S-531011
Based on 1 Customer Validation
S-531011 is a high-affinity, selective, and reversible CCR8 ligand with antibody-dependent cellular cytotoxicity (ADCC) against CCR8-expressing cells. S-531011 induces the death of tumor-infiltrating CCR8+ regulatory T cells while preserving regulatory T cells in peripheral blood, thereby reinvigorating anti-tumor immunity. The combination of S-531011 with anti-PD-1 antibody effectively inhibits tumor growth, and S-531011 can be used for research on advanced solid tumors and various cancers including non-small cell lung cancer, ovarian cancer, colon cancer, breast cancer, and pancreatic ductal adenocarcinoma.
For research use only. We do not sell to patients.
- Purity: 98.38%
- Molecular Weight:148.11 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
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CCR8 18.6 pM (Kd) |
S-531011 binds to CCR8 with an in vitro-measured association rate constant of 11.9 L/nmol/hr and a calculated dissociation rate constant of 6.65 1/hr[2].
S-531011 (0.08-0.3 nmol/L; overnight) binds specifically and with high affinity to human CCR8 (Kd = 18.6 pmol/L) and its CCR8A27G variant (Kd = 26.4 pmol/L) expressed on HEK293T cells, with no cross-reactivity to other tested receptors[3].
S-531011 (up to 300 μg/mL; 2 hours) lacks CDC activity against Ramos-hCCR8 cells, with no measurable EC50 at concentrations up to 300 μg/mL[3].
S-531011 (0.001-10 μg/mL; overnight) selectively depletes tumor-infiltrating Tregs, but not Tconv cells, in human NSCLC and ovarian cancer tissues via ADCC, whereas Mogamulizumab (HY-P99253) depletes both populations[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
S-531011 (100 μg/mouse; i.v.; 2 doses (days 5 and 12 post tumor inoculation)) induces potent antitumor activity in EMT6 tumor-bearing hCCR8 KI mice, with significantly greater tumor volume reduction than vehicle or anti-mouse PD-1 antibody treatment[3].
S-531011 (10 mg/kg; i.v.; single dose (day 5 post tumor inoculation)) enhances the antitumor activity of anti-mouse PD-1 antibody in CT26.WT tumor-bearing hCCR8 KI mice without observable adverse effects[3].
S-531011 (0.05-5 mg/kg; i.v.; single dose (day 8 post tumor inoculation)) induces dose-dependent depletion of tumor-infiltrating CCR8+ Tregs in CT26.WT tumor-bearing hCCR8 KI mice, with effects lasting at least 7 days after a single dose[3].
S-531011 (0.05-0.5 mg/kg; i.v.; single dose (day 8 post tumor inoculation)) induces dose-dependent depletion of tumor-infiltrating CCR8+ Tregs in Colon26 tumor-bearing hCCR8 KI mice 4 days after a single dose[3].
S-531011 (0.05-0.5 mg/kg; i.v.; single dose (day 8 post tumor inoculation)) induces dose-dependent depletion of tumor-infiltrating CCR8+ Tregs in EMT6 tumor-bearing hCCR8 KI mice 4 days after a single dose[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:humanized CCR8 knock-in (hCCR8 KI) (female, CT26.WT colorectal cancer cells subcutaneously implanted)[3]
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Dosage:0.15 mg/kg; 0.5 mg/kg; 1.5 mg/kg; 5 mg/kg; 15 mg/kg
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Administration:i.v.; 2 doses (days 4 and 11 post tumor inoculation)
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Result:Reduced tumor volumes significantly in the 0.15, 5, and 15 mg/kg groups compared with isotype control antibody group (P < 0.05, P < 0.001, P < 0.001, respectively, on day 19 after inoculation).
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Animal Model:humanized CCR8 knock-in (hCCR8 KI) (female, EMT6 mammary carcinoma cells subcutaneously implanted)[3]
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Dosage:100 μg/mouse
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Administration:i.v.; 2 doses (days 5 and 12 post tumor inoculation)
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Result:Reduced tumor volumes significantly compared with vehicle control group (P < 0.0001) and anti-mouse PD-1 antibody-treated group (P < 0.05) on day 28 after implantation.
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Animal Model:humanized CCR8 knock-in (hCCR8 KI) (female, CT26.WT colorectal cancer cells subcutaneously implanted)[3]
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Dosage:10 mg/kg
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Administration:i.v.; single dose (day 5 post tumor inoculation)
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Result:Suppressed tumor volume significantly when combined with anti-mouse PD-1 antibody compared with S-531011 alone (P < 0.05) on day 21 after inoculation.
Caused no reduction in body weight or worsening of general condition.
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Animal Model:humanized CCR8 knock-in (hCCR8 KI) (female, CT26.WT colorectal cancer cells subcutaneously implanted)[3]
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Dosage:0.05 mg/kg; 0.5 mg/kg; 5 mg/kg
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Administration:i.v.; single dose (day 8 post tumor inoculation)
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Result:Reduced the proportion of CCR8+ Tregs relative to total Tregs in a dose-dependent manner at 4 and 7 days post-administration (P < 0.001 and P < 0.0001 for all doses vs. isotype control).
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Animal Model:humanized CCR8 knock-in (hCCR8 KI) (female, Colon26 colorectal cancer cells subcutaneously implanted)[3]
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Dosage:0.05 mg/kg; 0.5 mg/kg
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Administration:i.v.; single dose (day 8 post tumor inoculation)
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Result:Reduced the proportion of CCR8+ Tregs relative to total Tregs in a dose-dependent manner (P < 0.05 for 0.05 mg/kg, P < 0.01 for 0.5 mg/kg vs. saline) 4 days after administration.
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Animal Model:humanized CCR8 knock-in (hCCR8 KI) (female, EMT6 mammary carcinoma cells subcutaneously implanted)[3]
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Dosage:0.05 mg/kg; 0.5 mg/kg
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Administration:i.v.; single dose (day 8 post tumor inoculation)
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Result:Reduced the proportion of CCR8+ Tregs relative to total Tregs in a dose-dependent manner (P < 0.05 for 0.05 mg/kg, P < 0.01 for 0.5 mg/kg vs. saline) 4 days after administration.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
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IgG1-kappa
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Product Image
ELISA, FACS, Functional assay
Chemical Information
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Appearance Liquid
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Molecular Weight 148.11 kDa
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Color Colorless to light yellow
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SMILES
[S-531011]
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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 (267 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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
S-531011 Related Classifications
HY-P991481 Related Classifications
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