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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-PARP-RK-582
RK-582

Chemical Structure : RK-582

CAS No.: 2171388-28-4

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RK-582 (RK582)

货号: PC-49498Not For Human Use, Lab Use Only.

RK-582 (RK582) is a highly selective, potent and orally efficacious tankyrase inhibitor with IC50 of 39.1 and 36.2 nM for TNKS/TNKS2, respectively.

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

    生物&药学活性

    RK-582 (RK582) is a highly selective, potent and orally efficacious tankyrase inhibitor with IC50 of 39.1 and 36.2 nM for TNKS1/TNKS2, respectively.
    RK-582 shows high potency comparable with that of RK-287107 and G007-LK, displays no significant effect (>200-fold selectivity) against human PARP family member enzymes PARP1, PARP2 (poly ADPribosylation), and PARP10 (mono ADP-ribosylation).
    RK-582 exhibits a high potency for the inhibition of TCF reporter activities at IC50 values of HEK293 (0.3 nM) and DLD-1 cells (3.1 nM).
    RK-582 exhibited potent GI50 (35 nM), high sensitivity and sigmoid dependency achieving complete growth inhibition at 10 uM on CRC cells via MTT assays.
    RK-582 induced AXIN2 accumulation and downregulation of β-catenin.
    RK-582 (10 or 20 mg/kg, twice daily, oral or i.p.) exhibited a markedly robust tumor growth inhibition in a COLO-320DM mouse xenograft model.

    物理化学性质&存储条件

    分子量 510.61
    分子式 C27H35FN6O3
    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

    6-(cis-2,6-dimethylmorpholino)-4-fluoro-1-methyl-1'-(8-methyl-4-oxo-3,4,5,6,7,8- hexahydropyrido[2,3-d]pyrimidin-2-yl)spiro[indoline-3,4'-piperidin]-2-one

    参考文献

    1. Fumiyuki Shirai, et al. J Med Chem. 2020 Apr 23;63(8):4183-4204.

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