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CAL-101

艾代拉里斯,Idelalisib,GS-1101

CAL-101 (Idelalisib, GS-1101) 是p110δ选择性抑制剂，IC50为2.5 nM，比对p110α/β/γ的抑制性高40到300倍，比对C2β，hVPS34，DNA-PK和mTOR的抑制。

目录号
EY0964
EY0964
EY0964
EY0964
纯度
98.90%
98.90%
98.90%
98.90%
规格
1 mg
5 mg
10 mg
50 mg
原价
160
300
500
1200
售价
160
300
500
1200
库存
现货
现货
现货
现货
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  • 生物活性

    CAL-101 (Idelalisib, GS-1101) is an oral bioactive, selective inhibitor of PI3K p110δ with IC50 of 2.5 nM. CAL-101 displays more than 40- to 300-fold selectivity over p110α, -β, -γ, and 400- to 4000-fold higher selectivity for C2β, hVPS34, DNA-PK and mTOR. CAL-101 inhibits the production of the second messenger phosphatedylinositol-3,4,5-trisphosphate (PIP3), blocking the activation of the PI3K signaling pathway and thus inducing tumor cell apoptosis.

  • 体外研究

  • 体内研究

    30% PEG 400 (dissolve first)+0.5% Tween 80+5% Propylene glycol

  • 激酶实验

  • 细胞实验

    0.01-100 μM

  • 动物实验

  • 不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）

    动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数


    例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。

  • 参考文献

    [1] Lannutti BJ, et al. Blood, 2011, 117(2), 591-594.
    [2] Herman, S.E. et al. 2010. Blood. 116(12): 2078-2088.
    [3] Xu, H. et al. 2013. Nature. 496(7446): 523-527.
    [4] Chiron, D. et al. 2014. Cancer Discov. 4(9): 1022-1035.
    [5] Boucrot, E. et al. 2015. Nature. 517(7535): 460-465.
    [6] Mounayar, M. et al. 2015. Stem Cells. 33(6): 1892-1901.

    分子式
    C22H18FN7O    		 分子量
    415.42    		 CAS号
    870281-82-6    		 储存方式
    ﹣20 ℃冷藏长期储存。冰袋运输
    溶剂（常温）
    		 DMSO
    83 mg/mL    		 Water
    <1 mg/mL    		 Ethanol
    35 mg/mL

    体内溶解度

  • Clinical Trial Information ( data from http://clinicaltrials.gov )

    NCT Number Conditions Interventions Sponsor/Collaborators Phases Start Date Last Updated
    NCT00836914 Allergic Rhinitis Drug: CAL-101|Drug: Placebo Gilead Sciences Phase 1 2009-02-01 2013-01-04
    NCT00710528 Chronic Lymphocytic Leukemia (CLL)|Lymphoma, Non-Hodgkin (NHL)|Acute Myeloid Leukemia (AML)|Multiple Myeloma (MM) Drug: CAL-101 Gilead Sciences Phase 1 2008-06-01 2012-08-29
    NCT02445131 Chronic Lymphocytic Leucemia Drug: Bendamustine|Drug: GA101|Drug: CAL-101 German CLL Study Group Phase 2 2015-05-01 2016-09-23
    NCT01659047 Chronic Lymphocytic Leukemia Drug: GS-1101 Gilead Sciences Phase 2 2012-08-01 2012-09-06
    NCT01090414 Chronic Lymphocytic Leukemia|Lymphoma, Non-Hodgkin Drug: Idelalisib Gilead Sciences Phase 1 2010-03-01 2016-11-18
    NCT01393106 Hodgkin Lymphoma Drug: Idelalisib Gilead Sciences Phase 2 2011-09-01 2015-11-20
    NCT01306643 Indolent Non-Hodgkin's Lymphoma|Follicular Lymphoma|Small Lymphocytic Lymphoma|Marginal Zone Lymphoma Drug: Idelalisib Gilead Sciences Phase 1|Phase 2 2011-02-01 2016-10-27
    NCT02536300 Follicular Lymphoma Drug: Idelalisib Gilead Sciences Phase 3 2016-01-14 2017-03-21
    NCT01282424 Follicular Lymphoma|Small Lymphocytic Lymphoma|Lymphoplasmacytic Lymphoma|Marginal Zone Lymphoma Drug: Idelalisib Gilead Sciences Phase 2 2011-05-01 2016-09-15
    NCT02135133 Chronic Lymphocytic Leukemia|Small Lymphocytic Lymphoma Drug: Idelalisib|Drug: Ofatumumab Dana-Farber Cancer Institute|Gilead Sciences|GlaxoSmithKline Phase 2 2014-06-01 2016-10-25
    NCT01659021 Chronic Lymphocytic Leukemia Drug: Idelalisib|Drug: Ofatumumab Gilead Sciences Phase 3 2012-12-01 2016-10-27
    NCT02739360 Lymphoid Malignancies Drug: Idelalisib Gilead Sciences Phase 4 2016-05-01 2016-07-18
    NCT02242045 Chronic Lymphocytic Leukemia|Indolent Non-Hodgkin Lymphoma|Follicular Lymphoma|Small Lymphocytic Lymphoma|Lymphoplasmacytic Lymphoma (With or Without Waldenstrom Macroglobulinemia)|Marginal Zone Lymphoma Drug: Idelalisib|Biological: Ofatumumab Gilead Sciences Phase 1 2014-10-01 2017-02-09
    NCT01539291 Chronic Lymphocytic Leukemia Drug: Idelalisib Gilead Sciences Phase 3 2012-10-01 2016-12-13
    NCT02439138 Waldenstrom's Macroglobulinemia Drug: GS-1101 Dana-Farber Cancer Institute|Gilead Sciences Phase 2 2015-10-01 2016-11-14
    NCT02436135 Myelofibrosis Drug: Idelalisib|Drug: Ruxolitinib Gilead Sciences Phase 1 2015-06-01 2016-10-21
    NCT02590588 Amyloidosis Drug: Idelalisib John Mark Sloan|Gilead Sciences|Boston Medical Center Phase 2 2016-01-01 2016-07-20
    NCT01203930 Chronic Lymphocytic Leukemia (CLL)|Small Lymphocytic Lymphoma (SLL) Drug: Idelalisib|Drug: Rituximab Gilead Sciences Phase 2 2010-10-01 2016-06-01
    NCT02468557 Pancreatic Ductal Adenocarcinoma Drug: Idelalisib|Drug: Nab-paclitaxel|Drug: mFOLFOX6 Gilead Sciences Phase 1 2015-07-01 2016-05-03
    NCT01732913 Indolent Non-Hodgkin's Lymphomas Drug: Idelalisib|Drug: Rituximab|Drug: Placebo to match idelalisib Gilead Sciences Phase 3 2013-01-01 2016-05-25
    NCT01539512 Chronic Lymphocytic Leukemia Drug: Idelalisib|Drug: Rituximab|Drug: Placebo to match idelalisib Gilead Sciences Phase 3 2012-04-01 2015-04-20
    NCT02044822 B-cell Chronic Lymphocytic Leukemia (CLL) With 17p Deletion Drug: Idelalisib|Drug: Rituximab Gilead Sciences Phase 2 2014-08-01 2016-05-19
    NCT01796470 Chronic Lymphocytic Leukemia|Mantle Cell Lymphoma|Diffuse Large B-cell Lymphoma|Indolent Non-Hodgkin's Lymphoma Drug: Entospletinib|Drug: Idelalisib Gilead Sciences Phase 2 2013-06-01 2017-01-20

    注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。

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