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

Fedratinib hydrochloride hydrate  (Synonyms: TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate)

Cat. No.: HY-10409A Purity: 99.92%
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Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

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

Fedratinib hydrochloride hydrate Chemical Structure

Fedratinib hydrochloride hydrate Chemical Structure

CAS No. : 1374744-69-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 77 In-stock
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10 mg USD 70 In-stock
100 mg USD 150 In-stock
200 mg USD 250 In-stock
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Customer Review

Based on 39 publication(s) in Google Scholar

Other Forms of Fedratinib hydrochloride hydrate:

Fedratinib hydrochloride hydrate Related Antibodies

Top Publications Citing Use of Products

35 Publications Citing Use of MCE Fedratinib hydrochloride hydrate

WB
Proliferation Assay
IF

    Fedratinib hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 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.

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    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • Purity & Documentation

    • References

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    Description

    Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC50s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate 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 hydrochloride hydrate Related Antibodies
    In Vivo

    Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) trewatment 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

    615.62

    Formula

    C27H40Cl2N6O4S
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    [H]Cl.[H]O[H].[H]Cl.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

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (162.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 100 mg/mL (162.44 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.6244 mL 8.1219 mL 16.2438 mL
    5 mM 0.3249 mL 1.6244 mL 3.2488 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (4.06 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.92%

    COA (253 KB) HNMR (322 KB) LCMS (95 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 (sealed storage, away from moisture). 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 / H2O 1 mM 1.6244 mL 8.1219 mL 16.2438 mL 40.6095 mL
    5 mM 0.3249 mL 1.6244 mL 3.2488 mL 8.1219 mL
    10 mM 0.1624 mL 0.8122 mL 1.6244 mL 4.0609 mL
    15 mM 0.1083 mL 0.5415 mL 1.0829 mL 2.7073 mL
    20 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0305 mL
    25 mM 0.0650 mL 0.3249 mL 0.6498 mL 1.6244 mL
    30 mM 0.0541 mL 0.2707 mL 0.5415 mL 1.3536 mL
    40 mM 0.0406 mL 0.2030 mL 0.4061 mL 1.0152 mL
    50 mM 0.0325 mL 0.1624 mL 0.3249 mL 0.8122 mL
    60 mM 0.0271 mL 0.1354 mL 0.2707 mL 0.6768 mL
    80 mM 0.0203 mL 0.1015 mL 0.2030 mL 0.5076 mL
    100 mM 0.0162 mL 0.0812 mL 0.1624 mL 0.4061 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Fedratinib hydrochloride hydrate 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:

    Fedratinib hydrochloride1374744-69-0TG-101348 hydrochlorideSAR 302503 hydrochlorideJAKApoptosisJanus kinaseJAK2orallymyeloproliferativeSTAT5phosphorylationanti-proliferationFLT3RETanti-cancerJAK2V617FInhibitorinhibitorinhibit

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