Chemical Structure : MS105
CAS No.:
2408339-39-7
MS105
Catalog No.: PC-23403Not For Human Use, Lab Use Only.
MS105 is a potent, selective protein tyrosine kinase 6 (PTK6) ROTAC 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)
Biological Activity
MS105 is a potent, selective protein tyrosine kinase 6 (PTK6) ROTAC 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
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M.Wt
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1072.32
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Formula
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C56H70FN13O6S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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(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
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References
1. Martinez C, et al. Cell Chem Biol. 2024 Nov 11:S2451-9456(24)00443-4.
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