2. Apoptosis
  3. Bcl-2 Family
  4. Mcl-1 inhibitor 3

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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Mcl-1 inhibitor 3 Related Antibodies

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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

Mcl-1

19 nM (IC50)

Mcl-1

0.061 nM (Ki)

Cellular Effect
Cell Line Type Value Description References
OPM-2 IC50
19 nM
Compound: 1
Antiproliferative activity against human OPM2 cells assessed as reduction in cell viability after 16 hrs by CellTiter-Glo based luminescence assay
Antiproliferative activity against human OPM2 cells assessed as reduction in cell viability after 16 hrs by CellTiter-Glo based luminescence assay
[PMID: 31736296]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Mcl-1 inhibitor 3 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
SMILES

ClC1=CC(CCC2)=C(C=C1)[C@]2(CO3)CN(C[C@H]4[C@@H](CC4)[C@@H](OCCN5CC(F)(F)C5)/C=C/CCN(C)C6=O)C7=C3C=CC([C@@](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.
Purity & Documentation
References
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Mcl-1 inhibitor 3 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mcl-1 inhibitor 32376774-73-9Bcl-2 FamilyMyeloma cancer,Inhibitorinhibitorinhibit

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