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首页-小分子抑制剂&激动剂-Tyrosine Kinase-c-Kit-BPR1J373
BPR1J373

Chemical Structure : BPR1J373

CAS No.: 2121515-47-5

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BPR1J373

货号: PC-35619Not For Human Use, Lab Use Only.

BPR1J373 is a potent, orally available multitargeted kinase inhibitor, potently inhibits FLT3, c-KIT, VEGFR1-3, Aurora A, PDGFRα, PDGFRβ, RET, and SRC with IC50 values of <100 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    BPR1J373 is a potent, orally available multitargeted kinase inhibitor, potently inhibits FLT3, c-KIT, VEGFR1-3, Aurora A, PDGFRα, PDGFRβ, RET, and SRC with IC50 values of <100 nM.
    BPR1J373 inhibits cell proliferation of myeloid leukemia cell lines and primary leukemia cells with constitutively activated c-KIT (KG-1, K562 cell with IC50 of 45 and 49 nM).
    BPR1J373also suppresses c-KIT in AML cell lines and primary AML cells; induces apoptosis by mitochondrial intrinsic pathway through upregulation of proapoptotic proteins Bax and Bak and caspase 8 and 9 activation in Kasumi-1 cells, induces cell-cycle arrest for c-KIT–driven leukemia cells via targeting different signals.
    BPR1J373 effectively suppressed Kasumi-1 cells in xenograft mouse model, effectively suppresses c-KIT phosphorylation of D816V mutation.

    物理化学性质&存储条件

    分子量 549.65
    分子式 C26H31N9O3S
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20 °C 12 个月; 4°C 6 个月
    配置液
    -80 °C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    1-(5-ethylisoxazol-3-yl)-3-(4-(2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazol-5-yl)phenyl)urea

    参考文献

    1. Chen LT, et al. Mol Cancer Ther. 2016 Oct;15(10):2323-2333.

    2. Tsai HJ, et al. Cancer Sci. 2018 Aug 24. doi: 10.1111/cas.13773.

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