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Chemical Structure : SJ45566
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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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.
| M.Wt | 728.31 | |
| Formula | C37H42ClN9O3S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jarusiewicz JA, et al. J Med Chem. 2024 Jul 8. doi: 10.1021/acs.jmedchem.4c00481.
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