1. Apoptosis
  2. Bcl-2 Family
    Apoptosis
  3. BM-1074

BM-1074 

Cat. No.: HY-13846
Handling Instructions

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.

For research use only. We do not sell to patients.

BM-1074 Chemical Structure

BM-1074 Chemical Structure

CAS No. : 1391108-10-3

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Description

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[1].

IC50 & Target[1]

Bcl-2

1.8 nM (IC50)

Bcl-xL

6.9 nM (IC50)

In Vitro

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].

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

Cell Proliferation Assay[1]

Cell Line: H146, H1963, H187, and H1417
Concentration: 0-200 nM
Incubation Time: 4 days
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.
In Vivo

BM-1074 (i.v., 15 mg/kg, daily, 5 days a week for 2 weeks) exhibits the maximum tolerated dose (MTD) (15 mg/kg) and strong antitumor activity in H146 tumor xenograft mice, as well as shows no significant weight loss (<5%) or other signs of toxicity[1].
BM-1074 (i.v., 15 mg/kg, single) induces strong apoptosis in H146 tumor tissues[1].

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

Animal Model: SCID mice (injected with 5 x 106 H146 cancer cells with Matrigel, subcutaneously)[1]
Dosage: 15 mg/kg
Administration: i.v., 15 mg/kg, daily, 5 days a week for 2 weeks
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.
Animal Model: SCID mice (injected with 5 x 106 H146 cancer cells with Matrigel, subcutaneously)[1]
Dosage: 15 mg/kg
Administration: i.v., 15 mg/kg, single dosage
Result: Induced robust cleavage of PARP and caspase-3 at both 3 and 6-hr time-points in H146 tumor tissues.
Molecular Weight

1013.69

Formula

C50H57ClN8O7S3

CAS No.
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[[email protected]](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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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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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.

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BM-1074
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HY-13846
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