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Afuresertib hydrochloride

CAS No. 1047645-82-8

Afuresertib hydrochloride ( GSK 2110183 hydrochloride | GSK2110183 hydrochloride )

产品货号. M10235 CAS No. 1047645-82-8

一种有效的、选择性的 ATP 竞争性泛 AKT 抑制剂,对于 AKT1/2/3 的生化 IC50 为 0.08/2/2.6 nM。

纯度: >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
规格 价格/人民币 库存 数量
2MG ¥356 有现货
5MG ¥551 有现货
10MG ¥778 有现货
25MG ¥1345 有现货
50MG ¥2155 有现货
100MG ¥3726 有现货
200MG ¥4844 有现货
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
    Afuresertib hydrochloride
  • 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
    一种有效的、选择性的 ATP 竞争性泛 AKT 抑制剂,对于 AKT1/2/3 的生化 IC50 为 0.08/2/2.6 nM。
  • 产品描述
    A potent, selective, ATP-competitive pan-AKT inhibitor with biochemical IC50 of 0.08/2/2.6 nM for AKT1/2/3; also inhibits PKA (IC50=1.3 nM) and AKT1 E17K mutant (IC50=0.2 nM), selective over PKC, PKG isoforms and p70S6K; orally bioactive.Gastric Cancer Phase 1 Discontinued(In Vitro):Afuresertib (GSK 2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase.Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response. (In Vivo):Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts.
  • 体外实验
    Afuresertib (GSK 2110183) exhibits favorable tumor-suppressive effects on malignant pleural mesothelioma (MPM) cells. Afuresertib significantly increases caspase-3 and caspase-7 activities and apoptotic cell number among ACC-MESO-4 and MSTO-211H cells. Afuresertib strongly arrests the cell cycle in the G1 phase. Western blotting analysis shows that Afuresertib increases the expression of p21WAF1/CIP1 and decreases the phosphorylation of Akt substrates, including GSK-3β and FOXO family proteins. Afuresertib-induced p21 expression promotes G1 phase arrest by inducing FOXO activity. Afuresertib significantly enhances cisplatin-induced cytotoxicity. Afuresertib modulates the expression E2F1 and MYC, which are associated with fibroblast core serum response.
  • 体内实验
    Mice bearing BT474 breast tumor xenografts are dosed orally with either vehicle or GSK2110183 at 10, 30 or 100 mg/kg daily for 21 days which result in 8, 37 and 61% TGI, respectively. Mice tolerated GSK2110183 well, with 1-3% body weight loss reported after 5 days of dosing which recover over the course of the study. Other tumor xenograft models which possess an activation of the Akt pathway are explored to further demonstrate compound efficacy. Mice treated with GSK2110183 at 10, 30 and 100 mg/kg result in 23, 37 and 97% TGI, respectively, of SKOV3 xenografts.
  • 同义词
    GSK 2110183 hydrochloride | GSK2110183 hydrochloride
  • 通路
    PI3K/Akt/mTOR signaling
  • 靶点
    Akt
  • 受体
    Akt
  • 研究领域
    Cancer
  • 适应症
    Gastric Cancer

化学信息

  • CAS Number
    1047645-82-8
  • 分子量
    463.7841
  • 分子式
    C18H18Cl3FN4OS
  • 纯度
    >98% (HPLC)
  • 溶解度
    DMSO: ≥ 52 mg/mL
  • SMILES
    CN1C(=C(C=N1)Cl)C2=C(SC(=C2)C(=O)NC(CC3=CC(=CC=C3)F)CN)Cl.Cl
  • 化学全称
    2-Thiophenecarboxamide, N-[(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl]-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-, hydrochloride (1:1)

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. Dumble M, et al. PLoS One. 2014 Jun 30;9(6):e100880. 2. Spencer A, et al. Blood. 2014 Oct 2;124(14):2190-5. 3. Arceci RJ, et al. Pediatr Blood Cancer. 2017 May;64(5).
产品手册
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