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.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.67%
- 분자량:146.34 kDa
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보관:Shipping with dry ice
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
제품 설명
Isotype
Human IgG1 kappa
Recommend Isotype Controls
Species Reactivity
Human
IC50 & Target
PLAUR/uPAR/CD87
In Vitro
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.
In Vivo
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.
Gene ID
Accession
Conjugated
Unconjugated
Reconsititution
The product can be reconstituted/diluted with sterile PBS or saline.
신청
ELISA, FACS, Functional assay
Verified Bioactivity
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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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분자량 146.34 kDa
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Color Colorless to light yellow
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SMILES
[huATN658]
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선적
Shipping with dry ice.
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Formulation
Please refer to the lot-specific COA for specific buffer information.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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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)