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首页-抗体药物偶连体和PROTACs-PROTAC-MS105
MS105

Chemical Structure : MS105

CAS No.: 2408339-39-7

MS105 (YX39-105, PTK6 PROTAC)

货号: PC-23403Not For Human Use, Lab Use Only.

MS105 (YX39-105) is a potent, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader, specifically and potently degrades PTK6 in a proteasome and VHL-dependent manner with DC50 of 21 nM and Dmax of 84% in MDA-MB-231/LM2-4 cells.

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

    生物&药学活性

    MS105 (YX39-105) is a potent, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader, specifically and potently degrades PTK6 in a proteasome and VHL-dependent manner with DC50 of 21 nM and Dmax of 84% in MDA-MB-231/LM2-4 cells.
    MS105 exhibits high selectivity against 468 kinases in the KINOMEScan platform in vitro, only five kinases (STK33, RIOK2, YSK4, TNK1, and TRKB) is inhibited >65% (S(35)).
    MS105 potently reduces PTK6 protein levels in a proteasome-dependent manner.
    MS105 inhibits growth of breast cancer cell lines, phenocopies PTK6 shRNA in suppressing viability of breast cancer cells.
    MS105 induces expression of Bim and apoptosis of breast cancer cells.

    物理化学性质&存储条件

    分子量 1072.32
    分子式 C56H70FN13O6S
    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

    (2S,4R)-1-((S)-2-(9-(2-(4-(4-((6-Cyclopropyl-3-(1H-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl)amino)-3-fluorobenzoyl)piperazin-1-yl)acetamido)nonanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide

    参考文献

    1. Martinez C, et al. Cell Chem Biol. 2024 Nov 11:S2451-9456(24)00443-4.

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