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

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

目录号: HY-20180 纯度: 99.72%
COA 产品使用指南 技术支持

Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) 是一种有效的 PI3Kα/δ 抑制剂，IC50 值为 3 nM；对 p110β 和 p110γ具有适度的选择性。

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Pictilisib dimethanesulfonate Chemical Structure

Pictilisib dimethanesulfonate Chemical Structure

CAS No. : 957054-33-0

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规格 价格 是否有货 数量
Free Sample (0.1 - 0.2 mg)   Apply now  
10 mM * 1 mL in DMSO ￥494
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5 mg ￥318
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10 mg ￥414
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25 mg ￥600
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50 mg ￥900
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100 mg ￥1440
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200 mg ￥2300
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500 mg   询价  
1 g   询价  

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Customer Review

Other Forms of Pictilisib dimethanesulfonate:

Pictilisib dimethanesulfonate 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 50 篇科研文献

WB
Proliferation Assay

    Pictilisib dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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 dimethanesulfonate 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.

    查看 PI3K 亚型特异性产品:

    查看所有亚型
    PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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

     

    体外研究
    (In Vitro)

    与单药处理相比，Pictilisib (GDC-0941) 和 RP-56976 可将乳腺癌细胞系中的肿瘤细胞活力降低 80% 或更多。GDC-0941 在 Hs578T1.2 (PI3Kα 野生型)、MCF7-neo/HER2 (PI3Kα-突变体) 和 MX-1 (PTEN 无效) 肿瘤模型中抑制 Akt 磷酸化和 Akt 信号通路的下游靶标，例如 pPRAS40 和 pS6 . Pictilisib (GDC-0941) 缩短细胞凋亡前 RP-56976 诱导的有丝分裂停滞时间[1]。
    Pictilisib 在两种 ZD1839 耐药的非小细胞肺癌 (NSCLC) 细胞系 A549 和 H460 中显示出高效的抗肿瘤活性。Pictilisib 与 U0126 联合使用可高效诱导细胞生长抑制、G0-G1 期阻滞和细胞凋亡。具有 PIK3CA 激活突变的 H460 细胞对 Pictilisib 的敏感性高于具有野生型 PIK3CA 的 A549 细胞[3]。
    Pictilisib 降低两种细胞系中的 PI3K 通路活性，表现为 pAK 降低。Pictilisib 显著减少所有细胞在缺氧/缺氧暴露后在培养基中检测到的分泌性 VEGF[4]。

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

    Pictilisib dimethanesulfonate 相关抗体:
    体内研究
    (In Vivo)

    Pictilisib (GDC-0941) (150 mg/kg，口服) 在携带 MCF7-neo/HER2 的动物模型中导致肿瘤停滞[1]。
    Pictilisib 和 RP-56976 在处理期间导致肿瘤消退，从而增强抗肿瘤反应[1]。
    Pictilisib 处理的小鼠体内的肿瘤显示出明显的非线性收缩，当 Pictilisib 处理停止时，测试组小鼠中的肿瘤再次生长[2]。
    Pictilisib (25 或 50 mg/kg) 可降低荷瘤 eGFP-FTC133 小鼠的肿瘤生长以及 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

    705.85

    Formula

    C25H35N7O9S4
    CAS 号
    性状

    固体

    颜色

    White to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

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

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : 7.14 mg/mL (10.12 mM; 超声助溶 (<60°C))

    DMSO 中的溶解度 : 7.14 mg/mL (10.12 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 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 (sealed storage, away from moisture)。-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。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

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

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    纯度 & 产品资料

    纯度: 99.72%

    COA (290 KB) LCMS (105 KB)

    产品使用指南 (1538 KB)
    参考文献
    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[1].

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

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

    Pictilisib dimethanesulfonate 相关分类

    完整储备液配制表

    * 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 (sealed storage, away from moisture)。-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。

    可选溶剂 浓度 溶剂体积 质量 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

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    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.

    Keywords:

    Pictilisib957054-33-0GDC-0941GDC-0941 2 MeSO3HGDC0941GDC 0941PI3KAutophagyApoptosisPhosphoinositide 3-kinaseInhibitorinhibitorinhibit

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