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KRAS G12D inhibitor 14

CAS No. 2765254-39-3

KRAS G12D inhibitor 14 ( —— )

产品货号. M35624 CAS No. 2765254-39-3

KRAS G12D inhibitor 14 是一种有效的 KRAS G12D 抑制剂,与 KRAS G12D蛋白结合的 KD 为 33 nM。KRAS G12D inhibitor 14 降低 KRAS G12D (KRAS G12D-GTP) 的活性形式,但不降低 KRAS G13D。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
500MG 获取报价 有现货
1G 获取报价 有现货

生物学信息

  • 产品名称
    KRAS G12D inhibitor 14
  • 注意事项
    本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
  • 产品简述
    KRAS G12D inhibitor 14 是一种有效的 KRAS G12D 抑制剂,与 KRAS G12D蛋白结合的 KD 为 33 nM。KRAS G12D inhibitor 14 降低 KRAS G12D (KRAS G12D-GTP) 的活性形式,但不降低 KRAS G13D。
  • 产品描述
    KRAS G12D inhibitor 14 is a potent KRAS G12D inhibitor with a KD of 33 nM for binding to KRAS G12D protein. KRAS G12D inhibitor 14 decreases the active form of KRAS G12D (KRAS G12D-GTP) but not KRAS G13D.
  • 体外实验
    KRAS G12D inhibitor 14 (compound KD-8) shows antiproliferative activity with an IC50 of 2.1 μM against three KRAS G12D-mutated cells (Panc1, SW1990 and CT26). KRAS G12D inhibitor 14 decreases the active form of KRAS (KRAS-GTP) in KRAS G12D mutated cancer cell lines (CT26 and SW1990) but not in KRAS G13D mutated cancer cell lines (HCT116). KD-8 also causes efficient apoptosis of SW1990 and CT26 cancer cells. KRAS G12D inhibitor 14 down-regulates the phosphorylated Raf and Erk in CT26 and SW1990 cancer cell lines but not in HeLa cells (KRAS WT).
  • 体内实验
    KRAS G12D inhibitor 14 (compound KD-8) (40 mg/kg or 60 mg/kg; i.p.) exhibits significant antitumor efficacy in a CT26 tumor model with a tumor growth inhibition (TGI) of 42% or 53% without causing apparent toxicity.
  • 同义词
    ——
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    Kras
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    2765254-39-3
  • 分子量
    420.45
  • 分子式
    C20H19F3N4OS
  • 纯度
    >98% (HPLC)
  • 溶解度
    In Vitro:?DMSO 中的溶解度 : 50 mg/mL (118.92 mM; 超声助溶 (<60°C)
  • SMILES
    O(C)C1=C(C2=CC3=C(N=CN=C3S2)N4C5CCC(C4)NC5)C=C(C(F)(F)F)C=C1
  • 化学全称
    ——

运输与储存

  • 储存条件
    (-20℃)
  • 运输条件
    With Ice Pack
  • 稳定性
    ≥ 2 years

参考文献

1. Li L, et al. Discovery of Thieno[2,3-d]pyrimidine-based KRAS G12D inhibitors as potential anticancer agents via combinatorial virtual screening. Eur J Med Chem. 2022;233:114243.?
产品手册
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