively).?Daily oral palbociclib treatment causes an 18%, 66%, and 87% tumor growth inhibition in the 10, 50, and 100 mg/kg dosage cohorts, respectively.

别名	G1T38
分子量	474.6
分子式	C26H34N8O
CAS No.	1628256-23-4

存储

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

计算器

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稀释计算器

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参考文献

1. Bisi JE, et al. Preclinical development of G1T38: A novel, potent and selective inhibitor of cyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors. Oncotarget. 2017 Jun 27;8(26):42343-42358.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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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