1391108-10-3
1391108-10-3 structure
- Name: BM-1074
- Chemical Name: (E)-2-methyl-3-[3-(trifluoromethylsulfanyl)phenyl]prop-2-enoic ac id
- CAS Number: 1391108-10-3
- Molecular Formula: C11H9F3O2S
- Molecular Weight: 262.24800
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2016-06-24 10:40:56
- Modify Date: 2024-04-02 00:19:48
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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].
| Name | (E)-2-methyl-3-[3-(trifluoromethylsulfanyl)phenyl]prop-2-enoic ac id |
|---|
| 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]. |
|---|---|
| Related Catalog | |
| Target |
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]. 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 dosage) induces strong apoptosis in H146 tumor tissues[1]. 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. |
| References |
| Molecular Formula | C11H9F3O2S |
|---|---|
| Molecular Weight | 262.24800 |
| Exact Mass | 262.02800 |
| PSA | 62.60000 |
| LogP | 3.78640 |