SJ45566 | LCK PROTAC | Probechem Biochemicals

Chemical Structure : SJ45566

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SJ45566 (SJ 45566, SJ-45566)

货号: PC-22646Not For Human Use, Lab Use Only.

SJ45566 is a potent, selective and orally active dasatinib-based LCK PROTAC degrader with DC50 of 1.21 nM (Dmax 98%) in KOPT-K1 cells.

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生物&药学活性

SJ45566 is a potent, selective and orally active dasatinib-based LCK PROTAC degrader with DC50 of 1.21 nM (Dmax 98%) in KOPT-K1 cells.
SJ45566 (0.01 nM to 1000 nM for 6 h) reduces levels of phospo-LCK in the KOPT-K1 cells.
SJ45566 displays high activity in the KOPT-K1 cell viability assay with LC50 of 1.98 nM.
SJ45566 exhibits moderate clearance (24.03 mL/min/kg) and high oral bioavailability (F = 58%).
SJ45566 (a single 30 mg/kg oral dose) demonstrates in vivo LCK degradation leading to a profound in vivo efficacy in PDX models of T-ALL.

物理化学性质&存储条件

分子量	728.31
分子式	C37H42ClN9O3S
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	N-(2-Chloro-6-methylphenyl)-2-((6-(4-((4-(4-(2,6-dioxopiperidin-3-yl)phenyl)piperazin-1-yl)methyl)piperidin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide

参考文献

1. Jarusiewicz JA, et al. J Med Chem. 2024 Jul 8. doi: 10.1021/acs.jmedchem.4c00481.

SJ45566 (SJ 45566, SJ-45566)

生物&药学活性

物理化学性质&存储条件

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SJ45566 (SJ 45566, SJ-45566)

生物&药学活性

物理化学性质&存储条件

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