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  2. PI3K/Akt/mTOR Autophagy Apoptosis
  3. PI3K Autophagy Apoptosis
  4. Pictilisib

Pictilisib (GDC-0941) 是有效的 PI3Kα/δ 抑制劑，IC50為 3 nM；對(duì)110β (11倍) 和 p110γ (25倍) 具有適度的選擇性。

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Pictilisib Chemical Structure

Pictilisib Chemical Structure

CAS No. : 957054-30-7

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥735
In-stock
1 mg ￥295
In-stock
5 mg ￥650
In-stock
10 mg ￥850
In-stock
25 mg ￥1379
In-stock
50 mg ￥2000
In-stock
100 mg ￥3200
In-stock
200 mg ￥4500
In-stock
500 mg   詢價(jià)  
1 g   詢價(jià)  

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Customer Review

Other Forms of Pictilisib:

MCE 顧客使用本產(chǎn)品發(fā)表的 50 篇科研文獻(xiàn)

WB
Proliferation Assay

    Pictilisib purchased from MCE. Usage Cited in: Int J Oncol. 2017 Sep;51(3):823-831.  [Abstract]

    Protein levels of BRD4, p-AKT and AKT in GDC-0941 treated NOZ cells after 72 h.

    Pictilisib purchased from MCE. Usage Cited in: Nat Commun. 2016 Feb 2;7:10438.  [Abstract]

    Western blot illustrating the effect of PI3K inhibitors on p21 protein levels in MEFs. Cells are treated for 24 hours with the indicated concentrations of the different drugs.

    Pictilisib purchased from MCE. Usage Cited in: Oncogene. 2016 Jun 9;35(23):2961-70.  [Abstract]

    Western blot analysis of p-AKT(T308), p-AKT(S473) and p-ERK in transplanted NIC+PIK3CAH1047R tumors treated as indicated.

    Pictilisib purchased from MCE. Usage Cited in: Oncotarget. 2016 Aug 16;7(33):53515-53525.  [Abstract]

    PI3KD/V-IN-01 affects autophagy HeLa cells are treated with different concentrations of PI3KD/V-IN-01, VPS34-IN-1, GDC-0941 or CAL-101 for 16 hours before they are fixed and stained for the autophagy marker LC3B.

    Pictilisib purchased from MCE. Usage Cited in: Oncotarget. 2016 May 31;7(22):32641-51.  [Abstract]

    The well-established PI3Kδ specific inhibitor, CAL-101, shows similar effects as PI3KD-IN-015 with an EC50 of 2.3 nM against PI3Kδ and over 1000-fold less potent against the other three isoforms. Determination of CAL-101 inhibitory activities against PI3Kα, β, δ and γ in cellular background.

    Pictilisib purchased from MCE. Usage Cited in: Cancer Res. 2014 Jan 1;74(1):15-23.  [Abstract]

    Differential responses of Pten Lkb1-deficient endometrial tumors to inhibitors targeting PI3K and/or mTOR. Mice bearing transplanted Pten Lkb1-deficient endometrial tumors are treated with indicated drugs for 3 days and sacrificed three hours after their dose on day 3 of treatment; their tumors are isolated and tumor lysates are immunoblotted with the indicated antibodies.

    Pictilisib purchased from MCE. Usage Cited in: Cancer Res. 2014 Jan 1;74(1):15-23.  [Abstract]

    Ectopic expression of LKB1 renders PTEN LKB1-deficient endometrial cancer cells susceptible to PI3K inhibition. Western blot analysis of pS6RP (Ser235/236) and p4EBP1(Ser65) in ETN-1 and HEC108 cells with stable expression of vector or flag- tagged LKB1. Cell lysates were harvested 24 hours after GDC-0941 treatment.

    Pictilisib purchased from MCE. Usage Cited in: Sci Transl Med. 2013 Jul 31;5(196):196ra99.  [Abstract]

    Sensitivity to GDC-0941 in parental MDA453 and T47D and BYL719-resistant MDA453R and T47DR cells. Protein lysates are isolated after 24 hours of treatment with 1 μM GDC-0941 and probed against the indicated proteins.

    Pictilisib purchased from MCE. Usage Cited in: Cancer Discov. 2012 May;2(5):425-33.  [Abstract]

    Effects of KIN-193, GDC-0941, PIK-75 and IC87114 on AKT phosphorylation in PTEN-deficient cell lines as indicated. Representative western blots are shown. Bar graphs represent mean ± SD of western blot quantitations of AKTT308 (n=3).

    Pictilisib purchased from MCE. Usage Cited in: Cell Metab. 2012 Mar 7;15(3):382-94.  [Abstract]

    Effect of the indicated PI3K inhibitors on pre-brown adipocytes. Cultures are treated with the inhibitors at the indicated concentrations (μM) for 4 h. Protein levels (top) and mRNA levels (bottom) of the indicated proteins and genes, respectively, are analyzed. Assays are performed in triplicate cultures. Values represent mean ± sd, and statistical significance is determined by the two-tailed Student’s t-test. *p<0.05, **p<0.01.

    • 生物活性

    • 實(shí)驗(yàn)參考方法

    • 純度 & 產(chǎn)品資料

    • 參考文獻(xiàn)

    生物活性

    Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).

    IC50 & Target[5]

    p110α

    3 nM (IC50)

    p110α-H1047R

    3 nM (IC50)

    p110α-E545K

    3 nM (IC50)

    p110δ

    3 nM (IC50)

    p110β

    33 nM (IC50)

    p110γ

    75 nM (IC50)

    mTOR

    0.58 μM (Ki)

    DNA-PK

    1.23 μM (IC50)

    Autophagy

     

    細(xì)胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A2780 IC50
    0.14 μM
    Compound: 17, GDC-0941
    Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay
    Antiproliferative activity against human A2780 cells with PIK3CA and PTEN mutation after 4 days by alamar blue assay
    		[PMID: 18754654]
    A549 IC50
    1.03 μM
    Compound: GDC-0941
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36599263]
    A549 IC50
    1.2 μM
    Compound: GDC-0941
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 27043268]
    A549 GI50
    1217 nM
    Compound: 2
    Cytotoxicity against ALK-negative human A549 cells harboring wild type PI3KCA and CDKN2A and KRAS mutations assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Cytotoxicity against ALK-negative human A549 cells harboring wild type PI3KCA and CDKN2A and KRAS mutations assessed as cell growth inhibition measured after 72 hrs by MTT assay
    		[PMID: 32184963]
    A549 IC50
    2.28 μM
    Compound: GDC0941
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    		[PMID: 25911625]
    A549 IC50
    2.48 μM
    Compound: GDC-0941
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    A549 IC50
    6.9 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    A549 IC50
    6.99 μM
    Compound: GDC-0941b
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells after 72 hrs by MTT assay
    		[PMID: 27353887]
    Calu-3 IC50
    2.87 μM
    Compound: GDC-0941
    Antiproliferative activity against human Calu3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human Calu3 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    HCC1954 IC50
    1.3 μM
    Compound: GDC0941
    Cytotoxicity against human HCC1954 cells by MTT assay
    Cytotoxicity against human HCC1954 cells by MTT assay
    		[PMID: 28006668]
    HCT-116 IC50
    0.37 μM
    Compound: GDC0941
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    		[PMID: 25911625]
    HeLa IC50
    2.97 μM
    Compound: GDC-0941
    Antiproliferative activity against paclitaxel-resistant human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against paclitaxel-resistant human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36599263]
    HeLa IC50
    3.15 μM
    Compound: GDC-0941
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36599263]
    Hep 3B2 IC50
    2.03 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human Hep3B cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    HepG2 IC50
    1 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HepG2 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    HepG2 IC50
    6.22 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    HT-29 IC50
    0.66 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    HT-29 IC50
    0.86 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 25440879]
    HT-29 IC50
    0.86 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
    		[PMID: 25086238]
    Huh-7 IC50
    1.72 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human HuH-7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    JeKo-1 GI50
    5 μM
    Compound: GDC-0941
    Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human JeKo1 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 30802730]
    K562 IC50
    6.34 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    LNCaP IC50
    0.34 μM
    Compound: 1; GDC-0941
    Antiproliferative activity against PTEN deficient human LNCAP cells after 72 hrs by CCK-8 assay
    Antiproliferative activity against PTEN deficient human LNCAP cells after 72 hrs by CCK-8 assay
    		[PMID: 28409639]
    MCF7 IC50
    0.07 μM
    Compound: GDC-0941b
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    		[PMID: 27353887]
    MCF7 IC50
    0.22 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay
    		[PMID: 29360358]
    MCF7 IC50
    1.09 μM
    Compound: GDC0941
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    		[PMID: 25911625]
    MCF7 IC50
    1.2 μM
    Compound: GDC-0941
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36599263]
    MCF7 IC50
    2 μM
    Compound: GDC0941
    Cytotoxicity against human MCF7 cells by MTT assay
    Cytotoxicity against human MCF7 cells by MTT assay
    		[PMID: 28006668]
    MCF7 GI50
    70.2 nM
    Compound: GDC-0941
    Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay
    Growth inhibition of human MCF7 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay
    		[PMID: 23360348]
    MDA-MB-231 IC50
    > 30 μM
    Compound: GDC0941
    Cytotoxicity against human MDA-MB-231 cells by MTT assay
    Cytotoxicity against human MDA-MB-231 cells by MTT assay
    		[PMID: 28006668]
    MDA-MB-231 IC50
    0.28 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 25440879]
    MDA-MB-231 IC50
    0.28 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
    		[PMID: 25086238]
    MDA-MB-231 GI50
    12 μM
    Compound: GDC-0941
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human MDA-MB-231 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 30802730]
    MDA-MB-231 IC50
    73.82 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    MDA-MB-361 IC50
    0.72 μM
    Compound: 17, GDC-0941
    Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation after 96 hrs by alamar blue assay
    Antiproliferative activity against human MDA-MB-361 cells with PIK3CA E545-K mutation after 96 hrs by alamar blue assay
    		[PMID: 18754654]
    MIA PaCa-2 GI50
    12 μM
    Compound: GDC-0941
    Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human MIAPaCa2 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 30802730]
    MKN-45 IC50
    0.6 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human MKN45 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human MKN45 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 25440879]
    MKN-45 IC50
    0.6 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay
    Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay
    		[PMID: 25086238]
    MM1.S IC50
    0.1 μM
    Compound: GDC-0941
    Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human MM1S cells after 72 hrs by CellTiter-Glo assay
    		[PMID: 30715878]
    MOLM-13 GI50
    0.048 μM
    Compound: 16; GDC-0941c
    Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay
    Growth inhibition of human MOLM13 cells after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 30053721]
    MOLM-14 GI50
    0.21 μM
    Compound: 16; GDC-0941c
    Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay
    Growth inhibition of human MOLM14 cells after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 30053721]
    MOLT-4 IC50
    0.18 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human MOLT-4 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    MV4-11 GI50
    0.88 μM
    Compound: 16; GDC-0941c
    Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay
    Growth inhibition of human MV4-11 cells after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 30053721]
    MV4-11 IC50
    1.46 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay
    		[PMID: 29360358]
    MV4-11 EC50
    10.7 μM
    Compound: Pic; GDC-0941
    Induction of apoptosis in human MV4-11 cells assessed as increase in caspase 3/7 activity measured at 24 hrs in presence of Z-DEVD-R110 or (Z-Asp-Glu-Val-Asp)2-rhodamine110 by fluorescence based microplate reader analysis
    Induction of apoptosis in human MV4-11 cells assessed as increase in caspase 3/7 activity measured at 24 hrs in presence of Z-DEVD-R110 or (Z-Asp-Glu-Val-Asp)2-rhodamine110 by fluorescence based microplate reader analysis
    		[PMID: 29360358]
    MV4-11 EC50
    2.71 μM
    Compound: Pic; GDC-0941
    Induction of cell death in human MV4-11 cells measured at 48 hrs by fluorescence based microplate reader analysis
    Induction of cell death in human MV4-11 cells measured at 48 hrs by fluorescence based microplate reader analysis
    		[PMID: 29360358]
    MV4-11 GI50
    3 μM
    Compound: GDC-0941
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 30802730]
    NALM-6 GI50
    0.15 μM
    Compound: 16; GDC-0941c
    Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay
    Growth inhibition of human NALM6 cells after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 30053721]
    NCI-H1650 IC50
    4.73 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human NCI-H1650 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    NCI-H1975 IC50
    0.27 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human NCI-H1975 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human NCI-H1975 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    NCI-H1975 IC50
    0.703 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    NCI-H1975 IC50
    2.42 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells overexpressing EGFR L858R/T790M mutant assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36599263]
    NCI-H2228 IC50
    1.07 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H2228 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36599263]
    NCI-H226 IC50
    2.9 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human NCI-H226 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human NCI-H226 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    NCI-H226 IC50
    5.91 μM
    Compound: GDC-0941
    Antiproliferative activity against human H226 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human H226 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    NCI-H23 IC50
    0.936 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human NCI-H23 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    NCI-H358 IC50
    1.33 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human NCI-H358 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    NCI-H460 IC50
    0.87 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human H460 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    NCI-H460 IC50
    0.87 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 25440879]
    NCI-H460 IC50
    0.87 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human H460 cells after 72 hrs by MTT assay
    Cytotoxicity against human H460 cells after 72 hrs by MTT assay
    		[PMID: 25086238]
    NCI-H460 IC50
    1.26 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    NCI-H460 IC50
    2.68 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36599263]
    NCI-H522 IC50
    2.14 μM
    Compound: GDC-0941
    Antiproliferative activity against human NCI-H522 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human NCI-H522 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    PC-3 IC50
    0.2 μM
    Compound: GDC-0941b
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    		[PMID: 27353887]
    PC-3 IC50
    0.28 μM
    Compound: 17, GDC-0941
    Antiproliferative activity against PTEN-null human PC3 cells after 96 hrs by alamar blue assay
    Antiproliferative activity against PTEN-null human PC3 cells after 96 hrs by alamar blue assay
    		[PMID: 18754654]
    PC-3 EC50
    0.34 μM
    Compound: 1, GDC-0941
    Antiproliferative activity against human PC3 cells after 3 to 4 days by Cell titer Glo assay
    Antiproliferative activity against human PC3 cells after 3 to 4 days by Cell titer Glo assay
    		[PMID: 21985639]
    PC-3 IC50
    0.39 μM
    Compound: 2, GDC-0941
    Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days
    Antiproliferative activity against human PC3 cells deficient in PTEN in after 3 to 4 days
    		[PMID: 20050669]
    PC-3 IC50
    0.457 μM
    Compound: 1; GDC-0941
    Antiproliferative activity against PTEN deficient human PC3 cells after 72 hrs by CCK-8 assay
    Antiproliferative activity against PTEN deficient human PC3 cells after 72 hrs by CCK-8 assay
    		[PMID: 28409639]
    PC-3 IC50
    0.75 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay
    Antiproliferative activity against human PC-3 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter-Glo luminescent assay
    		[PMID: 29360358]
    PC-3 IC50
    0.8 μM
    Compound: GDC-0941
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay
    		[PMID: 27043268]
    PC-3 IC50
    280 nM
    Compound: 1, GDC-0941
    Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay
    Antiproliferative activity against human PC3 cells after overnight incubation by CellTiter-Glo luminescence assay
    		[PMID: 21981714]
    PC-3 GI50
    3 μM
    Compound: GDC-0941
    Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human PC3 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 30802730]
    PF-382 GI50
    0.14 μM
    Compound: 16; GDC-0941c
    Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay
    Growth inhibition of human PF382 cells after 72 hrs by CellTiter-Glo luminescent assay
    		[PMID: 30053721]
    PLC-PRF-5 IC50
    3.07 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human PLC-PRF-5 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human PLC-PRF-5 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    Raji IC50
    6.5 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human Raji cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    Ramos IC50
    4.86 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human Ramos cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    RAW IC50
    298 nM
    Compound: 37, GDC-0941
    Inhibition of human PI3Kgamma expressed in C5a-stimulated mouse RAW 264.7 cells assessed as inhibition of AKT phosphorylation by ELISA
    Inhibition of human PI3Kgamma expressed in C5a-stimulated mouse RAW 264.7 cells assessed as inhibition of AKT phosphorylation by ELISA
    		[PMID: 22548342]
    Sf9 IC50
    0.003 μM
    Compound: 17, GDC-0941
    Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    Inhibition of human recombinant PI3K p110alpha expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    		[PMID: 18754654]
    Sf9 IC50
    0.003 μM
    Compound: 17, GDC-0941
    Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    Inhibition of human recombinant PI3K p110beta E545-K mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    		[PMID: 18754654]
    Sf9 IC50
    0.003 μM
    Compound: 17, GDC-0941
    Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    Inhibition of human recombinant PI3K p110beta H1047-R mutant expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    		[PMID: 18754654]
    Sf9 IC50
    0.003 μM
    Compound: 17, GDC-0941
    Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    Inhibition of human recombinant PI3K p110delta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    		[PMID: 18754654]
    Sf9 IC50
    0.033 μM
    Compound: 17, GDC-0941
    Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    Inhibition of human recombinant PI3K p110beta expressed in Sf9 cells coexpressing p85alpha by radiometric scintillation proximity assay
    		[PMID: 18754654]
    Sf9 IC50
    17 nM
    Compound: 37, GDC-0941
    Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP
    Inhibition of GST-fused human recombinant PI3Kbeta expressed in baculovirus infected SF9 cells after 1 hr by scintillation proximity assay in presence of [gamma-33P]-ATP
    		[PMID: 23540645]
    Sf9 IC50
    42 nM
    Compound: 37, GDC-0941
    Inhibition of human PI3Kgamma expressed in sf9 cells assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assay
    Inhibition of human PI3Kgamma expressed in sf9 cells assessed as amount of ATP consumed by luciferase-luciferin chemiluminescence assay
    		[PMID: 22548342]
    SGC-7901 IC50
    1.8 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human SGC7901 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human SGC7901 cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    SJRH30 IC50
    0.478 μM
    Compound: GDC-0941
    Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human Rh30 cells assessed as reduction in cell viability after 72 hrs by sulforhodamine B assay
    		[PMID: 33109399]
    SJRH30 IC50
    0.8 μM
    Compound: GDC-0941
    Antiproliferative activity against human Rh30 cells assessed as cell growth inhibition by SRB assay
    Antiproliferative activity against human Rh30 cells assessed as cell growth inhibition by SRB assay
    		[PMID: 32317209]
    SK-BR-3 IC50
    0.9 μM
    Compound: GDC0941
    Cytotoxicity against human SKBR3 cells by MTT assay
    Cytotoxicity against human SKBR3 cells by MTT assay
    		[PMID: 28006668]
    SK-HEP1 IC50
    4.3 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human SK-HEP1 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    SK-MEL19 GI50
    6 μM
    Compound: GDC-0941
    Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human SK-MEL-19 cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 30802730]
    SK-OV-3 IC50
    0.864 μM
    Compound: 1; GDC-0941
    Antiproliferative activity against human SKOV3 cells harboring PIK3CA mutant after 72 hrs by CCK-8 assay
    Antiproliferative activity against human SKOV3 cells harboring PIK3CA mutant after 72 hrs by CCK-8 assay
    		[PMID: 28409639]
    SK-OV-3 GI50
    147.6 nM
    Compound: GDC-0941
    Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay
    Growth inhibition of human SKOV3 cells assessed as cell viability after 96 hrs by Cell Titre Glo assay
    		[PMID: 23360348]
    SU-DHL-6 IC50
    0.03 μM
    Compound: Pic; GDC-0941
    Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    Antiproliferative activity against human SU-DHL-6 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay/CellTiter Glo-luminescent assay
    		[PMID: 29360358]
    T47D IC50
    1.2 μM
    Compound: GDC0941
    Cytotoxicity against human T47D cells by MTT assay
    Cytotoxicity against human T47D cells by MTT assay
    		[PMID: 28006668]
    T47D GI50
    3 μM
    Compound: GDC-0941
    Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human T47D cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 30802730]
    U-87MG ATCC GI50
    0.07 μM
    Compound: 61
    Antiproliferative activity against human U87MG cells after 96 hrs
    Antiproliferative activity against human U87MG cells after 96 hrs
    		[PMID: 30583248]
    U-87MG ATCC IC50
    0.55 μM
    Compound: 1; GDC-0941
    Antiproliferative activity against PTEN deficient human U87MG cells after 72 hrs by CCK-8 assay
    Antiproliferative activity against PTEN deficient human U87MG cells after 72 hrs by CCK-8 assay
    		[PMID: 28409639]
    U-87MG ATCC IC50
    0.95 μM
    Compound: 17, GDC-0941
    Antiproliferative activity against PTEN-null human U87MG cells after 4 days by alamar blue assay
    Antiproliferative activity against PTEN-null human U87MG cells after 4 days by alamar blue assay
    		[PMID: 18754654]
    U-87MG ATCC IC50
    1.24 μM
    Compound: GDC0941
    Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay
    Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay
    		[PMID: 25911625]
    U-87MG ATCC IC50
    3.13 μM
    Compound: GDC-0941
    Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human U-87 MG cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    		[PMID: 36599263]
    U-87MG ATCC GI50
    6 μM
    Compound: GDC-0941
    Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    Antiproliferative activity against human U87MG cells incubated for 72 hrs by CellTiter-Glo luminescence assay
    		[PMID: 30802730]
    U-87MG ATCC IC50
    7.77 μM
    Compound: 1, GDC-0941
    Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay
    		[PMID: 23059545]
    體外研究
    (In Vitro)

    Pictilisib (GDC-0941) 和 RP-56976 比單藥治療可將乳腺癌細(xì)胞系中的腫瘤細(xì)胞活力降低 80% 或更多。GDC-0941 可抑制 Hs578T1.2（PI3Kα 野生型）、MCF7-neo/HER2（PI3Kα 突變型）和 MX-1（PTEN 缺陷型）腫瘤模型中的 Akt 磷酸化和 Akt 信號(hào)傳導(dǎo)的下游靶標(biāo)（如 pPRAS40 和 pS6）。Pictilisib (GDC-0941) 可縮短 RP-56976 誘導(dǎo)的細(xì)胞凋亡前有絲分裂停滯時(shí)間[1]。
    Pictilisib (GDC-0941) 在兩種 ZD1839 耐藥非小細(xì)胞肺癌 (NSCLC) 細(xì)胞系 A549 和 H460 中表現(xiàn)出較高的抗腫瘤活性。 Pictilisib (GDC-0941) 與 U0126 聯(lián)合使用可有效誘導(dǎo)細(xì)胞生長(zhǎng)抑制、G0-G1 停滯和細(xì)胞凋亡。與具有野生型 PIK3CA 的 A549 細(xì)胞相比，具有 PIK3CA 激活突變的 H460 細(xì)胞對(duì) Pictilisib (GDC-0941) 相對(duì)更敏感[3]。
    Pictilisib (GDC-0941) 可降低兩種細(xì)胞系中的 PI3K 通路活性，表現(xiàn)為 pAK 降低。Pictilisib (GDC-0941) 可顯著降低所有細(xì)胞在缺氧/缺氧暴露后在培養(yǎng)基中檢測(cè)到的分泌性 VEGF[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    體內(nèi)研究
    (In Vivo)

    Pictilisib (GDC-0941) (150 mg/kg，口服) 導(dǎo)致 MCF7-neo/HER2 攜帶動(dòng)物模型中的腫瘤停滯。Pictilisib (GDC-0941) 和 RP-56976 在治療期間導(dǎo)致腫瘤消退，從而增強(qiáng)抗腫瘤反應(yīng)[1]。
    經(jīng) Pictilisib (GDC-0941) 治療的小鼠的腫瘤顯示出明顯的非線性收縮，當(dāng) Pictilisib (GDC-0941) 治療停止時(shí)，測(cè)試組小鼠的腫瘤再次生長(zhǎng)[2]。
    Pictilisib (GDC-0941) (25 或 50 mg/kg) 抑制 eGFP-FTC133 腫瘤攜帶小鼠的腫瘤生長(zhǎng)和 PI3K 和 HIF-1 通路活性[4]。

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    513.64

    Formula

    C23H27N7O3S2
    CAS 號(hào)
    性狀

    固體

    顏色

    White to yellow

    運(yùn)輸條件

    Room temperature in continental US; may vary elsewhere.
    儲(chǔ)存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性數(shù)據(jù)
    細(xì)胞實(shí)驗(yàn)： 

    DMSO 中的溶解度 : 100 mg/mL (194.69 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

    配制儲(chǔ)備液
    濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
    1 mM 1.9469 mL 9.7344 mL 19.4689 mL
    5 mM 0.3894 mL 1.9469 mL 3.8938 mL
    查看完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    • 摩爾計(jì)算器

    • 稀釋計(jì)算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    質(zhì)量
    =
    濃度
    ×
    體積
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    濃度 (start)

    C1

    ×
    體積 (start)

    V1

    =
    濃度 (final)

    C2

    ×
    體積 (final)

    V2

    動(dòng)物實(shí)驗(yàn)：

    請(qǐng)根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

    以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
    ——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
    以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

    • 方案 一

      請(qǐng)依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.87 mM); 澄清溶液

      此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

      生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
    • 方案 二

      請(qǐng)依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (4.87 mM); 懸濁液; 超聲助溶

      此方案可獲得 2.5 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。

      以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

      2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。

    以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比； 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶。

    • 方案 一

      請(qǐng)依序添加每種溶劑： 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

      Solubility: 5 mg/mL (9.73 mM); Suspened solution; 超聲助溶

    動(dòng)物溶解方案計(jì)算器
    請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

    給藥劑量

    mg/kg

    動(dòng)物的平均體重

    g

    每只動(dòng)物的給藥體積

    μL

    動(dòng)物數(shù)量

    只
    由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
    請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
    方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購(gòu)。 ，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。
    計(jì)算結(jié)果
    工作液所需濃度 : mg/mL
    儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
    您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。
    動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
    連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。
    請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
    純度 & 產(chǎn)品資料

    純度: 99.80%

    參考文獻(xiàn)
    Cell Assay
    [1]

    Cells are treated at EC50?concentrations of Pictilisib (GDC-0941), RP-56976, or both for 4 or 24 hours and lysed in 1×Cell Extraction Buffer supplemented with protease inhibitors and Phosphatase Inhibitor Cocktails 1 and 2. Protein concentrations are determined using the Pierce BCA Protein Assay Kit. For immunoblots, equal amounts of protein are separated by electrophoresis through NuPAGE Bis-Tris 10% gradient gels, transferred onto polyvinylidene difluoride membranes using the Criterion system, and probed with monospecific primary antibodies. Specific antigen-antibody interactions are detected with IRDye 680 or IRDye 800 infrared secondary antibodies using a LI-COR imaging system.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Female?nu/nu?mice are inoculated subcutaneously with MCF7-neo/HER2 or MX-1 breast cancer cells. When tumors reach a mean volume of 200 to 250 mm3, animals are size-matched and distributed into groups consisting of 10 animals per group. RP-56976 formulated in 3% EtOH, 97% saline is administered intravenously once weekly. Pictilisib (GDC-0941), formulated in MCT (0.5% methylcellulose, 0.2% Tween-80) is dosed orally and daily. MAXF1162 is an HER2+/ER+/PR+ patient-derived breast cancer tumor xenograft model established by directly implanting tumors subcutaneously from patient to NMRI?nu/nu?mice. Tumor volume is calculated. Tumor sizes are recorded twice weekly over the course of a study.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    參考文獻(xiàn)

    完整儲(chǔ)備液配制表

    * 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
    儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

    可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9469 mL 9.7344 mL 19.4689 mL 48.6722 mL
    5 mM 0.3894 mL 1.9469 mL 3.8938 mL 9.7344 mL
    10 mM 0.1947 mL 0.9734 mL 1.9469 mL 4.8672 mL
    15 mM 0.1298 mL 0.6490 mL 1.2979 mL 3.2448 mL
    20 mM 0.0973 mL 0.4867 mL 0.9734 mL 2.4336 mL
    25 mM 0.0779 mL 0.3894 mL 0.7788 mL 1.9469 mL
    30 mM 0.0649 mL 0.3245 mL 0.6490 mL 1.6224 mL
    40 mM 0.0487 mL 0.2434 mL 0.4867 mL 1.2168 mL
    50 mM 0.0389 mL 0.1947 mL 0.3894 mL 0.9734 mL
    60 mM 0.0324 mL 0.1622 mL 0.3245 mL 0.8112 mL
    80 mM 0.0243 mL 0.1217 mL 0.2434 mL 0.6084 mL
    100 mM 0.0195 mL 0.0973 mL 0.1947 mL 0.4867 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    產(chǎn)品名稱：
    Pictilisib
    目錄號(hào)：
    HY-50094
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