1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Apoptosis
  2. JAK
    Apoptosis
  3. Fedratinib

Fedratinib (Synonyms: TG-101348; SAR 302503)

Cat. No.: HY-10409 Purity: 99.90%
Handling Instructions

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

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Other Forms of Fedratinib:

Top Publications Citing Use of Products

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

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

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

    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 MCE. Usage Cited in: Cell Prolif. 2020 Jan 14:e12742.

    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 MCE. Usage Cited in: Cell Prolif. 2020 Jan 14:e12742.

    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.

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    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

    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].

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

    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].

    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.

    936091-26-8

    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 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 250 mg/mL (476.48 mM; Need ultrasonic)

    H2O : < 0.1 mg/mL (insoluble)

    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
    10 mM 0.1906 mL 0.9530 mL 1.9059 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

    • 2.

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

      Solubility: 2.5 mg/mL (4.76 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.76 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References

    Purity: 99.90%

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    Keywords:

    FedratinibTG-101348 SAR 302503TG101348TG 101348SAR302503SAR 302503SAR-302503JAKApoptosisJanus kinaseJAK2orallymyeloproliferativeSTAT5phosphorylationanti-proliferationFLT3RETanti-cancerJAK2V617FInhibitorinhibitorinhibit

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    Product Name:
    Fedratinib
    Cat. No.:
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