Mcl-1 inhibitor 3 (compound 1) is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (K_i= 0.061 nM; IC₅₀=19 nM in an OPM-2 cell viability assay). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity^[1].
.

Mcl-1 inhibitor 3 shows an IC₅₀ value of 19 nM in an OPM-2 cell viability assay, and a K_i value of 0.061 nM in Mcl-1 HTRF/TR-FRET assay^[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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 IC₅₀ values 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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

820.38

C₄₀H₅₂ClF₂N₅O₇S

2376774-73-9

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Rescourio G, Discovery and in Vivo Evaluation of Macrocyclic Mcl-1 Inhibitors Featuring an α-Hydroxy Phenylacetic Acid Pharmacophore or Bioisostere.J Med Chem. 2019 Nov 27;62(22):10258-10271.