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GCN2iB

CAS No. 2183470-12-2

GCN2iB ( —— )

产品货号. M26229 CAS No. 2183470-12-2

GCN2iB 是一种 ATP 竞争性的一般控制非阻抑物 2 (GCN2) 抑制剂,IC50 为 2.4 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
5MG ¥1549 有现货
10MG ¥2527 有现货
25MG ¥4157 有现货
50MG ¥5924 有现货
100MG ¥7857 有现货
500MG 获取报价 有现货
1G 获取报价 有现货
1 mL x 10 mM in DMSO ¥1701 有现货

生物学信息

  • 产品名称
    GCN2iB
  • 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
    GCN2iB 是一种 ATP 竞争性的一般控制非阻抑物 2 (GCN2) 抑制剂,IC50 为 2.4 nM。
  • 产品描述
    GCN2iB is an ATP-competitive inhibitor of general control nonderepressible 2 (GCN2) with an IC50 of 2.4 nM.(In Vitro):GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity.?In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity.(In Vivo):In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth.?Notably, a combination of ASNase and GCN2iB elicits potent antitumor activity (P=0.0002) with synergistic effects.?In MV-4-11 and SU.86.86 xenografts, the robust antitumor activity of the combination of GCN2iB and ASNase is observed with a synergistic effect, respectively.?ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation.
  • 体外实验
    GCN2iB shows an IC50 value of 2.4 nM for GCN2 and potent cellular activity. In a panel of 468 kinases, only GCN2 shows >99.5% inhibition, and three kinases (MAP2K5, STK10, and ZAK) show >95%inhibition at 1 μM GCN2iB, demonstrating high kinase selectivity.
  • 体内实验
    In the antitumor activity study of the CCRF-CEM xenografts, ASNase or GCN2iB alone does not significantly affect tumor growth. Notably, a combination of ASNase and GCN2iB elicit potent antitumor activity (P=0.0002) with synergistic effects. In MV-4-11 and SU.86.86 xenografts, robust antitumor activity of the combination of GCN2iB and ASNase is observed with synergistic effect, respectively. ASNase/GCN2iB-treated tumors do not show significant growth even after drug cessation. The combination of ASNase and GCN2iB yield survival advantage compared with the vehicle treated control with synergistic effect.
  • 同义词
    ——
  • 通路
    Others
  • 靶点
    Other Targets
  • 受体
    Antibacterial
  • 研究领域
    ——
  • 适应症
    ——

化学信息

  • CAS Number
    2183470-12-2
  • 分子量
    451.83
  • 分子式
    C18H12ClF2N5O3S
  • 纯度
    >98% (HPLC)
  • 溶解度
    In Vitro:?DMSO : 50 mg/mL (110.66 mM)
  • SMILES
    COc1ncc(Cl)cc1S(=O)(=O)Nc1ccc(F)c(C#Cc2cnc(N)nc2)c1F
  • 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.Losch K. [Pharmacokinetic studies of sulfamerazine-Na, sulfaperine-Na and sulfadimidine-Na in the hen]. Arch Exp Veterinarmed. 1980;34(4):587-94. German.
产品手册
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