1. Epigenetics Protein Tyrosine Kinase/RTK JAK/STAT Signaling Stem Cell/Wnt
  2. JAK
  3. Brepocitinib

Brepocitinib  (Synonyms: PF-06700841)

目录号: HY-112708 纯度: 98.64%
COA 产品使用指南

Brepocitinib (PF-06700841) 是一种有效的 JAK1TYK2 双重抑制剂, IC50 值分别为 17 nM 和 23 nM。Brepocitinib 还分别以 IC50 值为 77 nM 和 6.49 μM 抑制 JAK2JAK3

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Brepocitinib Chemical Structure

Brepocitinib Chemical Structure

CAS No. : 1883299-62-4

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Customer Review

Other Forms of Brepocitinib:

    Brepocitinib purchased from MCE. Usage Cited in: Heliyon. 2023 Jan 13.

    PF-06700841 (Brepocitinib; 20 nM; 24 h) blocks hyperin-induced expression of JAK1 and STAT3 in HTR-8/SVneo cells.

    查看 JAK 亚型特异性产品:

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Brepocitinib (PF-06700841) is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. Brepocitinib also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively[1].

    IC50 & Target[1]

    JAK1

    17 nM (IC50)

    JAK2

    77 nM (IC50)

    JAK3

    6.9 μM (IC50)

    体外研究
    (In Vitro)

    Brepocitinib (PF-06700841; Compound 23) potently inhibits TYK2/JAK2 mediated IL-12/pSTAT4 and IL-23/pSTAT3 (human whole blood (HWB) IC50s of 65 and 120 nM, respectively)[1].
    Brepocitinib has good potency against IL6/pStat1 in the CD3+ cellular subset (IC50 of 81 nM), but lower inhibition of IL6/pSTAT3, again in the CD3+ cellular subset (IC50 of 641 nM)[1].
    Brepocitinib also inhibits the JAK1/JAK3 driven γ-common chain cytokines, represented by IL-15/pStat5 and IL-21/pSTAT3 with reasonable potency (HWB IC50s of 238 and 204 nM, respectively)[1].
    Brepocitinib inhibits EPO/pSTAT5 (JAK2 homodimer) in HWB spiked with CD34+ progenitor cells (IC50 of 577 nM). IL10/pSTAT3 (TYK2/JAK1) and IL27/pSTAT3 (JAK1/JAK2/TYK2) are also inhibited by Brepocitinib with IC50s of 305 nM and 86 nM, respectively[1].

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

    体内研究
    (In Vivo)

    Brepocitinib (PF-06700841; Compound 23; 3-30 mg/kg; oral administration; for 7 consecutive days; female Lewis rats) treatment significantly reduces paw volume increase in a dose-dependent manner. The plasma concentrations in animals dosed with Brepocitinib at peak (30 min) and trough (24 h) time intervals post final dose respectively are as follows: 3 mg/kg, 3.54 μM, 0.0221 μM; 10 mg/kg, 10.95 μM, 0.06 μM; and 30 mg/kg, 23.89 μM, 0.06 μM[1].

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

    Animal Model: Female Lewis rats with induced arthritis[1]
    Dosage: 3 mg/kg, 10 mg/kg, or 30 mg/kg
    Administration: Oral administration; for 7 consecutive days
    Result: Increased in paw volume was significantly lower and dose-dependent.
    Clinical Trial
    分子量

    389.40

    Formula

    C18H21F2N7O

    CAS 号
    性状

    固体

    颜色

    Off-white to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 125 mg/mL (321.01 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 2.5681 mL 12.8403 mL 25.6805 mL
    5 mM 0.5136 mL 2.5681 mL 5.1361 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 (protect from light)。-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

    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

    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 (protect from light)。-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 2.5681 mL 12.8403 mL 25.6805 mL 64.2013 mL
    5 mM 0.5136 mL 2.5681 mL 5.1361 mL 12.8403 mL
    10 mM 0.2568 mL 1.2840 mL 2.5681 mL 6.4201 mL
    15 mM 0.1712 mL 0.8560 mL 1.7120 mL 4.2801 mL
    20 mM 0.1284 mL 0.6420 mL 1.2840 mL 3.2101 mL
    25 mM 0.1027 mL 0.5136 mL 1.0272 mL 2.5681 mL
    30 mM 0.0856 mL 0.4280 mL 0.8560 mL 2.1400 mL
    40 mM 0.0642 mL 0.3210 mL 0.6420 mL 1.6050 mL
    50 mM 0.0514 mL 0.2568 mL 0.5136 mL 1.2840 mL
    60 mM 0.0428 mL 0.2140 mL 0.4280 mL 1.0700 mL
    80 mM 0.0321 mL 0.1605 mL 0.3210 mL 0.8025 mL
    100 mM 0.0257 mL 0.1284 mL 0.2568 mL 0.6420 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.

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    产品名称:
    Brepocitinib
    目录号:
    HY-112708
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