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S84156

K-7174 (dihydrochloride)

源叶(MedMol) 99%
  • 英文名:
  • K-7174 (dihydrochloride)
  • 别名:
  • CAS号:
  • 191089-60-8
  • 分子式:
  • C33H50Cl2N2O6
  • 分子量:
  • 641.6659
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S84156-5mg 99% ¥880.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S84156-10mg 99% ¥1500.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S84156-50mg 99% ¥6400.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 产品描述: K-7174 dihydrochloride is an orally active proteasome and GATA inhibitor. K-7174 dihydrochloride is a cell adhesion inhibitor. K-7174 dihydrochloride induces cell apoptosis. K-7174 dihydrochloride shows antitumor activities, it can be used for the research of cancer
  • 靶点: Proteasome;Apoptosis;mTOR
  • 体外研究:
    K-7174 dihydrochloride (10 μM; 1 h) inhibits the adhesion by VCAM-1 and its ligand[1].K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the VCAM-1 expression with an IC50 value of 14 μM. K-7174 dihydrochloride (1-30 μM; 1 h) dose-dependently suppresses the induction of VCAM-1 mRNA by TNFα with an IC50 value of 9 μM. K-7174 dihydrochloride (10-20 μM; 24 h) dose-dependently rescues Epo production by Hep3B cells. K-7174 dihydrochloride (2.5-30 μM; 24 h) inhibits the binding activity of GATA. K-7174 dihydrochloride (0-25 μM; 72 h) inhibits MM cells growth and induces cell apoptosis. Cell Viability Assay Cell Line: KMS12-BM, U266, and RPMI8226 cell lines Concentration: 0-25 μM Incubation Time: 72 h Result: Inhibited MM cells growth. Apoptosis Analysis Cell Line: KMS12-BM, U266, and RPMI8226 cell lines Concentration: 10 μM Incubation Time: 48 h Result: Significantly increased apoptosis of MM cells with the increasing percentage of annexin-V-positive cells.
  • 体内研究:
    K-7174 dihydrochloride (30 mg/kg; i.p. once daily for 9 days) reverses the decreasing of hemoglobin concentrations and reticulocyte counts by IL-1β or TNF-α[2].K-7174 dihydrochloride (75 mg/kg; i.p. once daily for 14 days) inhibits the tumor growth in vivo. K-7174 dihydrochloride (50 mg/kg; p.o. once daily for 14 days) inhibits the tumor growth in vivo and shows a better effect than intraperitoneal injection. Animal Model: ICR mice with IL-β or TNF-α injection Dosage: 30 mg/kg Administration: Intraperitoneal injection; 30 mg/kg once daily for 9 days Result: Increased erythropoietin (Epo) production, reticulocyte counts, and hemoglobin (Hb) concentrations. Animal Model: NOD/SCID mice with murine xenograft Dosage: 75 mg/kg Administration: Intraperitoneal injection; once daily for 14 days Result: Significantly decreased tumor volume, but showed a significant body weight reduction after 10 days. Animal Model: NOD/SCID mice with murine xenograft Dosage: 50 mg/kg Administration: Oral gavage; once daily for 14 days Result: Showed an anti-myeloma activity. Porved oral administration is more effective than intraperitoneal injection.
  • 参考文献:
    1. Umetani M, et al. A novel cell adhesion inhibitor, K-7174, reduces the endothelial VCAM-1 induction by inflammatory cytokines, acting through the regulation of GATA. Biochem Biophys Res Commun. 2000 Jun 7;272(2):370-4. 2. Imagawa S, et al. A GATA-specific inhibitor (K-7174) rescues anemia induced by IL-1beta, TNF-alpha, or L-NMMA. FASEB J. 2003 Sep;17(12):1742-4. 3. Kikuchi J, et al. The novel orally active proteasome inhibitor K-7174 exerts anti-myeloma activity in vitro and in vivo by down-regulating the expression of class I histone deacetylases. J Biol Chem. 2013 Aug 30;288(35):25593-602.
  • 溶解性: Soluble  in  H2O
  • 保存条件: -20℃
  • 配置溶液浓度参考:
    1mg 5mg 10mg
    1 mM 1.558 ml 7.792 ml 15.584 ml
    5 mM 0.312 ml 1.558 ml 3.117 ml
    10 mM 0.156 ml 0.779 ml 1.558 ml
    50 mM 0.031 ml 0.156 ml 0.312 ml
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