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Lerociclib dihydrochloride (G1T38 dihydrochloride)

  • 產品貨號:CS-01Y70619
  • 產品價格:電議
  • 產品產地:進口、國產
  • 包裝類型:10mM*1mLinDMSO 5mg 10mg 25mg 50mg 100mg
  • 采購熱度:265
  • 庫存:100
  • CAS號:2097938-59-3
  • 方法:
  • 含量:>98.00%
  • 品牌名稱:莼試
  • 分子式:C26H36Cl2N8O
  • 分子量:547.52

簡介內容:質量保證、價格優惠

在線訂購  免費訂購熱線:021-59541103 021-60443211

標簽:Lerociclib dihydrochloride (G1T38 dihydrochloride) 

產品目錄

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規格

10mM*1mLinDMSO 5mg 10mg 25mg 50mg 100mg

CAS

2097938-59-3

別名

N/A

化學名

N/A

分子式

C26H36Cl2N8O

分子量

547.52

溶解度

H2O : 4 mg/mL (7.31 mM)

儲存條件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

產品描述:                                                                                                            

Lerociclib (G1 T38) dihydrochloride is a potent and selective inhibitor of CDK4/CDK6, with IC50s of 1 nM and 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

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[1].

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[1].

特別提醒:                                                                                                              

1. 本產品僅供科研使用。請勿用于醫藥、臨床診斷或治療,食品及化妝品等用途。請勿存放于普通住宅區。

2. 為了您的安全和健康,請穿好實驗服并佩戴一次性手套和口罩操作。

原創作者:上海莼試生物技術有限公司

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