2376774-73-9
2376774-73-9 structure
- Name: Mcl-1 inhibitor 3
- Chemical Name: Mcl-1 inhibitor 3
- CAS Number: 2376774-73-9
- Molecular Formula: C40H52ClF2N5O7S
- Molecular Weight: 820.38
- Catalog: Signaling Pathways Apoptosis Bcl-2 Family
- Create Date: 2020-04-08 04:41:25
- Modify Date: 2024-01-02 18:32:51
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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]. .
| Name | Mcl-1 inhibitor 3 |
|---|
| 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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| Related Catalog | |
| Target |
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. |
| References |
| Molecular Formula | C40H52ClF2N5O7S |
|---|---|
| Molecular Weight | 820.38 |