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MS105

Chemical Structure : MS105

CAS No.: 2408339-39-7

MS105 (YX39-105, PTK6 PROTAC)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 1072.32
    Formula C56H70FN13O6S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    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

    References

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

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