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-EGFR-TAS-121
TAS-121

Chemical Structure : TAS-121

CAS No.: 1451370-01-6

加入收藏

TAS-121 (TAS121)

货号: PC-38346Not For Human Use, Lab Use Only.

TAS-121 (TAS 121) is an orally available, potent, novel third-generation EGFR-TKI that selectively targets EGFR activating and T790M resistance mutations, sparing wild-type EGFR.

规格 价格 库存 数量
50 mg Get quote
100 mg Get quote
250 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

    TAS-121 (TAS 121) is an orally available, potent, novel third-generation EGFR-TKI that selectively targets EGFR activating and T790M resistance mutations, sparing wild-type EGFR.
    TAS-121 inhibited the L858R mutation and Ex19del mutation of EGFR with IC50 values of 1.7 and 2.7 nM, respectively.
    TAS-121 also inhibited the L858R/T790M mutation and Ex19del/T790M mutation with IC50 values of 0.56 and 1.1 nM, inhibits wild-type EGFR with IC50 of 8.2 nM.
    TAS-121 potently inhibited the growth of HCC827 cells (EGFR Ex19del) and NCI-H1975 cells (EGFR L858R, T790M), with IC50 values of 3.8 and 30 nM, respectively.
    TAS-121 (50 and 100 mg/kg) showed potent dose-dependent activity against NCI-H1975 tumors, and regression of lesions in NCI-H1975 xenograft models, also showed antitumor activity in an HCC827 xenograft model at doses from 6.3 to 25 mg/kg.
    TAS-121 (25 to 100 mg/kg) showed antitumor activity in an SW48 xenograft model harboring an EGFR G719S mutation.

    物理化学性质&存储条件

    分子量 384.443
    分子式 C22H20N6O
    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

    (S)-N-(4-amino-5-(quinolin-3-yl)-6,7,8,9-tetrahydropyrimido[5,4-b]indolizin-8-yl)acrylamide

    参考文献

    1. Nishio M, et al. Invest New Drugs. 2019 Dec;37(6):1207-1217.

    2. Ito K, et al. Mol Cancer Ther. 2019 May;18(5):920-928.

    3. Watanabe S, et al. Thorac Cancer. 2021 Mar;12(5):631-642.

    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: