Chemical Structure : SJ45566
CAS No.:
SJ45566
(SJ 45566, SJ-45566)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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728.31
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Formula
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C37H42ClN9O3S
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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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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
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References
1. Jarusiewicz JA, et al. J Med Chem. 2024 Jul 8. doi: 10.1021/acs.jmedchem.4c00481.
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