2. Neuronal Signaling Stem Cell/Wnt Apoptosis
  3. γ-secretase Apoptosis
  4. Nirogacestat dihydrobromide

Nirogacestat dihydrobromide  (Synonyms: PF-3084014 dihydrobromide; PF-03084014 dihydrobromide)

目录号: HY-15185B 纯度: 99.63%
COA 产品使用指南

摩尔计算器

Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) 是一种有效的，具有口服活性的，可逆的非竞争性的选择性的 γ-secretase 抑制剂，IC50 为 6.2 nM。Nirogacestat dihydrobromide 抑制 Notch 信号通路，同时最小化胃肠道毒性。可用于研究 Notch 受体依赖性肿瘤。

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Nirogacestat dihydrobromide Chemical Structure

Nirogacestat dihydrobromide Chemical Structure

CAS No. : 1962925-29-6

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规格 价格 是否有货 数量
1 mg ￥450
In-stock
5 mg ￥990
In-stock
10 mg ￥1650
In-stock
50 mg ￥4600
In-stock
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200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of Nirogacestat dihydrobromide:

Nirogacestat dihydrobromide 相关抗体

Top Publications Citing Use of Products

    Nirogacestat dihydrobromide purchased from MCE. Usage Cited in: Int J Oncol. 2018 Jul;53(1):99-112.  [Abstract]

    The expression of E-cadherin, N-cadherin and Snail in Enza-R cells is examined by western blot analysis. The cells are transfected with Ad-GFP or Ad-HepaCAM for 72 h and treated with 5 μM PF-3084014 for 48 h. GAPDH served as a loading control.

    Nirogacestat dihydrobromide purchased from MCE. Usage Cited in: EMBO Mol Med. 2017 Jul;9(7):950-966.  [Abstract]

    Turnover of endogenous CD74 P8 is inhibited by RO4929079 and BMS-906024. Cell lysate Western blot of A20 cells treated with GSIs is developed with In-1 antibody. MK-0752 and Semagacestat tests used the same control lane (0 nM).

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers[1].

    体外研究
    (In Vitro)

    The IC50 of Nirogacestat (PF-03084014) for γ-secretase enzyme inhibition in cell-free assay for Aβ production using detergent solubilized membranes derived from HeLa cells is determined to be 6.2 nM. When tested for inhibition of Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1, the cell IC50 is determined to be 13.3 nM. Nirogacestat causes a significant increase in caspase-3 activities in HPB-ALL and TALL-1 cells as well as an induction of cleaved PARP and cleaved caspase-3 after a 7-day treatment[1].

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

    Nirogacestat dihydrobromide 相关抗体:
    体内研究
    (In Vivo)

    Nirogacestat (PF-03084014) shows robust antitumor activity in this model on 14-day twice daily dosing. Tumor growth inhibition is dose dependent, with maximal tumor growth inhibition of ~92% obtained at high dose levels (150 mg/kg). In tumor growth inhibition studies where mice receive repetitive twice daily dosing for more than a week, Nirogacestat is well tolerated at dose levels below 100 mg/kg as no significant weight loss, morbidity, or mortality is observed. When the dose is increased to 150 mg/kg, however, mice have diarrhea and show weight loss (10-15%) approximately 10 days after compound administration. The body weight of treated animals usually returns to normal if dosing holidays are given, suggesting that the toxicity of Nirogacestat is reversible[1].

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

    651.47

    Formula

    C27H43Br2F2N5O
    CAS 号
    性状

    固体

    颜色

    White to off-white

    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： 

    DMSO 中的溶解度 : 80 mg/mL (122.80 mM; 超声助溶; 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 1.5350 mL 7.6750 mL 15.3499 mL
    5 mM 0.3070 mL 1.5350 mL 3.0700 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。

    • 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
    参考文献

    Nirogacestat dihydrobromide 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
    DMSO 1 mM 1.5350 mL 7.6750 mL 15.3499 mL 38.3748 mL
    5 mM 0.3070 mL 1.5350 mL 3.0700 mL 7.6750 mL
    10 mM 0.1535 mL 0.7675 mL 1.5350 mL 3.8375 mL
    15 mM 0.1023 mL 0.5117 mL 1.0233 mL 2.5583 mL
    20 mM 0.0767 mL 0.3837 mL 0.7675 mL 1.9187 mL
    25 mM 0.0614 mL 0.3070 mL 0.6140 mL 1.5350 mL
    30 mM 0.0512 mL 0.2558 mL 0.5117 mL 1.2792 mL
    40 mM 0.0384 mL 0.1919 mL 0.3837 mL 0.9594 mL
    50 mM 0.0307 mL 0.1535 mL 0.3070 mL 0.7675 mL
    60 mM 0.0256 mL 0.1279 mL 0.2558 mL 0.6396 mL
    80 mM 0.0192 mL 0.0959 mL 0.1919 mL 0.4797 mL
    100 mM 0.0153 mL 0.0767 mL 0.1535 mL 0.3837 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.

    Keywords:

    Nirogacestat dihydrobromide1962925-29-6PF-3084014 dihydrobromidePF-03084014 dihydrobromideγ-secretaseApoptosisGamma secretaseNotchgastrointestinaltoxicitycancerInhibitorinhibitorinhibit

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