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

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

Cat. No.: HY-10409A Purity: 99.31%
Handling Instructions

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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Top Publications Citing Use of Products

    Fedratinib hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 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 hydrochloride hydrate 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 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].

    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].

    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.
    Molecular Weight

    615.62

    Formula

    C₂₇H₄₀Cl₂N₆O₄S

    CAS No.

    1374744-69-0

    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
    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 (406.09 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
    10 mM 0.1624 mL 0.8122 mL 1.6244 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
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    Keywords:

    Fedratinib hydrochlorideTG-101348 hydrochlorideSAR 302503 hydrochlorideJAKApoptosisJanus kinaseJAK2orallymyeloproliferativeSTAT5phosphorylationanti-proliferationFLT3RETanti-cancerJAK2V617FInhibitorinhibitorinhibit

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    Product Name:
    Fedratinib hydrochloride hydrate
    Cat. No.:
    HY-10409A
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