BM 957
BM 957 is a potent Bcl-2 and Bcl-xL inhibitor, with Kis of 1.2, <1 nM and IC50s of 5.4, 6.0 nM respectively.
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- CAS. Nr.: 1391107-54-2
- Formel: C52H56ClF3N6O7S3
- Molecular Weight:1065.68
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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Bcl-2 5.4 nM (IC50) |
Bcl-xL 6.0 nM (IC50) |
Bcl-2 1.2 nM (Ki) |
Bcl-xL <1 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1417 | IC50 |
21 nM
Compound: 30, BM-957
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Cytotoxicity against human H1417 cells assessed as growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human H1417 cells assessed as growth inhibition after 4 days by WST-8 assay
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[PMID: 23030453] |
| NCI-H146 | IC50 |
22 nM
Compound: 30, BM-957
|
Cytotoxicity against human NCI-H146 cells assessed as growth inhibition after 4 days by WST-8 assay
Cytotoxicity against human NCI-H146 cells assessed as growth inhibition after 4 days by WST-8 assay
|
[PMID: 23030453] |
BM 957 (Compound 30) with ethyl and compound 31 with isopropyl bind to both Bcl-2 and Bcl-xL with very high affinities. While BM 957 and 31 bind to Bcl-2 with IC50 values of 5.4 and 4.0 nM, respectively (Ki values=1.2 and 0.8 nM, respectively), they bind to Bcl-xL with IC50 values of 6.0 and 3.9 nM, respectively (Ki values < 1 nM). BM 957 has IC50 values of 21 nM and 22 nM, respectively, in these two cancer cell lines (H1417 and H146 cell lines). All these compounds induce cell death in a dose-dependent manner but have different potencies. While BM 957 and 31 are several times more potent than 1 and 2. BM 957 at 10 nM, 28 at 100 nM and 2 at 30 nM all induce clear cleavage of PARP and activation of caspase-3 and have similar effects. Hence, the potencies for these three compounds in induction of cleavage of PARP and activation of caspase-3 in the H146 cells are consistent with their potencies in induction of cell death[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1391107-54-2
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Molecular Weight 1065.68
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Formel C52H56ClF3N6O7S3
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SMILES
O=C(C1=C(C)N(CC)C(C2=CC=C(Cl)C=C2)=C1C3=CC=CC(N4CCN(C5=CC=C(NS(=O)(C6=CC=C(N[C@H](CCN7CCC(O)CC7)CSC8=CC=CC=C8)C(S(=O)(C(F)(F)F)=O)=C6)=O)C=C5)CC4)=C3)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
Two cancer cell lines (H1417 and H146 cell lines) are used. Induction of cell death by compounds (e.g., BM 957) in the H146 cell line. Cells are treated with different concentrations of the compounds (e.g., BM 957: 10, 30, 100 nM) for 24 hr. Cell viability is determined using a trypan blue exclusion assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Induction of cleavage of PARP and caspase-3 in H146 xenograft tumors by compounds 28 and BM 957. SCID mice bearing H146 xenograft tumors (100-200 mm3) are treated with vehicle control, single dose of 28 (50 mg/kg, i.v.) or BM 957 (25 mg/kg, i.v.). SCID mice bearing xenograft tumors (100 mm3) are treated with vehicle control, compound 28 at 50 mg/kg, i.v. or BM 957 at 25 mg/kg, i.v., daily, 5 days a week for two weeks. The tumor growth inhibition for both compounds is statistically highly significant with p=0.0033 for compound 28 versus vehicle control and p=0.0006 for BM 957 versus vehicle control, respectively, when the mean tumor volume reaches 750 mm3 in the vehicle treated group in both experiments[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)