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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Topoisomerase-STA-8666
STA-8666

Chemical Structure : STA-8666

CAS No.: 1472614-83-7

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STA-8666 (STA8666;STA-21-8666;PEN-866)

货号: PC-35639Not For Human Use, Lab Use Only.

STA-8666 (STA8666, STA-21-8666, PEN-866) is a novel HSP90 inhibitor/SN-38 drug conjugate (HDC), a potent topoisomerase I inhibitor and pharmacologically active metabolite of irinotecan, STA-8666 is cleaved by carboxylesterase (CES) to release SN-38.

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

    生物&药学活性

    STA-8666 (STA8666, STA-21-8666, PEN-866) is a novel HSP90 inhibitor/SN-38 drug conjugate (HDC), a potent topoisomerase I inhibitor and pharmacologically active metabolite of irinotecan, STA-8666 is cleaved by carboxylesterase (CES) to release SN-38.
    STA-8666 demonstrates dramatically superior activity in comparison to equimolar doses of irinotecan against 5 patient-derived pancreatic adenocarcinoma xenografts with prolonged remissions in some tumors.
    STA-8666 also causes complete tumor regression in preclinical mouse models of pediatric sarcoma.

    物理化学性质&存储条件

    分子量 879.971
    分子式 C49H49N7O9
    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

    (S)-4,11-diethyl-4-hydroxy-3,14-dioxo-3,4,12,14-tetrahydro-1H-pyrano[3',4':6,7]indolizino[1,2-b]quinolin-9-yl 4-(2-(5-(3-(2,4-dihydroxy-5-isopropylphenyl)-5-hydroxy-4H-1,2,4-triazol-4-yl)-1H-indol-1-yl)ethyl)piperidine-1-carboxylate

    参考文献

    1. Proia DA, et al. Mol Cancer Ther. 2015 Nov;14(11):2422-32.

    2. Heske CM, et al. Oncotarget. 2016 Oct 4;7(40):65540-65552.

    3. Bobrov E, et al. Oncotarget. 2017 Jan 17;8(3):4399-4409.

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