CA IX/VEGFR-2-IN-2
CA IX/VEGFR-2-IN-2 (compound 5e) is a dual-targeted inhibitor. CA IX/VEGFR-2-IN-2 shows strong inhibitory effects on both CA IX (Ki=3.1 μM) and VEGFR-2 (IC50=32.1 nM). CA IX/VEGFR-2-IN-2 can be used for the study of pancreatic (PANC1), breast cancer (MCF7) and prostate cancer (PC3) .
For research use only. We do not sell to patients.
- Formula: C22H18FN3O3S
- Molecular Weight:423.46
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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VEGFR-2 32.1 nM (IC50) |
CA IX 3.1 μM (Ki) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
1.4 μM
Compound: 5e
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Cytotoxicity against human MCF7 cells under hypoxia condition by MTT assay
Cytotoxicity against human MCF7 cells under hypoxia condition by MTT assay
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[PMID: 38642371] |
| PANC-1 | IC50 |
1.04 μM
Compound: 5e
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Cytotoxicity against human PANC-1 cells under hypoxia condition by MTT assay
Cytotoxicity against human PANC-1 cells under hypoxia condition by MTT assay
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[PMID: 38642371] |
| PC-3 | IC50 |
5.03 μM
Compound: 5e
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Cytotoxicity against human PC-3 cells under hypoxia condition by MTT assay
Cytotoxicity against human PC-3 cells under hypoxia condition by MTT assay
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[PMID: 38642371] |
| Vero | IC50 |
34.88 μM
Compound: 5e
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Cytotoxicity against African green monkey Vero cells under hypoxic condition by MTT assay
Cytotoxicity against African green monkey Vero cells under hypoxic condition by MTT assay
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[PMID: 38642371] |
CA IX/VEGFR-2-IN-2 (compound 5e) has the sequence of the selectivity toward the responsive tumor cells is PANC1, then MCF7 and PC3, and decreases PANC1 cell migration[1].
CA IX/VEGFR-2-IN-2 (compound 5e) induces up-regulation of p53, BAX, cytochrome C and caspases 3, 8, 9, and down-regulation of Bcl-2 gene in pancreatic cancer cells[1].
CA IX/VEGFR-2-IN-2 (compound 5e) suppresses the HIF-1α from 6.1±0.13 to 3.7±0.09 ng/mL by more than 1.5-fold in PANC1 cells[1].
CA IX/VEGFR-2-IN-2 (compound 5e) is responsible for more than a 3.5-fold rise in the quantity of ROS to blame for seen cell cycle halt, or apoptosis, in PANC1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PANC1 , MCF7 and PC3 cell lines
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Concentration:
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Incubation Time:
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Result:Had a better growthinhibition effect on PANC1 and MCF7 cell lines, with IC50 values of 1.04 μM and 1.40 μM, had lower inhibitory effects against PC3, with an IC50 greater than 5 μM.
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Cell Line:PANC1 cell lines
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Concentration:
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Incubation Time:24 h
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Result:Increased the early apoptosis ratio from 0.37% (DMSO) to 21.39%, as did the late apoptosis ratio from 0.18 → 11.11.
CA IX/VEGFR-2-IN-2 (compound 5e) (5 and 10 mg/kg, ip.; 2 weeks) at a dosage of 10 mg/kg leads to additional decreases in the concentrations of VEGF, MMP-2, and MMP-9 in female Swiss albino mice[1].
CA IX/VEGFR-2-IN-2 (compound 5e) (5 and 10 mg/kg, ip.; 2 weeks) at a dosage of 5 mg/kg leads to the formation of necrotic regions interspersed with distinct neoplastic cells and at a dosage of 10 mg/kg displays marked improvement, and diffuse and wide areas of necrosis were replaced in the muscle bundles with a marked decline in the quantity of neoplastic cells, indicating a substantial inhibition in viable tumor cells in female Swiss albino mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:solid Ehrlich carcinoma (SEC)
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Dosage:5 and 10 mg/kg
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Administration:
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Result:Led to a 47.28% decrease in tumor volume and a 55.42% decrease in tumor weight at a dose of 5 mg/kg compared to the solid Ehrlich carcinoma.
Led to a 65.88% reduction in the volume of the tumor and a 75.71% decrease in tumor weight at a dose of 10 mg/kg relative to the control group of SEC.
Chemical Information
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Molecular Weight 423.46
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Formula C22H18FN3O3S
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SMILES
O=C1C(/C(C)=N/NC2=NC(C3=CC=C(F)C=C3)=CS2)=CC4=C(O1)C(OCC)=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CA IX/VEGFR-2-IN-2 Related Classifications
HY-158328A Related Classifications
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