Cat. No.: HY-118032

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.

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

CAS No.: 1207993-83-6
Formula: C₂₀H₁₄Cl₂N₆O₅S
Molecular Weight:521.33

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (290 KB)

Bozepinib Chemical Structure

CAS No.: 1207993-83-6

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

HER2

All JNK Isoforms :

All ERK Isoforms :

All EGFR Isoforms :

Cellular Effect

Cell Line	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.	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.	24946763
T84	IC50	1.019 μM	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.	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.	24946763
SW480	IC50	0.235 μM	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.	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.	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.	24946763
CCD-18Co	IC50	2.012 μM	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.	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.	24194639
MCF7	IC50	0.78 μM	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	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.	24194639
MCF7	IC50	0.44 μM	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.	24194639
HCT-116	IC50	0.31 μM	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.	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.

Cell Viability Assay^[2]

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)
Concentration:

dose range
Incubation Time:

6 days
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).

Western Blot Analysis^[2]

Cell Line:

SKBR-3, MCF-7, MDA-MB 468, MCF-10A human breast cell lines
Concentration:

5 μM
Incubation Time:

2 h, 4 h, 8 h, 16 h
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.

Western Blot Analysis^[3]

Cell Line:

human breast cancer MCF-7 cells, human colon cancer HCT-116 cells
Concentration:

5 µM
Incubation Time:

4 h, 8 h, 16 h, 24 h
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 exhibits in vivo anti-tumor and anti-metastatic activities in nude mouse xenograft models without subacute toxicity^[1].
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.

Animal Model:

BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of MDA-MB 468 human breast cancer cells)^[2]
Dosage:

25 mg/kg
Administration:

i.p.; three times a week; 45 days
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.

Animal Model:

BALB/c nude (female, 6-8 weeks old, subcutaneous xenograft of HT-29 human colon cancer cells)^[2]
Dosage:

25 mg/kg
Administration:

i.p.; three times a week; two weeks
Result:

Significantly reduced tumor volume from day 3 post-injection onward compared to control mice.

Animal Model:

BALB/c (female, 6 weeks old)^[2]
Dosage:

100 mg/kg
Administration:

i.p.; twice a week; 29 days
Result:

Caused no weight loss, unusual behavior, or histopathologic damage to liver or kidneys.

Chemical Information

CAS No. 1207993-83-6
Molecular Weight 521.33
Formula C₂₀H₁₄Cl₂N₆O₅S
SMILES

O=S(N1CC(OCC2=CC=CC=C21)N3C=NC4=C3N=C(N=C4Cl)Cl)(C5=CC=C(C=C5)[N+]([O-])=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Morales F, et al. p-Nitrobenzenesulfonamides and their fluorescent dansylsulfonamides derived from N-alkylated o-(purine-methyl) anilines as novel antitumour agents[J]. RSC advances, 2015, 5(93): 76615-76619.

[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]

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How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Bozepinib

All JNK Isoforms

All ERK Isoforms

All EGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Bozepinib Related Classifications

HY-118032 Related Classifications

Bioz