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    TG-101209
    TG-101209

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0050
    CAS #: 936091-14-4Purity ≥98%

    Description: TG101209 is a novel, potent, orally bioactive and selective small molecule JAK2 inhibitor with IC50 of 6 nM. It is less potent to Flt3 and RET with IC50 of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, and is sensitive to JAK2V617F and MPLW515L/K mutations. It  induced dose- and time-dependent cytotoxicity in a variety of multiple myeloma (MM) cell lines. TG101209 has anticancer activity.

    References: Am J Hematol. 2010 Sep;85(9):675-86;  2007 Aug;21(8):1658-68.


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    Molecular Weight (MW)509.67
    FormulaC26H35N7O2S
    CAS No.936091-14-4
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 102 mg/mL (200.12 mM)
    Water:<1 mg/mL (slightly soluble or insoluble)
    Ethanol: <1 mg/mL (slightly soluble or insoluble)
    Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 12mg/mL
    Synonyms/Chemical NameTG101209; TG-101209; TG 101209; N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide


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    In VitroTG101209 is an orally bioavailable, small molecule, ATP-competitive inhibitor towards several tyrosine kinases. TG101209 inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 of B200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 inducs cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3
    In Vivo100 mg/kg of TG101209 effectively prolongs the survival in JAK2V617F-induced disease (10 days). Compared with placebo-treated animals, TG101209-treated animals exhibit statistically significant, dose-dependent reduction in the circulating tumor cell burden at day +11 to 20%.
    Animal modelBa/F3-V617F-GFP cells are injected into immunodeficient SCID mice to induce a rapidly fatal, fully penetrant hematopoietic disease.
    Formulation & DosageTG101209 is dissolved in DMSO; 100 mg/kg; oral gavage
    References[1] Pardanani A, et al, Leukemia, 2007, 21(8), 1658-1668.


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

     

    TG101209

    Mechanism of action of TG101209. Am J Hematol. 2010 Sep;85(9):675-86.
     

    TG101209

    Preferential killing of CD45+ cells by TG101209. Am J Hematol. 2010 Sep;85(9):675-86.
     

    TG101209

    TG101209 synergizes with PI3K inhibitor LY294002 in killing myeloma cells. Am J Hematol. 2010 Sep;85(9):675-86.



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