欢迎访问ProbeChem中文网站，英文网站请访问www.probechem.com
    英文 |     中文

产品咨询: sales@probechem.com
订购: order@probechem.com

首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-Culmerciclib
Culmerciclib

Chemical Structure : Culmerciclib

CAS No.: 2004705-28-4

加入收藏

Culmerciclib (TQB3616, TQB 3616)

货号: PC-49131Not For Human Use, Lab Use Only.

TQB3616 (Culmerciclib) is a potent, selective inhibitor of CDK4/6 with IC50 of 0.35 nM and 0.49 nM for CDK4/D1CDK6/D1 respectively, shows remarkable inhibitory effect on hormone receptor-positive breast cancer cells.

规格 价格 库存 数量
25 mg Get quote
50 mg Get quote
100 mg Get quote
获取报价单
* 请选择数量再加入购物车
 or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    TQB3616 (Culmerciclib) is a potent, selective inhibitor of CDK4/6 with IC50 of 0.35 nM and 0.49 nM for CDK4/D1CDK6/D1 respectively, shows remarkable inhibitory effect on hormone receptor-positive breast cancer cells.
    TQB3616 shows enzymatic inhibitory IC50 of 246 nM, 35.3 nM, and 12.5 nM against CDK1/cyclin B, CDK5/p25, and CDK9/cyclin T1 respectively,
    TQB3616 potently inhibits tumor cell proliferation for T47D cells (IC50=82.4 nM) and MCF-7 cells (IC50=115.5 nM).
    TQB3616 shows better inhibitory activity in the HER2-positive /HR-positive breast cancer cells than abemaciclib.
    TQB3616 (1.5 uM) reduces colony formation of T47D and BT474 cells, inhibits the abnormal activation of phosphorylated Cyclin D protein.
    TQB3616 not only induced G1 stalling, leading to a profound reduction in the level of RB protein phosphorylated at Ser807/811, but also showed enhanced tumor killing effects by promoting cell apoptosis.
    TQB3616 showed more potent antitumor activity than abemaciclib in an in vitro breast cancer xenograft model.

    物理化学性质&存储条件

    分子量 446.534
    分子式 C24H27FN8
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    5-fluoro-4-[2-methyl-3-(propan-2-yl)-2H-indazol-5-yl]-N-[5-(piperazin-1-yl)pyridin-2-yl]pyrimidin-2-amine

    参考文献

    1. Patent WO2021259203 A1 2021-12-30.
    2. Patent WO2016141881 A1 2016-09-15.
    3. Xu Z, et al. Bioorg Med Chem Lett. 2024 Apr 24:129769.

    备案号：沪ICP备16042516号-1 Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright

    联系我们 sales@probechem.com

    Bulk Inquiry

    * Indicates a Required FieldYour information is safe with us.

    • *Product name:
    • *Applicant name:
    • *Email address:
    • *Organization name:
    • *Requested quantity:
    • *Country:
    • *Additional Information:

    询单

    • *产品名称:
    • *姓名:
    • *邮箱:
    • *公司名称:
    • *询单数量:
    • *国籍:
    • 询单信息: