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首页-小分子抑制剂&激动剂-Tyrosine Kinase-RET Tyrosine Kinase (c-RET)-BOS172738
BOS172738

Chemical Structure : BOS172738

CAS No.: 2216753-97-6

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BOS172738 (Zeteletinib, DS 5010)

货号: PC-72475Not For Human Use, Lab Use Only.

BOS172738 (Zeteletinib, DS 5010) is a potent, selective oral RET kinase inhibitor with nanomolar potency against wtRET and RET mutations (Ki <1 nM), >300-fold selectivity against VEGFR2.

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

    生物&药学活性

    BOS172738 (Zeteletinib, DS 5010) is a potent, selective oral RET kinase inhibitor with nanomolar potency against wtRET and RET mutations (Ki <1 nM), >300-fold selectivity against VEGFR2.
    BOS172738 demonstrated exquisite potency for RET and RET mutations with Kd values <1 nM for RETwt, RET(M918T), RET(V804L) and RET(V804M), also demonstrated high selectivity over KDR.
    BOS172738 demonstrated similar potency to ponatinib (IC50=0.5 uM) in inhibiting the in vitro proliferation of a NCO4-RET human CRC cell line (CR1520).
    BOS172738 significantly less anti-proliferative activity in HUVEC normal endothelial cells (IC50=2.9 uM).
    BOS172738 demonstrated potent and durable tumor regression at doses of 30 mg/kg in NSCLC PDX model (CTG-0838:KIF5B-RET), also demonstrated potent tumor regression on larger, established tumors.

    物理化学性质&存储条件

    分子量 500.48
    分子式 C25H23F3N4O4
    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

    2-[6-(6,7-dimethoxyquinolin-3-yl)pyridin-3-yl]-N-[3-(1,1,1-trifluoro-2-methylpropan-2-yl)-1,2-oxazol-5-yl]acetamide

    参考文献

    1. Mitchell Keegan, et al. Cancer Res (2019) 79 (13_Supplement): 2199.

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