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    Tirbanibulin (KX2391; KX-O1)
    Tirbanibulin (KX2391; KX-O1)

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    This product is for research use only, not for human use. We do not sell to patients.
    Number: - + Pieces(InventoryPieces)
    InvivoChem Cat #: V0666
    CAS #: 897016-82-9 Purity ≥98%

    Description: Tirbanibulin (also known as KXO1; KX2-391; Klisyri) is novel, potent and the first clinical peptidomimetic Src kinase inhibitor as well as a mitotic/tubulin inhibitor with potential anticancer activity. It has been approved by FDA in 2020 as a medication for the treatment of actinic keratosis on the face or scalp. Tirbanibulin inhibits the peptide substrate site of Src with GI50s of 9-60 nM in cell-based assays. KX2-391 is an orally bioavailable small molecule Src inhibitor with potential antineoplastic activity. Unlike other Src kinase inhibitors which bind to the ATP-binding site, Src kinase inhibitor KX2-391 specifically binds to the peptide substrate binding site of Src kinase; inhibition of kinase activity may result in the inhibition of primary tumor growth and the suppression of metastasis. Src tyrosine kinases are upregulated in many tumor cells and play important roles in tumor cell proliferation and metastasis. 

    References: Dig Dis Sci. 2009 Jul;54(7):1465-74; Eur J Med Chem. 2011 Oct;46(10):4853-8. 

    Related CAS: 897016-82-9 (free base); 1038395-65-1 (HCl); 1080645-95-9 (Tirbanibulin Mesylate); 

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    Molecular Weight (MW)431.53
    CAS No.897016-82-9 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (199.3 mM)
    Water: <1 mg/mL
    Ethanol: 2 mg/mL (3.8 mM)
    Solubility (In vivo)4% DMSO+30% PEG 300+ddH2O: 5 mg/mL
    SynonymsKX 01, KX2-391; KX-01, KX-2-391; Tirbanibulin; KX2391; KX-2391; Tirbanibulin free base; KXO1; KX 2-391; KX 2391 

    Chemical Name: (E)-(4-(2-(1H-indazol-3-yl)vinyl)phenyl)(piperazin-1-yl)methanone


    InChi Code: InChI=1S/C20H20N4O/c25-20(24-13-11-21-12-14-24)16-8-5-15(6-9-16)7-10-19-17-3-1-2-4-18(17)22-23-19/h1-10,21H,11-14H2,(H,22,23)/b10-7+

    SMILES Code: O=C(C1=CC=C(/C=C/C2=NNC3=C2C=CC=C3)C=C1)N4CCNCC4

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    In Vitro

    In vitro activity: KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines. KX2-391 is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. KX2-391 is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively.

    Kinase Assay: Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. Tirbanibulin (KX2-391) shows steep dose-response curves against Huh7 (GI50=9 nM), PLC/PRF/5 (GI50=13 nM), Hep3B (GI50=26 nM), and HepG2 (GI50=60 nM), four hepatic cell cancer (HCC) cell lines.

    Cell Assay: Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 (NutriCyte, Buffalo, NY) are routinely cultured and maintained in basal medium containing 2% fetal bovine serum (FBS) at 37 °C and 5% CO2. Cells are seeded at 4.0 × 103/190 μL and 8.0 × 103/190 μL per well of 96-well plate in basal medium containing 1.5% FBS. These are cultured overnight at 37 °C and 5% CO2 prior to the addition of KX2-391, at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten microliters of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/mL) is then added to each well on day 3 and cells incubated for 4 hours. The formazan product is dissolved with 10% SDS in dilute HCl. Optical density at 570 nm is measured by using BioTek Synergy HT multiplatform microplate reader. For comparison of activity and potency, parallel experiments are performed using KX2-391. Growth inhibition curves, 50% inhibition concentration (GI50), and 80% inhibition concentration (GI80) are determined using GraphPad Prism 5 statistical software. Data are normalized to represent percentage of maximum response as well as reported in optical density at wavelength of 570 nm (OD570) signal format.

    In VivoIn pre-clinical animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis.
    Animal model N/A
    Formulation & Dosage Oral
    ReferencesDig Dis Sci. 2009 Jul;54(7):1465-74; Eur J Med Chem. 2011 Oct;46(10):4853-8. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.



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