CCT137690

CCT137690

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  • ¥600 - 3200
  • 上海莼试
  • CS-01Y65462
  • 国产
  • 2025年07月11日
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    • 详细信息
    • 技术资料
    • 库存

      59

    • 英文名

      CCT137690

    • CAS号

      1095382-05-0

    • 供应商

      上海莼试

    • 保存条件

      Store at -20°C

    • 规格

      10mM (in 1mL DMSO) 10mg 50mg

    产品描述:
    分子式:C26H31BrN8O

    CCT137690
    分子量:551.48
    溶解度:≥ 6.9 mg/mL in DMSO
    储存条件:Store at -20°C
    General tips:For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the   ultrasonic bath for a while.
    Shipping Condition:Evaluation sample solution : ship with blue ice All other available size: ship with RT , or   blue ice upon request                                      
    Aurora kinase is a family of serine/threonine kinases including Aurora-A, B and C. They play important roles in the regulation of mitosis and take participate in the causation and progression of various tumors including ovarian, breast, glioma and colon. Therefore aurora kinases have been regarded as anti-cancer targets in cancer chemotherapeutics.CCT137690 is a selective small-molecular inhibitor of aurora kinases and showed anti-tumor activities both in vitro and in vivo. Besides that, CCT137690 exerted good stability in mouse liver microsomes [1].When tested toward a panel of 94 kinases, CCT137690inhibited 80% activities of VEG-FR, Aurora-A, and FGF-R1 at concentration of 1 μM. It suppressed the phosphorylation of histone H3 caused by Aurora-B. The IC50 values of CCT137690 against Aurora-B and C were 25 and 19 nM, respectively. CCT137690 showed potent anti-proliferation effects on various kinds of tumors such as A2780 ovarian tumor cell (IC50 value of 140 nM), SW620 (IC50 value of 300 nM) and SW48 colon carcinoma (IC50 value of 157 nM). It caused cell cycle perturbations. In addition, CCT137690 was found to have synergistic effects with radiotherapy. It increased the sensitivity of SW620 cells to radiation. The combination treatment resulted in much more cell death through apoptosis [1 and 2].In mice model bearing SW620 xenografts, administration of CCT137690slowed the growth of tumors without orved toxicity. The ratio of treat/control group based on tumor weight was 37% at the dose of 75 mg/kg. Besides that, CCT137690 was found to significantly reduced neuroblastoma tumor mass in MYCN transgenic mice, which meant CCT137690 could benefit patients with MYCN-amplified neuroblastoma [1 and 3].References:[1] Bavetsias V, Large J M, Sun C, et al.  Imidazo [4, 5-b] pyridine derivatives as inhibitors of Aurora kinases: lead optimization studies toward the identification of an orally bioavailable preclinical development candidate. Journal of medicinal chemistry, 2010, 53(14): 5213-5228.[2] Wu X, Liu W, Cao Q, et al.  Inhibition of Aurora B by CCT137690 sensitizes colorectal cells to radiotherapy. J ExpClin Cancer Res, 2014, 33(1): 13.[3] Faisal A, Vaughan L, Bavetsias V, et al.  The aurora kinase inhibitor CCT137690 downregulates MYCN and sensitizes MYCN-amplified neuroblastoma in vivo. Molecular cancer therapeutics, 2011, 10(11): 2115-2123.
    商品属性:
    货号CS-01Y65462规格10mM (in 1mL DMSO) 10mg 50mg
    CAS号1095382-05-0分子量551.48
    含量>98.00%别名 
    分子式C26H31BrN8O化学名3-[[4-[6-bromo-2-[4-(4-methylpiperazin-1-yl)phenyl]-1H-imidazo[4,5-b]pyridin-7-yl]piperazin-1-yl]methyl]-5-methyl-1,2-oxazole
    产地国产用途仅供科研研究实验
    注意事项:
    抗逆滴加序列
    每次向板内滴加抗原时,移液器滴头要与平面45度悬空,不要触碰到孔内的液体,由后向前依次滴加(即浓度由低往高滴加)。
    抗感染反应期
    抗原抗体在室温20~25℃下,必须反应30min以上,若环境温度低于室温,可将微量反应板置于恒温培养箱中,使二者充分反应。
    旅游温度
    磷酸盐缓冲液的pH值要在高压灭菌后进行滴定,往往在高压后pH值会有所改变,所以高压后再调一次pH值更为准确。磷酸盐缓冲液一经使用保存期不要超过3周。当pH<5.8时,红细胞会产生自凝现象;当pH>7.8时,图形洗脱加快,易造成肉眼观察产生误差;p H=7.2时,红细胞沉降最充分,图形最清晰。
    当滴注 1%红细胞悬液时,应经常摇晃红细胞悬液,使红细胞均匀地分布在磷酸缓冲液中,以防止红细胞下降。
    反应时间及温度
    加入鸡红血球之后,反应板在室温(20~25℃)静置30~40min,对照孔血球下沉于孔底,即可判定结果。若室温达不到实验要求,需相应调整反应时间。当环境温度低于4℃时,红细胞发生自凝;高于37℃时,会发生反应物分离和红细胞溶血。
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    使用方法:
    1.本蛋白酶抑制剂混合物为100×的储存液,使用时按照1:100的比例加入到裂解液中(例如,1ml裂解液中加入10μl蛋白酶抑制剂混合物),混匀后即可使用。根据需要,0.5M的EDTA也按照1:100的比例加入到裂解液中(如用于检测金属蛋白酶活性,则不宜添加EDTA)。含有蛋白酶抑制剂混合物的裂解液宜现用现配,不宜配制后冻存待后续使用。
    2. 待所需的抑制剂添加完毕混匀后,就可以开始进行哺乳动物组织的裂解和蛋白提取。

     

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