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  3. Mcl-1 inhibitor 3

Mcl-1 inhibitor 3 

Cat. No.: HY-133015
Handling Instructions

Mcl-1 inhibitor 3 (compound 1) 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). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.
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Mcl-1 inhibitor 3 Chemical Structure

Mcl-1 inhibitor 3 Chemical Structure

CAS No. : 2376774-73-9

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Description

Mcl-1 inhibitor 3 (compound 1) 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). Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity[1].
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IC50 & Target[1]

Mcl-1

19 nM (IC50)

Mcl-1

0.061 nM (Ki)

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[1].

In Vivo

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].

Animal Model: Nude miceinjected with HEK293 cells[1]
Dosage: 3, 10, or 30 mg/kg
Administration: Oral administration
Result: Showed a disruption of the Mcl-1/Bak interaction in this in vivo model.
Animal Model: Nude mice injected with human OPM-2 multiple myeloma tumor cells[1]
Dosage: 10, 30, or 60 mg/kg
Administration: Oral administration
Result: Exhibited a inhibition of tumor growth without any toxicity.
Molecular Weight

820.38

Formula

C₄₀H₅₂ClF₂N₅O₇S

CAS No.

2376774-73-9

SMILES

ClC1=CC(CCC2)=C(C=C1)[[email protected]]2(CO3)CN(C[[email protected]]4[[email protected]@H](CC4)[[email protected]@H](OCCN5CC(F)(F)C5)/C=C/CCN(C)C6=O)C7=C3C=CC([[email protected]@](O)(C(NS(=O)(N(C)C)=O)=O)C6)=C7

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

References
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Keywords:

Mcl-1 inhibitor 3Bcl-2 FamilyMyeloma cancer,Inhibitorinhibitorinhibit

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