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

Pictilisib  (Synonyms: GDC-0941)

Cat. No.: HY-50094 Purity: 99.80%
COA Handling Instructions

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).

For research use only. We do not sell to patients.

Pictilisib Chemical Structure

Pictilisib Chemical Structure

CAS No. : 957054-30-7

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 73 In-stock
Solid
10 mg USD 66 In-stock
50 mg USD 99 In-stock
100 mg USD 158 In-stock
200 mg USD 277 In-stock
500 mg   Get quote  
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Customer Review

Based on 49 publication(s) in Google Scholar

Other Forms of Pictilisib:

Top Publications Citing Use of Products

39 Publications Citing Use of MCE Pictilisib

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]

    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: 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: 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.

    View All PI3K Isoform Specific Products:

    View All Isoforms
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    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)

    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

     

    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].

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

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

    513.64

    Appearance

    Solid

    Formula

    C23H27N7O3S2
    CAS No.
    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; ultrasonic and warming and heat to 60°C)

    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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  0.5% MC  0.5% Tween-80

      Solubility: 5 mg/mL (9.73 mM); Suspened solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

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

    • 3.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (4.87 mM); Suspended solution; Need ultrasonic

    • 4.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: 2.5 mg/mL (4.87 mM); Suspended solution; Need ultrasonic

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.80%

    COA (251 KB) HNMR (268 KB) LCMS (266 KB)

    Handling Instructions (2659 KB)
    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
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    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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    Keywords:

    Pictilisib957054-30-7GDC-0941GDC0941GDC 0941PI3KAutophagyApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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