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

Pictilisib dimethanesulfonate  (Synonyms: GDC-0941 dimethanesulfonate ; GDC-0941 (2 MeSO3H salt))

製品番号: HY-20180 純度: 99.72%
COA 取扱説明書 Technical Support

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

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CAS 番号 : 957054-33-0

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
5 mg $38 在庫あり
10 mg $60 在庫あり
50 mg $90 在庫あり
100 mg $144 在庫あり
200 mg $252 在庫あり
500 mg   お問い合わせ  
1 g   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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カスタマーレビュー

Based on 68 publication(s) in Google Scholar

Other Forms of Pictilisib dimethanesulfonate:

Pictilisib dimethanesulfonate 関連抗体

Top Publications Citing Use of Products

顧客検証

WB
Cell Proliferation/Viability Assay

    Pictilisib dimethanesulfonate purchased from MedChemExpress. 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 dimethanesulfonate purchased from MedChemExpress. 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 dimethanesulfonate purchased from MedChemExpress. 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 dimethanesulfonate purchased from MedChemExpress. 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 dimethanesulfonate purchased from MedChemExpress. 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 dimethanesulfonate purchased from MedChemExpress. 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 dimethanesulfonate purchased from MedChemExpress. 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 dimethanesulfonate purchased from MedChemExpress. 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.

    PI3K アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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    製品説明

    Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with 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

     

    体外実験

    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].

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

    Pictilisib dimethanesulfonate 関連抗体
    体内実験

    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]. GDC-0941Pictilisib (GDC-0941) (25 or 50 mg/kg) reduces tumor growth and PI3K and HIF-1 pathway activity in eGFP-FTC133 tumor-bearing mice[4].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    分子量

    705.85

    分子式

    C25H35N7O9S4
    CAS 番号
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=S(N1CCN(CC1)CC2=CC3=C(S2)C(N4CCOCC4)=NC(C5=CC=CC6=C5C=NN6)=N3)(C)=O.O=S(O)(C)=O.O=S(O)(C)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
    溶剤 & 溶解度
    体外: 

    H2O : 7.14 mg/mL (10.12 mM; ultrasonic and warming and heat to 60°C)

    DMSO : 7.14 mg/mL (10.12 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.4167 mL 7.0837 mL 14.1673 mL
    5 mM 0.2833 mL 1.4167 mL 2.8335 mL
    10 mM 0.1417 mL 0.7084 mL 1.4167 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    純度とドキュメンテーション

    純度: 99.72%

    COA (251 KB) LCMS (104 KB)

    取扱説明書 (2659 KB)
    参考文献
    細胞実験
    [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[1].

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    動物実験
    [1]

    Mice[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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.4167 mL 7.0837 mL 14.1673 mL 35.4183 mL
    5 mM 0.2833 mL 1.4167 mL 2.8335 mL 7.0837 mL
    10 mM 0.1417 mL 0.7084 mL 1.4167 mL 3.5418 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Pictilisib dimethanesulfonate Related Classifications

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    The dilution calculator equation

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

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
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    • 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.

    Keywords:

    Pictilisib957054-33-0GDC-0941 dimethanesulfonate GDC-0941 2 MeSO3HPI3KAutophagyApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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    製品名:
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    製品番号:
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