货号	规格	价格	上海	北京	珠海	重庆	武汉
T23442-5mg	≥98%	￥900.00 T23442-5mg ￥900.00 3-5天	0 货期：3-5天	-	-	-	-
T23442-10mg	≥98%	￥1200.00 T23442-10mg ￥1200.00 3-5天	0 货期：3-5天	-	-	-	-
T23442-25mg	≥98%	￥2400.00 T23442-25mg ￥2400.00 3-5天	0 货期：3-5天	-	-	-	-
T23442-100mg	≥98%	￥7200.00 T23442-100mg ￥7200.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

Lerociclib dihydrochloride (G1T38 dihydrochloride) 是一种有效的选择性 CDK4/CDK6 抑制剂，抑制 CDK4/CyclinD1 和 CDK6/CyclinD3，IC50 值分别为 1 nM 和 2 nM。

靶点：

Cdk4/cyclin D1:1 nM (IC50);cdk6/cyclin D3:2 nM (IC50)

体外研究：

Within the CDK family, Lerocyclib is least selective against CDK9/cyclin T, ~30 fold between CDK4/cyclin D1 and CDK9/ cyclin T at the biochemical IC50. 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 G1T38 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 G1T38 reduces RB phosphorylation within 1 hour post-treatment and generates near complete inhibition of RB phosphorylation by 16 hours post-treatment. G1T38 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.

体内研究：

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 Lerociclib 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. Interestingly, at 50 mg/kg, Lerociclib is significantly more efficaciou than palbociclib. Similar results are seen in the ER+ ZR-75-1 breast cancer xenograft model when comparing Lerocyclib and palbociclib at the 50 mg/kg dose. Lerociclib treated mice exhibits 77% TGI with an overall 60% tumor growth delay demonstrating Lerociclib alone is highly efficacious in this NSCLC tumor model.

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.

溶解性：

soluble in H2O

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.826 ml	9.132 ml	18.264 ml
5 mM	0.365 ml	1.826 ml	3.653 ml
10 mM	0.183 ml	0.913 ml	1.826 ml
50 mM	0.037 ml	0.183 ml	0.365 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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