MPD-1
MPD-1 (Maleimide-KGDEVD-doxorubicin) is a peptide drug conjugate (PDC). MPD-1 releases Doxorubicin (HY-15142) via radiation-activated caspase-3 cleavage, triggering a cytotoxic amplification cascade at the tumor site. MPD-1 enhances CD8+ T cell tumor infiltration, and activates antigen-presenting cells. MPD-1 enables dual-trigger payload release, amplifies cytotoxicity via in situ feedback, and selectively delivers payload to tumor microenvironments via enhanced albumin metabolism and macropinocytosis. MPD-1 exhibits antitumor efficacy in mouse colorectal cancer models. MPD-1 can be used for the research of colorectal cancer.
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- CAS No.: 1911555-88-8
- 화학식: C73H90N10O29
- 분자량:1571.55
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
MPD-1 (25-50 μM; 24 h) induces immunogenic cell death of mouse colorectal CT26.CL25 cancer cells when combined with 2 Gy radiation or activated by caspase-3 protein, as evidenced by 2.5-fold higher surface calreticulin and 8.6-fold higher extracellular HMGB1 levels compared to control[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:mouse colorectal CT26.CL25 cancer cells
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Concentration:0; 25; 50 μM
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Incubation Time:24 h
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Result:Increased HMGB1 levels in the cell lysate and supernatant in a dose-dependent manner.
Increased HSP70 levels in the cell lysate at 50 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (7-8 weeks old) subcutaneously implantated with CT26.CL25 colon carcinoma cells[2]
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Dosage:5 mg/kg
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Administration:i.v.; every other day; 4 doses
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Result:Induced a 2.5-fold increase in calreticulin mean fluorescence intensity (MFI) and a 5.3-fold increase in HMGB1-positive tumor tissue fraction compared to control.
Increased tumor-infiltrating lymphocytes (CD45+ cells).
Increased activation markers (CD40, CD80, CD86, CD103) on tumor dendritic cells (CD11c+).
Increased β-galactosidase (tumor antigen) MFI by 3.1-fold on CD11c+MHCII+ cells and 4.4-fold on CD11b+MHCII+ cells in tumors compared to control.
Increased β-galactosidase MFI by 4.8-fold on CD11c+MHCII+ cells and 4.1-fold on CD11b+MHCII+ cells in tumor-draining lymph nodes compared to control.
Showed negligible immune-related toxicity, with no significant reduction in lymph node/spleen weight or CD45+CD3+, CD4+, CD8+ T cell populations in lymph nodes, spleens, or blood compared to control/radiation groups.
Achieved 95.2% tumor growth inhibition and induced tumor-specific IFNγ secretion (3.4-fold higher than MPD-1+RT alone) when combined with FS nanocage and RT.
Chemical Information
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CAS No. 1911555-88-8
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분자량 1571.55
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화학식 C73H90N10O29
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SMILES
[H][C@@]1(C[C@H](NC(OCC2=CC=C(NC([C@H](CC(O)=O)NC([C@H](C(C)C)NC([C@H](CCC(O)=O)NC([C@H](CC(O)=O)NC(CNC([C@H](CCCCNC(CCCCCN3C(C=CC3=O)=O)=O)NC(C)=O)=O)=O)=O)=O)=O)=O)C=C2)=O)[C@H](O)[C@H](C)O1)O[C@@H](C[C@](C(CO)=O)(CC4=C5O)O)C4=C(C(C(C6=C7OC)=O)=C5C(C6=CC=C7)=O)O
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Synonyms
Maleimide-KGDEVD-doxorubicin
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MPD-1 Related Classifications
Cat. No.: HY-183866
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- MPD-1
- 1911555-88-8
- Maleimide-KGDEVD-doxorubicin
- MPD1
- MPD 1
- Peptide-Drug Conjugates (PDCs)
- HSP
- IFNAR
- PARP inhibition
- dendritic cell
- cathepsin B
- microsatellite-stable colorectal cancer
- mKRAS-mutant colorectal cancer
- antigen-presenting cells
- CT26.CL25 cancer cells
- CD8+ T cell
- caspase-3/7
- PTEN-loss non-small cell lung cancer
- Inhibitor
- inhibitor
- inhibit