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: 99.87%
COA 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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10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 64 In-stock
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10 mg USD 77 In-stock
100 mg USD 165 In-stock
200 mg USD 275 In-stock
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Customer Review

Based on 33 publication(s) in Google Scholar

Other Forms of Fedratinib:

Fedratinib Related Antibodies

Top Publications Citing Use of Products

29 Publications Citing Use of MCE Fedratinib

Proliferation Assay
WB
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.

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    JAK1 JAK2 JAK3 Tyk2 JAK

    • Biological Activity

    • Purity & Documentation

    • References

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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[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

    Appearance

    Solid

    Formula

    C27H36N6O3S
    CAS No.
    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)

    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:  5% DMSO    40% PEG300    5% Tween-80    50% Saline

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

    • 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

    • 3.

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

      Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

    • 4.

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

      Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

    • 5.

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.08 mg/mL (3.96 mM); Clear solution

    *All of the co-solvents are available by MedChemExpress (MCE).
    Purity & Documentation

    Purity: 99.87%

    COA (250 KB) HNMR (281 KB) LCMS (266 KB)

    Handling Instructions (2659 KB)
    References
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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.

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    The molarity calculator equation

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

    Mass   Concentration   Volume   Molecular Weight *
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    The dilution calculator equation

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2

    Keywords:

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

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