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

Pictilisib (Synonyms: GDC-0941)

目录号: HY-50094 纯度: 99.62%
产品使用指南

Pictilisib (GDC-0941) 是有效的 PI3Kα/δ 抑制剂,IC50为 3 nM;对110β (11倍) 和 p110γ (25倍) 具有适度的选择性。

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Pictilisib Chemical Structure

Pictilisib Chemical Structure

CAS No. : 957054-30-7

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Size Price Stock Quantity
10 mM * 1 mL in DMSO ¥735 In-stock
5 mg ¥650 In-stock
10 mg ¥850 In-stock
50 mg ¥2000 In-stock
100 mg ¥3200 In-stock
200 mg ¥4500 In-stock
500 mg   Get quote  
1 g   Get quote  

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Customer Review

Other Forms of Pictilisib:

Top Publications Citing Use of Products

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

    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.

    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.

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

    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 Res. 2014 Jan 1;74(1):15-23.

    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.

    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: Oncogene. 2016 Jun 9;35(23):2961-70.

    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: Nat Commun. 2016 Feb 2;7:10438.

    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: Oncotarget. 2016 May 31;7(22):32641-51.

    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: Oncotarget. 2016 Aug 16;7(33):53515-53525.

    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: Int J Oncol. 2017 Sep;51(3):823-831.

    Protein levels of BRD4, p-AKT and AKT in GDC-0941 treated NOZ cells after 72 h.
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    • 实验参考方法

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    • 参考文献

    Description

    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)

    p110β

    33 nM (IC50)

    p110δ

    3 nM (IC50)

    p110γ

    75 nM (IC50)

    p110α-H1047R

    3 nM (IC50)

    p110α-E545K

    3 nM (IC50)

    DNA-PK

    1.23 μM (IC50)

    mTOR

    0.58 μM (Ki)

    Autophagy

     

    In Vitro

    Pictilisib (GDC-0941) and RP-56976 reduce tumor cell viability by 80% or greater in the breast cancer cell lines than single-agent treatment. GDC-0941 inhibits Akt phosphorylation and downstream targets of Akt signaling such as pPRAS40 and pS6 in Hs578T1.2 (PI3Kα wild-type), MCF7-neo/HER2 (PI3Kα-mutant), and MX-1 (PTEN-null) tumor models. Pictilisib (GDC-0941) decreases the time of RP-56976-induced mitotic arrest prior to apoptosis[1]. Pictilisib (GDC-0941) shows a high efficacy of antitumor activity in two ZD1839-resistant non-small cell lung cancer (NSCLC) cell lines, A549 and H460. Pictilisib (GDC-0941) is highly efficacious in combination with U0126 in inducing cell growth inhibition, G0-G1 arrest and cell apoptosis. H460 cells with activating mutations of PIK3CA are relatively more sensitive to Pictilisib (GDC-0941) than A549 cells with wild-type PIK3CA[3]. Pictilisib (GDC-0941) reduces PI3K pathway activity in both cell lines, illustrated by decreased pAK. Pictilisib (GDC-0941) significantly reduces secreted VEGF detected in the medium after hypoxic/anoxic exposure in all cells[4].

    In Vivo

    Pictilisib (GDC-0941) (150 mg/kg, p.o.) leads to tumor stasis in MCF7-neo/HER2-bearing animals model. Pictilisib (GDC-0941) and RP-56976 result in tumor regressions during the treatment period leading to enhanced antitumor responses[1]. Tumours in the Pictilisib (GDC-0941)-treated mice show a marked non-linear shrinkage, and when the Pictilisib (GDC-0941) treatment ceased, the tumours in the test cohort mice grow again[2]. Pictilisib (GDC-0941) (25 or 50 mg/kg) reduces tumor growth and PI3K and HIF-1 pathway activity in eGFP-FTC133 tumor-bearing mice[4].

    Clinical Trial
    Molecular Weight

    513.64

    Formula

    C₂₃H₂₇N₇O₃S₂

    CAS No.

    957054-30-7

    SMILES

    CS(N1CCN(CC2=CC3=C(C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)S2)CC1)(=O)=O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (194.69 mM)

    * "≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.1947 mL 0.9734 mL 1.9469 mL
    *

    请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。 -80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

    In Vivo:

    请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
    分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 1.

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

      此方案可获得 ≥ 2.5 mg/mL (4.87 mM,饱和度未知) 的澄清溶液。

      以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

      将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,澄清透明的生理盐水溶液
    *以上所有助溶剂都可在 MCE 网站选购。
    References
    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.

    References

    Purity: 99.62%

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    Keywords:

    PictilisibGDC-0941GDC0941GDC 0941PI3KAutophagyApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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    产品名称:
    Pictilisib
    目录号:
    HY-50094
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