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Mcl-1 inhibitor 3

Catalog No. T11972 CAS 2376774-73-9

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

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Mcl-1 inhibitor 3, CAS 2376774-73-9

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Description	Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate macrocyclic Mcl-1 inhibitor (Ki= 0.061 nM; IC50=19 nM in an OPM-2 cell viability assay).
Targets&IC50	MCL1:0.061 nM (ki), MCL1:19 nM
In vitro	Mcl-1 inhibitor 3 shows an IC50 value of 19 nM in an OPM-2 cell viability assay, and a Ki value of 0.061 nM in Mcl-1 HTRF/TR-FRET assay.
In vivo	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.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.?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.

Molecular Weight	820.39
Formula	C40H52ClF2N5O7S
CAS No.	2376774-73-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Keywords

Mcl-1 inhibitor 3 2376774-73-9 Apoptosis BCL Mcl 1 inhibitor 3 Mcl1 inhibitor 3 inhibitor inhibit

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