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

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.

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CAS No. : 1883299-62-4

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고객리뷰

Based on 3 publication(s) in Google Scholar

Other Forms of Brepocitinib:

Brepocitinib Related Antibodies

Top Publications Citing Use of Products

    Brepocitinib purchased from MedChemExpress. Usage Cited in: Heliyon. 2023 Jan 13;9(1):e12958.

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

    View All JAK Isoform Specific Products:

    View All Isoforms
    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • 순도&문서

    • References

    • 고객리뷰

    제품 설명

    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)

    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].

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

    Brepocitinib Related Antibodies
    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].

    MedChemExpress (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.
    분자량

    389.40

    화학식

    C18H21F2N7O
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C([C@H]1C(F)(F)C1)N2C3CN(C4=NC(NC5=CN(C)N=C5)=NC=C4)CC2CC3
    선적

    Room temperature in continental US; may vary elsewhere.
    보관

    4°C, protect from light

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

    용액&용해도
    In Vitro: 

    DMSO : 125 mg/mL (321.01 mM; Need ultrasonic; 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 2.5681 mL 12.8403 mL 25.6805 mL
    5 mM 0.5136 mL 2.5681 mL 5.1361 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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    In Vivo Dissolution Calculator
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    순도&문서

    Purity: 99.97%

    SDS (393 KB)

    COA (247 KB) HNMR (264 KB) LCMS (91 KB)

    Handling Instructions (2659 KB)
    References

    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 (protect from light). 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
    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
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    Brepocitinib Related Classifications

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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:

    Brepocitinib1883299-62-4PF-06700841PF06700841PF 06700841JAKJanus kinaseInhibitorinhibitorinhibit

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