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S81536

Danusertib (PHA-739358)

源葉(MedMol) 99%
  • 英文名:
  • Danusertib (PHA-739358)
  • 別名:
  • PHA739358;達(dá)魯舍替;N-[5-((2R)-2-甲氧基-2-苯基乙?;?-1,4,5,6-四氫吡咯并[3,4-c]吡唑-3-基]-4-(4-甲基哌嗪-1-基)苯甲酰胺
  • CAS號(hào):
  • 827318-97-8
  • 分子式:
  • C26H30N6O3
  • 分子量:
  • 474.55
  • 核磁/質(zhì)譜:
品牌貨號(hào)產(chǎn)品規(guī)格價(jià)格(RMB) 庫(kù)存(上海) 北京 武漢 南京 數(shù)量計(jì)量單位 加入購(gòu)物車(chē)...
源葉(MedMol) S81536-2mg 99% ¥552.50元 5 - - - EA 加入購(gòu)物車(chē)
源葉(MedMol) S81536-5mg 99% ¥765.00元 6 - - - EA 加入購(gòu)物車(chē)
源葉(MedMol) S81536-10mg 99% ¥1390.00元 5 - - - EA 加入購(gòu)物車(chē)
源葉(MedMol) S81536-25mg 99% ¥2750.00元 6 - - - EA 加入購(gòu)物車(chē)
源葉(MedMol) S81536-50mg 99% ¥4100.00元 預(yù)計(jì)交期:2-3天 - - - EA 加入購(gòu)物車(chē)
源葉(MedMol) S81536-100mg 99% ¥5800.00元 預(yù)計(jì)交期:2-3天 - - - EA 加入購(gòu)物車(chē)
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產(chǎn)品介紹

參考文獻(xiàn)

質(zhì)檢證書(shū)(COA)

摩爾濃度計(jì)算器

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  • 提示:詳情請(qǐng)下載說(shuō)明書(shū)。
  • 產(chǎn)品描述: Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.
  • 靶點(diǎn): Aurora A:13 nM (IC50);Aurora B:79 nM (IC50);Aurora C:61 nM (IC50);FGFR;?Trkreceptor;?c-RET;?Bcr-Abl;?AuroraKinase;?Autophagy
  • 體內(nèi)研究:
    PHA-739358 (15 mg/kg twice a day, i.p.) and IM are well tolerated, and significantly inhibit proliferation of K562 cells andvirtually suppressed tumor growth during the 10-day treatment period. In a subcutaneous murine xenograft model, danusertibsertib (2×15 mg/kg/d, i.p.) significantly reduces tumor growth in vivo compared with controls or mice treated with streptozotocine/5-fluorouracil
  • 參考文獻(xiàn):
    1. Zi D, et al. Danusertib Induces Apoptosis, Cell Cycle Arrest, and Autophagy but Inhibits Epithelial to Mesenchymal Transition Involving PI3K/Akt/mTOR Signaling Pathway in Human Ovarian Cancer Cells. Int J Mol Sci. 2015 Nov 13;16(11):27228-51. 2. Gontarewicz A, et al. Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I. Blood. 2008 Apr 15;111(8):4355-64. 3. Fraedrich K, et al. Targeting Aurora Kinases with Danusertib (PHA-739358) Inhibits Growth of Liver Metastases from Gastroenteropancreatic Neuroendocrine Tumors in an Orthotopic Xenograft Model. Clin Cancer Res. 2012 Sep 1;18(17):4621-32. Epub 2012 Jul 2.
  • 溶解性: DMSO  :  50  mg/mL  (105.36  mM;  Need  ultrasonic)
  • 保存條件: -20℃
  • 配置溶液濃度參考:
    1mg 5mg 10mg
    1 mM 2.107 ml 10.536 ml 21.073 ml
    5 mM 0.421 ml 2.107 ml 4.215 ml
    10 mM 0.211 ml 1.054 ml 2.107 ml
    50 mM 0.042 ml 0.211 ml 0.421 ml
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