全部分类
  • Umbralisib
Umbralisib的可视化放大

Umbralisib

A PI3K p110δ inhibitor

此产品仅用于科学研究,我们不为任何个人用途提供产品和服务

Umbralisib的二维码
  • 库存: 现货
可选规格
  • 包装
    价格
    促销价
    数量
  • 1mg
    ¥425.00
    340.00
    - +
  • 5mg
    ¥937.00
    750.00
    - +
  • 10mg
    ¥1612.00
    1290.00
    - +
  • 25mg
    ¥3687.00
    2950.00
    - +
  • 50mg
    ¥4862.00
    3890.00
    - +
  • 100mg
    ¥8312.00
    6650.00
    - +
已选 0 0
金额: ¥0.00
首页 收藏
  • 货号: ajci22952
  • CAS: 1532533-67-7
  • 别名: TGR-1202; RP5264
  • 分子式: C31H24F3N5O3
  • 分子量: 571.55
  • 纯度: >98%
  • 溶解度: DMSO : 20 mg/mL (34.99 mM)
  • 储存: Store at -20°C
  • 库存: 现货

Background

TGR-1202 is a PI3Kδ inhibitor, with IC50 and EC50 of 22.2 nM and 24.3 nM, respectively.


RP5264 causes a half-maximal inhibition of human whole blood CD19 cell proliferation between 100-300 nM[1]. In human lymphoma and leukemia cell lines, TGR-1202 (10 nM-100 uM) inhibits phosphorylated AKT at Ser473 in a concentration-dependent manner. TGR-1202 and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. TGR-1202 and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. TGR-1202 (15-50 uM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells[2].


In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, TGR-1202 (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25[2].

参考文献:
[1]. Swaroop Vakkalankaa, et al. Inhibition of PI3Kδ kinase by a selective, small molecule inhibitor suppresses B-cell proliferation and leukemic cell growth.
[2]. Deng C, et al. Silencing c-Myc translation as a therapeutic strategy through targeting PI3Kδ and CK1ε in hematological malignancies. Blood. 2017 Jan 5;129(1):88-99

没有评价数据

温馨提示 ×
商品已成功加入购物车!
购物车共 0 件商品
去购物车结算