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  • 艾代拉里斯

    Idelalisib (CAL-101)

    艾代拉里斯
    产品编号 CFN60050
    CAS编号 870281-82-6
    分子式 = 分子量 C22H18FN7O = 415.42
    产品纯度 >=98%
    物理属性 Powder
    化合物类型 Alkaloids
    植物来源
    ChemFaces的产品在影响因子大于5的优秀和顶级科学期刊中被引用
    提供自定义包装
    产品名称 产品编号 CAS编号 包装 QQ客服
    艾代拉里斯 CFN60050 870281-82-6 1mg QQ客服:1457312923
    艾代拉里斯 CFN60050 870281-82-6 5mg QQ客服:1457312923
    艾代拉里斯 CFN60050 870281-82-6 10mg QQ客服:1457312923
    艾代拉里斯 CFN60050 870281-82-6 20mg QQ客服:1457312923
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    ChemFaces的产品在许多优秀和顶级科学期刊中被引用

    Cell. 2018 Jan 11;172(1-2):249-261.e12.
    doi: 10.1016/j.cell.2017.12.019.
    IF=36.216(2019)

    PMID: 29328914

    Cell Metab. 2020 Mar 3;31(3):534-548.e5.
    doi: 10.1016/j.cmet.2020.01.002.
    IF=22.415(2019)

    PMID: 32004475

    Mol Cell. 2017 Nov 16;68(4):673-685.e6.
    doi: 10.1016/j.molcel.2017.10.022.
    IF=14.548(2019)

    PMID: 29149595

    ACS Nano. 2018 Apr 24;12(4): 3385-3396.
    doi: 10.1021/acsnano.7b08969.
    IF=13.903(2019)

    PMID: 29553709

    Nature Plants. 2016 Dec 22;3: 16206.
    doi: 10.1038/nplants.2016.205.
    IF=13.297(2019)

    PMID: 28005066

    Sci Adv. 2018 Oct 24;4(10): eaat6994.
    doi: 10.1126/sciadv.aat6994.
    IF=12.804(2019)

    PMID: 30417089
    我们的产品现已经出口到下面的研究机构与大学,并且还在增涨
  • FORTH-IMBB (Greece)
  • Seoul National University of Science and Technology (Korea)
  • University of Maryland (USA)
  • University of Auckland (New Zealand)
  • University of Helsinki (Finland)
  • Mendel University in Brno (Czech Republic)
  • Celltrion Chemical Research Institute (Korea)
  • Srinakharinwirot University (Thailand)
  • Warszawski Uniwersytet Medyczny (Poland)
  • Institute of Bioorganic Chemistry Polish Academy of Sciences (Poland)
  • National Hellenic Research Foundation (Greece)
  • University of Hull (United Kingdom)
  • Mahidol University (Thailand)
  • Monash University (Australia)
  • More...
  • 国外学术期刊发表的引用ChemFaces产品的部分文献
  • Asian Journal of Chemistry2014, 26(22):7811-7816
  • Anal Chim Acta.2021, 1180:338874.
  • Oncol Rep.2019, 41(4):2453-2463
  • The Japan Society for Analytical Chemistry2018, 67(4):201-206
  • PLoS One.2015, 10(5):e0127060
  • New Zealand J. Forestry Sci.2014, 44:17
  • Journal of Ginseng Research2019, 10.1016
  • Molecules.2022, 27(7):2360.
  • Molecules.2023, 28(13):4907.
  • Int J Mol Sci.2021, 22(19):10405.
  • Phytomedicine.2022, 99:153997.
  • Rev. Chim.2020, 71(3),558-564
  • Sci Rep.2019, 9(1):4646
  • Asian J Beauty Cosmetol2020, 18(3): 265-272.
  • Food Funct.2022, doi: 10.1039
  • Sci Rep.2021, 11(1):11936.
  • Chem Res Toxicol. 2022, acs.chemrestox.2c00049.
  • Mol Pharmacol.2021, 99(2):163-174.
  • Molecules.2021, 26(16):4722.
  • J Nat Med.2020, 74(3):550-560.
  • Inflammation.2020, 43(5):1716-1728.
  • Tokyo Pharmaceutical University2020, 500001431953.
  • Molecules.2022, 27(22):7887.
  • ...
  • 生物活性
    Description: Idelalisib (CAL-101, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM in cell-free assays; shown to have 40- to 300-fold greater selectivity for p110δ than p110α/β/γ, and 400- to 4000-fold more selectivity to p110δ than C2β, hVPS34, DNA-PK and mTOR. Idelalisib also stimulates autophagy.
    Targets: p110δ | Autophagy
    In vitro:
    Blood,2011 Jan 13;117(2):591-4.
    CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability.[Pubmed: 20959606]
    Phosphatidylinositol-3-kinase p110δ serves as a central integration point for signaling from cell surface receptors known to promote malignant B-cell proliferation and survival. This provides a rationale for the development of small molecule inhibitors that selectively target p110δ as a treatment approach for patients with B-cell malignancies.
    METHODS AND RESULTS:
    We thus identified 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one (CAL-101), a highly selective and potent p110δ small molecule inhibitor (half-maximal effective concentration [EC(50)] = 8nM). Using tumor cell lines and primary patient samples representing multiple B-cell malignancies, we have demonstrated that constitutive phosphatidylinositol-3-kinase pathway activation is p110δ-dependent. CAL-101 blocked constitutive phosphatidylinositol-3-kinase signaling, resulting in decreased phosphorylation of Akt and other downstream effectors, an increase in poly(ADP-ribose) polymerase and caspase cleavage and an induction of apoptosis.
    CONCLUSIONS:
    These effects have been observed across a broad range of immature and mature B-cell malignancies, thereby providing a rationale for the ongoing clinical evaluation of CAL-101.
    Blood,2012 Feb 23;119(8):1897-900.
    PI3Kδ inhibitor, GS-1101 (CAL-101), attenuates pathway signaling, induces apoptosis, and overcomes signals from the microenvironment in cellular models of Hodgkin lymphoma.[Pubmed: 22210877]
    GS-1101 (CAL-101) is an oral PI3Kδ-specific inhibitor that has shown preclinical and clinical activity in non-Hodgkin lymphoma and chronic lymphocytic leukemia.
    METHODS AND RESULTS:
    To investigate the potential role of PI3Kδ in Hodgkin lymphoma (HL), we screened 5 HL cell lines and primary samples from patients with HL for PI3Kδ isoform expression and constitutive PI3K pathway activation. Inhibition of PI3Kδ by GS-1101 resulted in the inhibition of Akt phosphorylation. Cocultures with stroma cells induced Akt activation in HL cells, and this effect was blocked by GS-1101. Conversely, production of the stroma-stimulating chemokine, CCL5, by HL cells was reduced by GS-1101. GS-1101 also induced dose-dependent apoptosis of HL cells at 48 hours. Reductions in cell viability and apoptosis were enhanced when combining GS-1101 with the mTOR inhibitor everolimus.
    CONCLUSIONS:
    Our findings suggest that excessive PI3Kδ activity is characteristic in HL and support clinical evaluation of GS-1101, alone and in combination, as targeted therapy for HL.
    制备储备液(仅供参考)
    1 mg 5 mg 10 mg 20 mg 25 mg
    1 mM 2.4072 mL 12.036 mL 24.072 mL 48.144 mL 60.1801 mL
    5 mM 0.4814 mL 2.4072 mL 4.8144 mL 9.6288 mL 12.036 mL
    10 mM 0.2407 mL 1.2036 mL 2.4072 mL 4.8144 mL 6.018 mL
    50 mM 0.0481 mL 0.2407 mL 0.4814 mL 0.9629 mL 1.2036 mL
    100 mM 0.0241 mL 0.1204 mL 0.2407 mL 0.4814 mL 0.6018 mL
    * Note: If you are in the process of experiment, it's need to make the dilution ratios of the samples. The dilution data of the sheet for your reference. Normally, it's can get a better solubility within lower of Concentrations.
    部分图片展示
    产品名称 产品编号 CAS编号 分子式 = 分子量 位单 联系QQ
    Sanshodiol; Sanshodiol CFN96282 54854-91-0 C20H22O6 = 358.4 5mg QQ客服:2159513211
    二乙酸哥纳香二醇酯; Goniodiol diacetate CFN96047 136778-40-0 C17H18O6 = 318.3 5mg QQ客服:3257982914
    酸浆苦味D; Physalin D CFN92939 54980-22-2 C28H32O11 = 544.55 5mg QQ客服:1413575084
    芦西定 3-O-葡萄糖苷; Lucidin 3-O-glucoside CFN91032 22255-29-4 C21H20O10 = 432.38 5mg QQ客服:1413575084

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