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-Tyrosine Kinase-ROS1-TY-2136
TY-2136

Chemical Structure : TY-2136

CAS No.: 2649878-59-9

加入收藏

TY-2136 (TY-2136b, TY2136)

货号: PC-21571Not For Human Use, Lab Use Only.

TY-2136 is a next generation ROS1/TRK/ALK inhibitor with IC50 of 1.6 nM and 460.1 nM for ROS1 G2032R and TRKA G595R, respectively, inhibits ROS1/TRK/ALK mutations and overcomes drug resistance due to acquired solvent-front mutations.

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

    TY-2136 is a next generation ROS1/TRK/ALK inhibitor with IC50 of 1.6 nM and 460.1 nM for ROS1 G2032R and TRKA G595R, respectively, inhibits ROS1/TRK/ALK mutations and overcomes drug resistance due to acquired solvent-front mutations.
    TY-2136 shows similar potency to TPX-0005 inhibiting ROS1 G2032R mutant activity, confers significantly stronger potency than LOXO-101 inhibiting TRKA activity with G595R substitution.
    TY-2136b is similar potent as TPX-0005 inhibiting cell proliferation of the Ba/F3 strain expressing mutant ROS1 bearing G2032R mutation, a major resistance mutation.
    TY-2136b also shows potent inhibition towards ROS1, ERK and AKT phosphorylation and downstream signaling in Ba/F3-CD74-ROS1-G2032R cells.
    TY-2136b is better than TPX-0005 and LOXO-195 against TRKA G595R/F589L dual mutations in vitro.
    TY-2136b shows dose-dependent anti-tumor effect at the dose of 5, 10, and 20 mg/kg, bid, in xenograft tumor models carrying ROS1 G2032R and TRKA G595R mutation, and is more effective than Crizotinib and LOXO-101.

    物理化学性质&存储条件

    分子量 390.37
    分子式 C18H17F3N6O
    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

    (R)-3-(5,5-dimethyl-4,5-dihydro-1,2,4-oxadiazol-3-yl)-N-(1-(2,3,5-trifluorophenyl)ethyl)pyrazolo[1,5-a]pyrimidin-5-amine

    参考文献

    1. Chengshan Niu, et al. Cancer Res (2023) 83 (7_Supplement): 3400.

    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: