Mcl-1 inhibitor3 (compound 1) is a highly potent and orally activate macrocyclicMcl-1inhibitor (K_i= 0.061 nM;IC₅₀=19 nM in an OPM-2 cell viability assay).Mcl-1 inhibitor3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity^[1].
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Mcl-1 inhibitor 3 shows an IC₅₀value of 19 nM in an OPM-2 cell viability assay, and a K_ivalue of 0.061 nM in Mcl-1 HTRF/TR-FRET assay^[1].

Mcl-1 inhibitor 3 (oral administration; 3, 10, or 30 mg/kg; 6 hours) causes a significant loss of luminescence (~40%) over vehicle at 30 mg/kg,This effect was observed with unbound drug levels in plasma, the [plasma]_u/OPM-2 IC₅₀values are 0.24, 0.93 and 3.65 μM in 3, 10, 30 mg/kg doses,respectively^[1].
Mcl-1 inhibitor 3 (oral administration; 10, 30, or 60 mg/kg; 6 hours) activates Bak by 8-fold at 30 mg/kg and by 14-fold at 60 mg/kg in this OPM-2 Luc assay,this test is based on the detection of activated Bak in nude mice subcutaneously injected with via electrochemiluminescence.^[1].
Mcl-1 inhibitor 3 (oral administration; 10, 30, or 60 mg/kg; 30 days) led to a robust dose-dependent tumor growth inhibition at 30 mg/kg (44% TGI) and 34% tumor regression when the animals were dosed at 60 mg/kg.Lastly, no body weight loss is observed in any of the mice in this study efficacy models^[1].

820.38

C₄₀H₅₂ClF₂N₅O₇S

2376774-73-9

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