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Adavosertib AZD1775; MK-1775

Adavosertib (AZD-1775; MK-1775) 是一种有效的 Wee1 抑制剂,IC50 值为 5.2 nM。

  • 货号:
    TK0250
  • 规格:
    1mg
    2mg
    5mg
    10mg
  • 价格:
    0.00

产品参数

CAS No.955365-80-7
生物活性Adavosertib (AZD-1775; MK-1775) is a potent Wee1 inhibitor with an IC50 of 5.2 nM.
分子式C27H32N8O2
分子量500.6
运输条件Room temperature in continental US; may vary elsewhere.
储存条件 Powder -20°C 3 years
溶解性数据DMSO : 125 mg/mL (249.70 mM; Need ultrasonic)
体内研究In vivo, Adavosertib (MK-1775) potentiates the anti-tumor efficacy of 5-FU at tolerable doses. Adavosertib (MK-1775) (60 mg/kg twice daily, p.o.) enhances H1299 xenograft tumor response to fractionated radiotherapy. Adavosertib (MK-1775) (30 mg/kg. p.o.) regresses tumor growth in PANC198, PANC215 and PANC185 as compared to GEM treated mice.
体外研究Adavosertib (MK-1775) enhances the cytotoxic effects of 5-FU in p53-deficient human colon cancer cells. Adavosertib (MK-1775) inhibits CDC2 Y15 phosphorylation in cells, abrogates DNA damaged checkpoints induced by 5-FU treatment, and causes premature entry of mitosis determined by induction of Histone H3 phosphorylation. Adavosertib (MK-1775) abrogates the radiation-induced G2 block in p53-defective cells but not in p53 wild-type lines. The combination of NSC 613327 with Adavosertib (MK-1775) produces robust anti-tumor activity and remarkably enhances tumor regression response (4.01 fold) compared to NSC 613327 treatment in p53-deficient tumors.
文献•Sci Transl Med. 2018 Jul 18;10(450). pii: eaaq1093. •J Hematol Oncol. 2018 Aug 1;11(1):99. •Sci Adv. 2021 Apr 30;7(18):eabd4676. •Cancer Res. 2017 Sep 1;77(17):4663-4672. •Blood Cancer J. 2021 Jul 31;11(7):137. •Clin Cancer Res. 2020 Jul 1;26(13):3431-3442. •Oncogene. 2021 Jan;40(3):564-577. •Cell Rep. 2020 Jul 7;32(1):107858. •Cancers (Basel). 2021 Aug 20;13(16):4200. •Cancers. 2019 Oct 25;11(11):1654. •Int J Mol Sci. 2021, 22(7), 3664. •Mol Cancer Res. 2020 Jan;18(1):91-104. •Reprod Biol Endocrinol. 2021 Oct 22;19(1):161. •Sci Rep. 2021 Feb 4;11(1):3176. •Sci Rep. 2019 Apr 23;9(1):6458. •PLoS One. 2019 Jan 10;14(1):e0209224. •bioRxiv. January 12, 2022. •Universitätsklinikum Ulm. UKU. Institut für Pathologie. 2020 Nov. •Master of Science in Engineering-Biotechnology. 2020 Jul. •Department of medicine. Georg-August-Universität Göttingen. 2019 Apr. •University of Bologna. Scienze biomediche. 2016 Apr 22. •Scienze biomediche. University of Bologna. 2016 Apr. •Harvard Medical School LINCS LIBRARY
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