Bozepinib
Bozepinib is an anticancer agent. Bozepinib induces Apoptosis, and inhibits the HER-2 signaling pathway as well as JNK and ERK kinases. Bozepinib induces the down-regulation of c-MYC, β-catenin and SOX2 proteins, and the up-regulation of GLI-3. Bozepinib can be used in the research of breast cancer and colon cancer.
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- CAS No.: 1207993-83-6
- Formule: C20H14Cl2N6O5S
- Masse moléculaire:521.33
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
HER2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
0.355 μM
|
Antiproliferative activity against human breast cancer MCF-7 cells.
Antiproliferative activity against human breast cancer MCF-7 cells.
|
p-Nitrobenzenesulfonamides-and-their-fluorescent |
| MDA-MB-231 | IC50 |
0.166 μM
|
Antiproliferative activity against human MDA-MB 231 breast cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against human MDA-MB 231 breast cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
|
24946763 |
| MDA-MB-468 | IC50 |
0.850 μM
|
Antiproliferative activity against human MDA-MB 468 breast cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against human MDA-MB 468 breast cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
|
24946763 |
| SK-BR-3 | IC50 |
0.330 μM
|
Antiproliferative activity against human SKBR-3 breast cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against human SKBR-3 breast cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
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24946763 |
| Caco-2 | IC50 |
0.631 μM
|
Antiproliferative activity against human Caco-2 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against human Caco-2 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
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24946763 |
| T84 | IC50 |
1.019 μM
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Antiproliferative activity against human T-84 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against human T-84 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
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24946763 |
| HT-29 | IC50 |
1.352 μM
|
Antiproliferative activity against human HT-29 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against human HT-29 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
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24946763 |
| SW480 | IC50 |
0.235 μM
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Antiproliferative activity against human SW-480 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against human SW-480 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
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24946763 |
| HCT-116 | IC50 |
0.570 μM
|
Antiproliferative activity against human HCT-116 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against human HCT-116 colon cancer cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
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24946763 |
| MCF-10A | IC50 |
1.825 μM
|
Antiproliferative activity against non-tumor human MCF-10A breast cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against non-tumor human MCF-10A breast cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
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24946763 |
| CCD-18Co | IC50 |
2.012 μM
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Antiproliferative activity against non-tumor human CCD-18Co colon cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
Antiproliferative activity against non-tumor human CCD-18Co colon cells assessed as reduction in cell viability incubated for a total of 6 days by sulforhodamine-B assay.
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24946763 |
| RKO | IC50 |
0.13 μM
|
Antiproliferative activity against human colon cancer RKO cells assessed by Sulforhodamine-B cell survival assay with a total 6-day single-agent treatment.
Antiproliferative activity against human colon cancer RKO cells assessed by Sulforhodamine-B cell survival assay with a total 6-day single-agent treatment.
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24194639 |
| MCF7 | IC50 |
0.78 μM
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Antiproliferative activity against human breast cancer MCF-7 cells assessed by Sulforhodamine-B cell survival assay with a total 6-day single-agent treatment.
Antiproliferative activity against human breast cancer MCF-7 cells assessed by Sulforhodamine-B cell survival assay with a total 6-day single-agent treatment.
|
24194639 |
| HCT-116 | IC50 |
0.48 μM
|
Antiproliferative activity against human colon cancer HCT-116 cells assessed by Sulforhodamine-B cell survival assay with a total 6-day single-agent treatment.
Antiproliferative activity against human colon cancer HCT-116 cells assessed by Sulforhodamine-B cell survival assay with a total 6-day single-agent treatment.
|
24194639 |
| RKO | IC50 |
0.09 μM
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Antiproliferative activity against human colon cancer RKO cells assessed by Sulforhodamine-B cell survival assay with a total 6-day treatment combined with 50 IU/mL interferon alpha.
Antiproliferative activity against human colon cancer RKO cells assessed by Sulforhodamine-B cell survival assay with a total 6-day treatment combined with 50 IU/mL interferon alpha.
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24194639 |
| MCF7 | IC50 |
0.44 μM
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Antiproliferative activity against human breast cancer MCF-7 cells assessed by Sulforhodamine-B cell survival assay with a total 6-day treatment combined with 50 IU/mL interferon alpha.
Antiproliferative activity against human breast cancer MCF-7 cells assessed by Sulforhodamine-B cell survival assay with a total 6-day treatment combined with 50 IU/mL interferon alpha.
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24194639 |
| HCT-116 | IC50 |
0.31 μM
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Antiproliferative activity against human colon cancer HCT-116 cells assessed by Sulforhodamine-B cell survival assay with a total 6-day treatment combined with 50 IU/mL interferon alpha.
Antiproliferative activity against human colon cancer HCT-116 cells assessed by Sulforhodamine-B cell survival assay with a total 6-day treatment combined with 50 IU/mL interferon alpha.
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24194639 |
In Vitro
Bozepinib induces apoptosis in breast and colon cancer cells via double-stranded RNA-dependent protein kinase (PKR), and IFNα enhances this apoptotic effect while promoting autophagy and senescence[1].
Bozepinib (at low micromolar concentrations) inhibits cancer stem cell activity, suppresses the formation of mammospheres and colonospheres, eliminates the ALDH+ CSC subpopulation, and regulates key CSC pathway proteins in breast cancer and colon cancer models[1].
Bozepinib (6 days) potently inhibits the proliferation of MCF-7, MDA-MB 231, MDA-MB 468, SKBR-3, Caco-2, T-84, HT-29, SW-480 and HCT-116 cancer cells, with IC50 values ranging from 0.166 μM to 1.352 μM. Meanwhile, compared with non-tumor cells MCF-10A and CCD-18Co, this compound exhibits selective activity against cancer cells, with a maximum selectivity index of 11[2].
Bozepinib (50 μM) inhibits a variety of cancer-related kinases, including JNK, ERKs, HER2, AKT2 and VEGF receptors, in cell-free multikinase screening assays[2].
Bozepinib (5 μM; 2-16 h) inhibits the phosphorylation of HER2, AKT, JNK and ERK1/2 and reduces VEGF levels in SKBR-3, MCF-7 and MDA-MB 468 breast cancer cells, while exerting minimal effects on non-tumorigenic MCF-10A cells[2].
Bozepinib (0.01-5 μM; 4-8 h) dose-dependently inhibits capillary-like structure formation in HUVEC cells at 4 h and 8 h, while maintaining high cell viability and inducing extremely low levels of apoptosis[2].
Bozepinib (0.2-5 μM; 48 h) inhibits the migration of SKBR-3 breast cancer cells and HCT-116 colon cancer cells in a dose-dependent manner in scratch wound healing assays, with a treatment duration of 48 h[2].
Bozepinib (4-16 h) alters gene expression in MDA-MB 468 breast cancer cells. After 4 h and 16 h of exposure, it upregulates antiproliferative and antiangiogenic genes, while downregulating oncogenes and cell cycle-related genes[2].
Bozepinib potently inhibits the proliferation of breast adenocarcinoma MDA-MB-231 cells, with an IC50 of 0.166 µM[3].
Bozepinib (5 µM; 4-24 h) upregulates and activates PKR, induces eIF2α phosphorylation, but has no effect on the expression or phosphorylation of p53 in breast cancer MCF-7 cells and colon cancer HCT-116 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human breast cancer cell lines (MCF-7, MDA-MB 231, MDA-MB 468, SKBR-3), human colon cancer cell lines (Caco-2, T-84, HT-29, SW-480, HCT-116), non-tumor cell lines (MCF-10A, CCD-18Co)
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Concentration:dose range
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Incubation Time:6 days
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Result:Exhibited selective antiproliferative activity with IC50 values: MCF-7 (0.355 μM), MDA-MB 231 (0.166 μM), MDA-MB 468 (0.850 μM), SKBR-3 (0.330 μM), Caco-2 (0.631 μM), T-84 (1.019 μM), HT-29 (1.352 μM), SW-480 (0.235 μM), HCT-116 (0.570 μM), MCF-10A (1.825 μM), CCD-18Co (2.012 μM).
Showed selectivity indices ranging from 1.48 (HT-29) to 11 (MDA-MB 231).
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Cell Line:SKBR-3, MCF-7, MDA-MB 468, MCF-10A human breast cell lines
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Concentration:5 μM
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Incubation Time:2 h, 4 h, 8 h, 16 h
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Result:Completely inhibited phosphorylated HER2 after 2 h, inhibited phosphorylated AKT, and decreased total VEGF levels over time in SKBR-3 cells.
Inhibited phosphorylated JNK and ERK1/2 starting at 4 h, with greater inhibition at later time points in MCF-7 cells.
Inhibited phosphorylated JNK and ERK1/2 starting at 8 h in MDA-MB 468 cells.
Weakly up-regulated phosphorylated ERK1/2 at 8 h and returned to control levels by 16 h, while phosphorylated JNK was undetectable in non-tumor MCF-10A cells.
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Cell Line:human breast cancer MCF-7 cells, human colon cancer HCT-116 cells
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Concentration:5 µM
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Incubation Time:4 h, 8 h, 16 h, 24 h
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Result:Increased phosphorylation of PKR and its substrate eIF2α in both MCF-7 and HCT-116 cells.
Increased total PKR protein levels, more notably in HCT-116 cells.
Left levels of total p53 and phosphorylated p53 unchanged in both cell lines.
In Vivo
Bozepinib (25 mg/kg; i.p.; three times per week; for 45 consecutive days) inhibits the growth of MDA-MB 468 breast cancer xenografts in BALB/c nude mice and reduces the incidence of lung metastasis to 16.6%[2].
Bozepinib (25 mg/kg; i.p.; three times per week; for 2 consecutive weeks) inhibits the growth of HT-29 colon cancer xenografts in BALB/c nude mice[2].
Bozepinib (100 mg/kg; i.p.; twice weekly; for 29 consecutive days) causes no subacute toxicity in female BALB/c mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of MDA-MB 468 human breast cancer cells)[2]
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Dosage:25 mg/kg
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Administration:i.p.; three times a week; 45 days
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Result:Reduced average tumor volume to approximately 30 mm3 by day 45, compared to 150 mm3 in control mice.
Reduced lung metastasis incidence to 16.6%, compared to 83.3% in control mice.
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Animal Model:BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of HT-29 human colon cancer cells)[2]
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Dosage:25 mg/kg
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Administration:i.p.; three times a week; two weeks
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Result:Significantly reduced tumor volume from day 3 post-injection onward compared to control mice.
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Animal Model:BALB/c (female, 6 weeks old)[2]
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Dosage:100 mg/kg
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Administration:i.p.; twice a week; 29 days
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Result:Caused no weight loss, unusual behavior, or histopathologic damage to liver or kidneys.
Chemical Information
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CAS No. 1207993-83-6
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Masse moléculaire 521.33
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Formule C20H14Cl2N6O5S
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SMILES
O=S(N1CC(OCC2=CC=CC=C21)N3C=NC4=C3N=C(N=C4Cl)Cl)(C5=CC=C(C=C5)[N+]([O-])=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[2]. Ramírez A, et al. HER2-signaling pathway, JNK and ERKs kinases, and cancer stem-like cells are targets of Bozepinib small compound. Oncotarget. 2014 Jun 15;5(11):3590-606. [Content Brief]
[3]. Marchal JA, et al. Bozepinib, a novel small antitumor agent, induces PKR-mediated apoptosis and synergizes with IFNα triggering apoptosis, autophagy and senescence. Drug design, development and therapy. 2013;7:1301-13. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Bozepinib Related Classifications
HY-118032 Related Classifications
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