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-ITK-ATI-2138
ATI-2138

Chemical Structure : ATI-2138

CAS No.: 2411407-25-3

加入收藏

ATI-2138

货号: PC-24215Not For Human Use, Lab Use Only.

ATI-2138 is a potent, selective, covalent and irreversible dual inhibitor of ITK/JAK3 with IC50 of 0.18 nM, 0.83 nM, and 0.52 nM for ITK, TXK, and JAK3 respectrively.

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)

生物&药学活性

ATI-2138 is a potent, selective, covalent and irreversible dual inhibitor of ITK/JAK3 with IC50 of 0.18 nM, 0.83 nM, and 0.52 nM for ITK, TXK, and JAK3 respectrively.
ATI-2138 is 27-fold less potent for inhibiting BTK and >4200-fold less potent for inhibiting the other JAK family members, JAK1, JAK2, and tyrosine kinase 2 (Tyk2).
ATI-2138 dose-dependently decreased JAK1/JAK3-dependent IL-2–stimulated STAT5 phosphorylation in human PBMCs with IC50 of 23.1 nM, with no inhibitory effect on the JAK1/JAK2-dependent IFNγ-induced STAT1 phosphorylation or the JAK2/Tyk2-dependent IL-12–induced STAT4 phosphorylation (>20 uM).
ATI-2138 inhibited anti-CD3–induced TCR-dependent activation and subsequent ITK/TXK-dependent phosphorylation of PLCγ1 in a concentration-dependent manner (IC50=7.6 nM.
ATI-2138 potently inhibited anti-CD3–stimulated IL-2 cytokine production (an ITK-dependent effect downstream of TCR stimulation) from PBMCs (IC50=8.6 nM),  inhibited IL-15-induced IFNγ production (IC50=2.6 nM).
ATI-2138 demonstrated disease-modifying activity in rodent models of arthritis and an adoptive T cell model of colitis.
ATI-2138 has the potential for enhanced therapeutic efficacy in the treatment of autoimmune and chronic inflammatory disease.

物理化学性质&存储条件

分子量 361.40
分子式 C18H21F2N5O
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

1-((2S,5R)-5-((5-((R)-2,2-difluorocyclopropyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)-2-methylpiperidin-1-yl)prop-2-en-1-one

参考文献

1. Kaul A, et al. J Pharmacol Exp Ther. 2025 Feb;392(2):100054.

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: