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首页-抗体药物偶连体和PROTACs-PROTAC-(R)-SL18
(R)-SL18

Chemical Structure : (R)-SL18

CAS No.: 3023189-40-1

(R)-SL18 (ANXA3 degrader (R)-SL18)

货号: PC-20755Not For Human Use, Lab Use Only.

(R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.

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

    生物&药学活性

    (R)-SL18 is a first-in-class, selective Annexin A3 (ANXA3) degrader, induces degradation of ANXA3 in MDA-MB-231 cells with DC50 value of 3.17 uM.
    (R)-SL18 directly binds to ANXA3 (SPR Kd=0.58 uM) and increases its ubiquitination, thereby inducing ANXA3 degradation with moderate family selectivity.
    (R)-SL18 inhibits cell proliferation against TNBC cells with IC50 of 2.52 uM for MDA-MB-231 and 1.64 uM for MDA-MB-468, induces apoptosis.
    (R)-SL18 showed certain selectivity for the anti-proliferative activity of ANXA3 high-expressing cells over ANXA3 low-expressing cells.
    (R)-SL18 induced ANXA3 selective degradation mainly via the ubiquitin-proteasome system.
    (R)-SL18 showed excellent family selectivity toward ANXA3 degradation (except ANXA6) in vitro.
    (R)-SL18 (1-5 uM) inhibited the wnt/β-catenin signaling pathway in MDA-MB-231 cells.
    (R)-SL18 (20 mg/kg, i.p.) suppressed tumor growth in TNBC PDX model.

    物理化学性质&存储条件

    分子量 597.06
    分子式 C26H21ClN6O5S2
    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-(3-(5-chloro-2-nitrophenyl)ureido)-2-oxoethyl (R)-(1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamodithioate

    参考文献

    1. Liang Y, et al. Acta Pharm Sin B. 2023 Apr;13(4):1686-1698.

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