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    Radotinib
    Radotinib

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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 #: V0673
    CAS #: 926037-48-1Purity ≥98%

    Description: Radotinib (formerly also known as IY-5511) is a novel, potent, selective, orally bioavailable, and second-generation BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM. It is used to treat Chronic Myeloid Leukemia. Radotinib has demonstrated potential antineoplastic activity. 

    References: Haematologica. 2014 Jul;99(7):1191-6; PLoS One. 2015 Jun 12;10(6):e0129853.

    Related CAS #: 926037-48-1 (free base)    926037-85-6 (2HCl) 

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    Molecular Weight (MW)530.50
    FormulaC27H21F3N8O
    CAS No.926037-48-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (188.5 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Other info

    Chemical Name: 4-methyl-N-(3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl)-3-((4-(pyrazin-2-yl)pyrimidin-2-yl)amino)benzamide

    InChi Key: DUPWHXBITIZIKZ-UHFFFAOYSA-N

    InChi Code: InChI=1S/C27H21F3N8O/c1-16-3-4-18(9-23(16)37-26-33-6-5-22(36-26)24-13-31-7-8-32-24)25(39)35-20-10-19(27(28,29)30)11-21(12-20)38-14-17(2)34-15-38/h3-15H,1-2H3,(H,35,39)(H,33,36,37)

    SMILES Code: O=C(NC1=CC(C(F)(F)F)=CC(N2C=C(C)N=C2)=C1)C3=CC=C(C)C(NC4=NC=CC(C5=NC=CN=C5)=N4)=C3

    SynonymsRadotinib; IY-5511; IY5511; IY-5511 HCl; IY 5511; IY5511 HCl; trade name Supect.


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    In Vitro

    In vitro activity: In vitro, Radotinib binds BCR-ABL1 and reduces phosphorylation of CrkL, a BCR-ABL1 target protein. Radotinib also effectively inhibits the proliferation of common mutant clones of BCR-ABL1, with the exception of T315I. In AML cells, radotinib significantly decreases the cell viability, promotes differentiation, and induces CD11b expression and apoptosis. In NB4, THP-1, and Kasumi-1 cells, radotinib also induces CD11b expression, and decreases the viability.


    Kinase Assay: Radotinib (formerly also known as IY-5511) is a novel, potent, selective, orally bioavailable, and second-generation BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM.


    Cell Assay: Cells (BMCs of AML and CML patients, NB4, HL60, KASUMI-1, and THP-1 cells) are seeded in 96-well plates at a density of 2×104 cells/ml with 100 μL of medium per well and then incubated with various concentrations of radotinib (0, 1, 10, and 100 μM) for 72 h at 37°C. The CellTiter 96 solution (20 μL) is added directly to each well and plates are incubated for 4 h in a humidified 5% CO2 atmosphere at 37°C. Absorbance is measured with a PowerWave XS2 Microplate Spectrophotometer at 490 nm and the results are expressed as percentage changes from the basal condition using four to five culture wells for each experimental treatment. In some experiments, HL60 cells are cultured with 100 nM ATRA and 1 μM dasatinib for 4 days, and 10 μM radotinib is added to each group according to the planned schedule

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    References

    Haematologica. 2014 Jul;99(7):1191-6; PLoS One. 2015 Jun 12;10(6):e0129853.


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

    Radotinib

    Radotinib induces caspase-3 dependent apoptosis of CD11b+ cells differentiated from AML cells. PLoS One. 2015 Jun 12;10(6):e0129853.

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