PLT012
Based on 1 Customer Validation
PLT012 is a humanized IgG4 antibody targeting CD36. PLT012 inhibits the lipid-binding domain of CD36. PLT012 blocks CD36-mediated metabolic adaptation in regulatory T cells (Tregs) and CD8+ tumor-infiltrating lymphocytes (TILs), thereby inhibiting tumor growth and shifting the tumor microenvironment from immunosuppressive to immunosupportive. PLT012 reduces intratumoral Tregs, enhances CD8+ T cell infiltration and cytotoxic function, and increases the abundance of progenitor-exhausted T cells. PLT012 exerts robust antitumor activity and synergizes with anti-PD-L1 or standard-of-care regimens (anti-VEGF + anti-PD-L1). PLT012 can be used for hepatocellular carcinoma, colorectal cancer and solid tumor research.
For research use only. We do not sell to patients.
- Purity: 98.90%
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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
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CD36 |
PLT012 (0.001-100 μg/mL, 30 min) strongly inhibits the binding (IC50: 1.798nM) and uptake (IC50: 1.357nM) of fluorochrome-labeled oxidized low-density lipoprotein (oxLDL) in F293 cells (overexpress human CD36)[1].
PLT012 (5 mg/mL, 30 min) significantly represses oxLDL uptake in primary tumor-infiltrating immune cells, including myeloid cells, CD3+ T lymphocytes, and intratumoral Tregs isolated from MC38 tumor-bearing mice[1].
PLT012 can restore effector functions in exhausted T cells and induce CD8 T cell-mediated anti-HCC responses in isolated CD45+ tumor-infiltrating cells by using single-cell RNA sequencing (scRNA seq)[1].
PLT012 (2 days) effectively modulates the TME in HCCs by targeting CD36 in human HCC tumors, induces increase in CD8+ T cell percentage and GrB expression occurred in 45.4% of the patients[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
PLT012 (10 mg/kg, i.p. once) has the potential to restore anti-tumor immunity against HCC by targeting CD36-mediated immune regulations in CTNNB1N90/MYCOEHCC-bearing mice[1].
PLT012 (10 mg/kg, i.p., once every three days, 18 days) is capable of restoring anti-tumor responses in HCC and might also improve responsiveness to PD-1 blockade in the MYCOE/p53KO HCC mice model[1].
PLT012 (10 mg/kg, i.p., once every three days for 5 doses) remodels the immunosuppressive TME in β-catenin-mutant HCC, effectively activating anti-tumor T-cell immunity in CTNNB1N90/MYCOEHCC-bearing mice[1].
PLT012 () significantly enhances anti-tumor efficacy when combination with an anti-PD-L1 monoclonal antibody or anti-VEGF and anti-PD-L1, and achieved a >70% overall positive response rate and a 45% complete response rate when combinates with anti-PD-L1 and anti-VEGF in CTNNB1N90/MYCOEHCC-bearing mice[1].
PLT012 () restrains HCC progression under conditions of high dietary lipid intake in CTNNB1N90/MYCOE HCC-bearing mice, whether fed a standard chow diet (CD) or a high-fat Western (WD) diet[1].
PLT012 () reprograms the tumor immune microenvironment, thereby restricting colon cancer liver metastasis and enhancing sensitivity to PD-1 blockade in mice MC38 xenografts models[1].
PLT012 (0-200 mg/kg, once a week, for 5 weeks) is well-tolerated in non-human primates (cynomolgus monkeys)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (6 weeks) (received 12 μg of pT3-b-catenin, 12 μg of pT3-Myc_LucOVA plasmid, and 8 μg of SB100x)[1]
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Dosage:10 mg/kg
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Administration:i.p. once
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Result:Mainly accumulated in the liver, lung, intestine, epididymal white adipose tissue, and pancreas.
Showed average fluorescence intensity levels because of the presence of adipocytes and endothelial cells.
Significantly stronger in livers after 24 h.
Resulted a higher percentage of labeled cells in both Tregs and CD8+ T cells after persisted for 48 h.
Resulted a higher signal in NK cells at the 24 h but not at the 48 h.
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Animal Model:C57BL/6 mice (6 weeks) (received a total of 12 μg of pT3-Myc_LucOVA plasmid, 13.2 μg of p53 gRNA plasmid, and 4 μg of SB100x) [1]
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Dosage:10 mg/kg
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Administration:i.p. once every three days, 18 days
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Result:Inhibited the growth of MYCOE/p53KO HCC and led to complete tumor regression in 32% of tumor-bearing mice (this finding was further corroborated by measurements of tumor weight and ex vivo liver bioluminescence imaging).
Reduced serum alanine transaminase (ALT) activity.
Led to a reduction of Tregs and an increase of CD8+ T cells within the TME.
Resulted a higher CD8+ T/Tregs ratios.
Enhanced the abundance of CD8+ GrB+ T cells.
Resulted in an increase in both progenitor-exhausted T cells (Prog Tex, characterized by CD44+ PD-1+ TCF1+ Tim3-) and terminally exhausted T cells (Term Tex, characterized by CD44+ PD-1+ TCF1- Tim3+).
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Animal Model:C57BL/6 mice (6 weeks) (received 12 μg of pT3-b-catenin, 12 μg of pT3-Myc_LucOVA plasmid, and 8 μg of SB100x)[1]
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Dosage:10 mg/kg
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Administration:i.p. once every three days for 5 doses
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Result:Significantly inhibited tumor growth and markedly decreased circulating ALT levels.
Also increased the abundance of CD8+ T cells and decreased the proportion of Tregs, thereby resulting in increased ratios of CD8+ T cells to Tregs within individual tumors.
Increased the abundance of GrB-expressing CD8+ T cells as well as the population of Prog Tex and Term Tex CD8+ T cells.
Observed a stronger signal for GrB and cleaved caspase-3 in tumors.
Significantly enhanced the antigen-specific T cell response.
Increased frequencies of antigen-specific Prog Tex and Term Tex in CD8+ T cells.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
P16671-1
Unconjugated
The product can be reconstituted/diluted with sterile PBS or saline.
ELISA, FACS, Functional assay
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Immobilized hu-CD36-ECD-His can bind PLT012. The EC50 for this effect is 14.04 ng/mL.
Chemical Information
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Appearance Liquid
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Color Colorless to light yellow
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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 (266 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)
PLT012 Related Classifications
HY-P991911 Related Classifications
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