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

Fedratinib  (Synonyms: TG-101348; SAR 302503)

Cat. No.: HY-10409 Purity: 99.59%
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Fedratinib (TG-101348) est un inhibiteur sélectif de JAK2 avec un IC50 de 3 nM, présentant une sélectivité de 35 et 334 fois sur JAK1 et JAK3, respectivement.

Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

For research use only. We do not sell to patients.

Fedratinib Chemical Structure

Fedratinib Chemical Structure

CAS No. : 936091-26-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 64 In-stock
Solution
10 mM * 1 mL in DMSO USD 64 In-stock
Solid
1 mg USD 28 In-stock
5 mg USD 55 In-stock
10 mg USD 77 In-stock
100 mg USD 165 In-stock
200 mg USD 275 In-stock
500 mg USD 605 In-stock
1 g USD 1045 In-stock
2 g USD 1815 In-stock
5 g USD 3575 In-stock
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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Fedratinib:

Fedratinib Related Antibodies

Top Publications Citing Use of Products

35 Publications Citing Use of MCE Fedratinib

WB
Proliferation Assay
IF

    Fedratinib purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2020 Feb;53(2):e12742.  [Abstract]

    EdU staining of HPASMCs pre-treated with DMSO or TG for 1 h following 24 h hypoxic exposure. All images were taken at an original magnification of ×400.

    Fedratinib purchased from MedChemExpress. Usage Cited in: Cell Prolif. 2020 Feb;53(2):e12742.  [Abstract]

    Hypoxia-induced HPASMC proliferation is suppressed by a JAK2 inhibitor. Western blot analysis of p-JAK2, JAK2, p-STAT3 and STAT3 in HPASMCs.

    Fedratinib purchased from MedChemExpress. Usage Cited in: IUBMB Life. 2018 Jan;70(1):81-91.  [Abstract]

    A549 cells are treated with TG101348 (3 nM), BMS-911543 (1.5 nM), and Stattic (2.5 lM) for 24 h, and the conditioned media are collected and applied for tube formation assay in HUVECs.

    Fedratinib purchased from MedChemExpress. Usage Cited in: Mol Pharm. 2017 Jan 3;14(1):274-283.  [Abstract]

    Effects of AP24534 and SAR302503 combination on BCR-ABL1 kinase and related proteins activity in the existence of IL-3.

    View All JAK Isoform Specific Products:

    View All Isoforms
    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fedratinib (TG-101348) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib induces cancer cell apoptosis and has the potential for myeloproliferative disorders research[1][2].

    IC50 & Target[1]

    JAK2

    3 nM (IC50)

    JAK2(V617F)

    3 nM (IC50)

    Flt3

    15 nM (IC50)

    Ret

    48 nM (IC50)

    In Vitro

    Fedratinib (TG101348) inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with an IC50 value of approximately 300 nM for either line. Proliferation of parental Ba/F3 cells was inhibited to a comparable level, with an IC50 value of ～420 nM[1].
    ? Exposure of these cells to Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation[1].
    ? Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner[1].

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

    Fedratinib Related Antibodies
    In Vivo

    Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) shows a dose-dependent reduction in polycythemia and a marked dose-dependent reduction in splenomegaly of treated animals[1].

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

    Animal Model: C57Bl/6 mice induced by the JAK2V617F mutation[1]
    Dosage: 60 mg/kg, 120 mg/kg
    Administration: Oral gavage; twice daily; for 42 days
    Result: Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis.
    Clinical Trial
    Molecular Weight

    524.68

    Formula

    C27H36N6O3S
    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=S(C1=CC=CC(NC2=NC(NC3=CC=C(C=C3)OCCN4CCCC4)=NC=C2C)=C1)(NC(C)(C)C)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 125 mg/mL (238.24 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 1.9059 mL 9.5296 mL 19.0592 mL
    5 mM 0.3812 mL 1.9059 mL 3.8118 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    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)

    C1

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    Volume (start)

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    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.87 mg/mL (5.47 mM); Clear solution

    • Protocol 2

      Add each solvent one by one:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: 2.87 mg/mL (5.47 mM); Suspended solution; Need ultrasonic

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  50% PEG300    50% Saline

      Solubility: 10 mg/mL (19.06 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.87%

    COA (250 KB) HNMR (281 KB) LCMS (266 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9059 mL 9.5296 mL 19.0592 mL 47.6481 mL
    5 mM 0.3812 mL 1.9059 mL 3.8118 mL 9.5296 mL
    10 mM 0.1906 mL 0.9530 mL 1.9059 mL 4.7648 mL
    15 mM 0.1271 mL 0.6353 mL 1.2706 mL 3.1765 mL
    20 mM 0.0953 mL 0.4765 mL 0.9530 mL 2.3824 mL
    25 mM 0.0762 mL 0.3812 mL 0.7624 mL 1.9059 mL
    30 mM 0.0635 mL 0.3177 mL 0.6353 mL 1.5883 mL
    40 mM 0.0476 mL 0.2382 mL 0.4765 mL 1.1912 mL
    50 mM 0.0381 mL 0.1906 mL 0.3812 mL 0.9530 mL
    60 mM 0.0318 mL 0.1588 mL 0.3177 mL 0.7941 mL
    80 mM 0.0238 mL 0.1191 mL 0.2382 mL 0.5956 mL
    100 mM 0.0191 mL 0.0953 mL 0.1906 mL 0.4765 mL
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    Fedratinib Related Classifications

    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:

    Fedratinib936091-26-8TG-101348 SAR 302503TG101348TG 101348SAR302503SAR 302503SAR-302503JAKApoptosisJanus kinaseJAK2orallymyeloproliferativeSTAT5phosphorylationanti-proliferationFLT3RETanti-cancerJAK2V617FInhibitorinhibitorinhibit

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