huATN-658
Based on 1 Customer Validation
huATN-658 is an inhibitor that specifically targets the DIII domain of human urokinase plasminogen activator receptor (uPAR). huATN-658 neutralizes uPAR function by blocking the interaction between uPAR and integrins, without interfering with the binding of uPA or vitronectin to uPAR. huATN-658 inhibits the proliferation and invasion of breast cancer cells, slows the growth of primary breast tumors, reduces breast cancer-induced bone lesions and decreases osteoclast activity. huATN-658 also alters the gene expression of the TGF-β receptor complex signaling pathway. huATN-658 exerts synergistic anticancer effects when combined with Zoledronic Acid (HY-13777), and does not cause physiological or behavioral abnormalities in immunodeficient mice. huATN-658 can be used in research related to breast cancer, metastatic breast cancer and breast cancer-induced bone disease.
For research use only. We do not sell to patients.
- Purity: 99.67%
- Molecular Weight:146.34 kDa
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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
Human IgG1 kappa
Human
PLAUR/uPAR/CD87
huATN-658 (50 μg/mL; 48 h) significantly inhibits the proliferation of human breast cancer cell lines MDA-MB-231 and Hs578T in vitro, but exerts no such effect on MDA-BoM-1833 cells[1].
huATN-658 (50 μg/mL; 18 h) significantly inhibits the invasion of human breast cancer cell lines MDA-MB-231, Hs578T and MDA-BoM-1833 in vitro[1].
huATN-658 (50 μg/mL) alters the transcriptome of human breast cancer MDA-MB-231 cells in vitro, and differentially regulates 61 genes, among which the most highly enriched pathway is the TGF-β receptor complex signaling pathway[1].
huATN-658 effectively inhibits invasion, migration and proliferation of human prostate cancer cells in vitro[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231, Hs578T, MDA-BoM-1833
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Concentration:50 μg/mL
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Incubation Time:48 h
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Result:Caused a significant reduction in proliferation of MDA-MB-231 and Hs578T cells compared with control IgG-treated cells.
Showed no significant effect on proliferation of MDA-BoM-1833 cells compared with control IgG-treated cells.
huATN-658 (10 mg·kg-1; intraperitoneal; twice a week; 10 weeks) significantly reduces skeletal lesion progression, osteoclast number, and tumor cell proliferation in female CD-1 nude mice with intratibial MDA-MB-231 xenografts[1].
huATN-658 (10 mg·kg-1; intraperitoneal; twice a week; 6 weeks) reduces skeletal lesion development in female CD-1 nude mice with intratibial MDA-BoM-1833 xenografts[1].
huATN-658 causes a significant reduction in primary breast tumor growth in immunocompromised mice bearing MDA-MB-231 breast cancer xenografts[2].
huATN-658 significantly reduces breast cancer-induced skeletal lesions and intratumoral bone microenvironment growth in immunocompromised mice, with enhanced efficacy when combined with zoledronic acid[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CD-1 nude mice (female, intratibial xenograft model)[1]
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Dosage:10 mg·kg-1
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Administration:intraperitoneal; twice a week; 10 weeks
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Result:Significantly reduced the progressive increase in skeletal lesion area over time compared with controls, as measured by radiologic assessment.
Reduced the rate of skeletal lesion development to 57% at week 10 post-inoculation (vs.
100% of controls).
Caused a 68% decrease in osteoclast number compared with controls.
Significantly reduced the percentage of Ki67-positive tumor cells compared with controls.
Confirmed reduced tumor burden in tibias via histological analysis.
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
ELISA, FACS, Functional assay
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Flow Cytometry analysis of Hela cells with huATN-658 (HY-P990552A, red). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then cells were stained with the primary antibody at 1/200 dilution for an hour at 4℃. Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa(HY-P99001, blue) was used as the isotype control, cells without incubation with primary antibody were used as the unlabeled control (black). -
Immobilized huuPAR-Fc can bind huATN-658. The EC50 for this effect is 51.98 ng/mL.
Chemical Information
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Appearance Liquid
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Molecular Weight 146.34 kDa
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Color Colorless to light yellow
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SMILES
[huATN658]
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Shipping
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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Data Sheet (262 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Inhibitory Antibodies User Guide (603 KB)
References
[1]. Mahmood N, et al. uPAR antibody (huATN-658) and Zometa reduce breast cancer growth and skeletal lesions. Bone Res. 2020;8:18. Published 2020 Apr 17. [Content Brief]
[2]. Mahmood N, et al. Fibrinolytic System and Cancer: Diagnostic and Therapeutic Applications. Int J Mol Sci. 2021;22(9):4358. Published 2021 Apr 22. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
huATN-658 Related Classifications
HY-P990552A Related Classifications
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