BM-1074
BM-1074 is a potent and specific Bcl-2/Bcl-xL inhibitor with Ki values of < 1 nM and IC50 values of 1.8 nM and 6.9 nM for Bcl-2 and Bcl-xL, respectively. BM-1074 induces apoptosis, and exhibits antiproliferative activity against four small-cell lung cancer cell lines (H146, H1963, H187 and H1417) with IC50 values of 1-2 nM.
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- No. CAS: 1391108-10-3
- Fòrmula: C50H57ClN8O7S3
- Peso molecular:1013.69
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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Bcl-2 1.8 nM (IC50) |
Bcl-xL 6.9 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1417 | IC50 |
2.3 nM
Compound: 32, BM-1074
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Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay
Cytotoxicity against human NCI-H1417 cells assessed as growth inhibition after 4 days by WST assay
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[PMID: 23448298] |
| NCI-H146 | IC50 |
1.3 nM
Compound: 32, BM-1074
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Cytotoxicity against human NCI-H146 cells assessed as growth inhibition after 4 days by WST assay
Cytotoxicity against human NCI-H146 cells assessed as growth inhibition after 4 days by WST assay
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[PMID: 23448298] |
| NCI-H187 | IC50 |
1.4 nM
Compound: 32, BM-1074
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Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay
Cytotoxicity against human NCI-H187 cells assessed as growth inhibition after 4 days by WST assay
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[PMID: 23448298] |
| NCI-H1963 | IC50 |
1 nM
Compound: 32, BM-1074
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Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay
Cytotoxicity against human NCI-H1963 cells assessed as growth inhibition after 4 days by WST assay
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[PMID: 23448298] |
BM-1074 (Compound 32) shows high binding affinity to both Bcl-2 and Bcl-xL proteins and exhibits inhibitory activity against H146, H1963, H187, and H1417 cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H146, H1963, H187, and H1417
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Concentration:0-200 nM
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Incubation Time:4 days
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Result:Inhibited the cell growth of H146, H1963, H187 and H1417 cell lines with IC50 values of 1.3 nM, 1.0 nM, 1.4 nM and 2.3 nM, respectively.
BM-1074 (i.v., 15 mg/kg, single) induces strong apoptosis in H146 tumor tissues[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SCID mice (injected with 5 x 106 H146 cancer cells with Matrigel, subcutaneously)[1]
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Dosage:15 mg/kg
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Administration:i.v., 15 mg/kg, daily, 5 days a week for 2 weeks
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Result:Showed good toleration and did not cause significant weight loss or other signs of toxicity, also induced completely and persistent tumor regression in the H146 xenograft model.
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Animal Model:SCID mice (injected with 5 x 106 H146 cancer cells with Matrigel, subcutaneously)[1]
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Dosage:15 mg/kg
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Administration:i.v., 15 mg/kg, single dosage
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Result:Induced robust cleavage of PARP and caspase-3 at both 3 and 6-hr time-points in H146 tumor tissues.
Chemical Information
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No. CAS 1391108-10-3
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Peso molecular 1013.69
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Fòrmula C50H57ClN8O7S3
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SMILES
O=C(C1=C(C)N(C(C)C)C(C2=CC=C(Cl)C=C2)=C1C3=CC=CC(N4CCN(C5=CC=C(NS(=O)(C6=CC=C(N[C@H](CCN(C)C)CSC7=CC=CC=C7)C([N+]([O-])=O)=C6)=O)C=C5)CC4)=C3)NS(=O)(C)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BM-1074 Related Classifications
HY-13846 Related Classifications
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