PEG9MA10-PAB10-GalMA10
PEG9MA10-PAB10-GalMA10 is a CD147 LYTAC degrader. PEG9MA10-PAB10-GalMA10 binds to the asialoglycoprotein receptor (ASGPR) via its galactose methacrylate domain, mediating its uptake by hepatoma cells. PEG9MA10-PAB10-GalMA10 induces lysosome-dependent degradation of CD147, resulting in concurrent loss of associated MCT1 and MCT4. PEG9MA10-PAB10-GalMA10 reduces extracellular lactate levels, increases intracellular lactate accumulation, inhibits glycolytic activity, and enhances mitochondrial respiratory capacity. PEG9MA10-PAB10-GalMA10 decreases the secretion of MMP-2 and MMP-9, and upregulates the expression of E-cadherin. PEG9MA10-PAB10-GalMA10 exhibits anti-tumor efficacy in hepatoma models. PEG9MA10-PAB10-GalMA10 can be used for research on liver cancer (hepatocellular carcinoma).
For research use only. We do not sell to patients.
- Formula: C690H1056N20O273S3
- Molecular Weight:14095.93
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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MCT1 |
MCT4 |
MMP-2 |
MMP-9 |
PEG9MA10-PAB10-GalMA10 (10-40 μM; 48 h) induces dose-dependent degradation of CD147 in HepG2 cells, and its level decreases to 49% of that in the control group after treatment with 40 μM for 48 h[1].
PEG9MA10-PAB10-GalMA10 (5-20 μM; 48 h) induces dose-dependent degradation of CD147 in H22 cells, with its level decreasing to 39% of that in the control group after treatment with 20 μM for 48 h[1].
PEG9MA10-PAB10-GalMA10 (20 μM) promotes lysosomal colocalization and degradation of CD147, MCT1 and MCT4 in Hepa1-6 cells[1].
PEG9MA10-PAB10-GalMA10 increases intracellular lactate levels and decreases extracellular lactate levels in Hepa1-6 cells under both normoxic and hypoxic conditions, indicating impaired lactate efflux[1].
PEG9MA10-PAB10-GalMA10 inhibits glycolytic activity (reduces maximal ECAR) and enhances mitochondrial respiratory capacity (increases maximal OCR) in Hepa1-6 cells[1].
PEG9MA10-PAB10-GalMA10 (12-48 h) significantly inhibits the migration of Hepa1-6 cells in scratch wound healing assays[1].
PEG9MA10-PAB10-GalMA10 reduces the secretion of MMP-2 and MMP-9 in Hepa1-6 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 human hepatocellular carcinoma cells
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Concentration:0, 10, 20, 40 μM
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Incubation Time:48 h
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Result:Reduced CD147 levels to 97%, 74%, and 49% of control at 10, 20, 40 μM after 48 h, respectively.
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Cell Line:H22 murine liver cancer cells
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Concentration:0, 5, 20 μM
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Incubation Time:48 h
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Result:Reduced CD147 levels to 89% and 39% of control at 5, 20 μM after 48 h, respectively.
PEG9MA10-PAB10-GalMA10 (40 mg/kg; administered via intratracheal injection; 4 doses given on days 0, 3, 6, and 9) potently inhibits the growth of subcutaneous Hepa1-6-GFP tumors in female C57BL/6 mice via selective degradation of CD147 in tumor cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female, 6-8 weeks old, subcutaneous injection of 2×106 H22 cells)[1]
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Dosage:40 mg/kg
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Administration:i.t.; 4 doses on days 0, 3, 6, 9
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Result:Suppressed tumour growth compared to controls.
Prolonged survival compared to controls.
Reduced intra-tumoural lactate levels.
Selectively degraded CD147 in CD45- tumour cells (no effect on CD45+ immune cells).
Showed no significant body weight loss.
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Animal Model:C57BL/6 (female, 6-8 weeks old, subcutaneous injection of 2×106 Hepa1-6-GFP cells)[1]
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Dosage:40 mg/kg
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Administration:i.t.; 4 doses on days 0, 3, 6, 9
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Result:Suppressed tumour growth, with reduced tumour volume compared to controls.
Showed no significant body weight loss.
Selectively degraded CD147 in CD45- GFP+ tumour cells (no effect on CD45+ GFP- immune/stromal cells).
Chemical Information
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Molecular Weight 14095.93
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Formula C690H1056N20O273S3
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SMILES
CCCCCCCCCCCCSC(SC(C(NC1=CC=C(O[C@H](O2)[C@H](O)[C@@H](O)[C@@H](O)[C@H]2CO)C=C1)=O)(C)CC(C(NC3=CC=C(O[C@H](O4)[C@H](O)[C@@H](O)[C@@H](O)[C@H]4CO)C=C3)=O)(C)CC(C(NC5=CC=C(O[C@H](O6)[C@H](O)[C@@H](O)[C@@H](O)[C@H]6CO)C=C5)=O)(C)CC(C(NC7=CC=C(O[C@H](O8)[C@H](O)[C@@H](O)[C@@H](O)[C@H]8CO)C=C7)=O)(C)CC(C(NC9=CC=C(O[C@H](O%10)[C@H](O)[C@@H](O)[C@@H](O)[C@H]%10CO)C=C9)=O)(C)CC(C(NC%11=CC=C(O[C@H](O%12)[C@H](O)[C@@H](O)[C@@H](O)[C@H]%12CO)C=C%11)=O)(C)CC(C(NC%13=CC=C(O[C@H](O%14)[C@H](O)[C@@H](O)[C@@H](O)[C@H]%14CO)C=C%13)=O)(C)CC(C(NC%15=CC=C(O[C@H](O%16)[C@H](O)[C@@H](O)[C@@H](O)[C@H]%16CO)C=C%15)=O)(C)CC(C(NC%17=CC=C(O[C@H](O%18)[C@H](O)[C@@H](O)[C@@H](O)[C@H]%18CO)C=C%17)=O)(C)CC(C(NC%19=CC=C(O[C@H](O%20)[C@H](O)[C@@H](O)[C@@H](O)[C@H]%20CO)C=C%19)=O)(C)CC(CC(CC(CC(CC(CC(CC(CC(CC(C(OCCNC(/C(C)=C/C=C/C(C)(OC%21=O)C(C%22(CC%23)OC(C)=O)CCC%21%22CC=C%23C(OC)=O)=O)=O)(CC(CC(CC(CC(CC(CC(CC(CC(CC(CC(CC(C#N)(CCC(O)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)(C(OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)=O)C)C)(C(OCCNC(/C(C)=C/C=C/C(C)(OC%24=O)C(C%25(CC%26)OC(C)=O)CCC%24%25CC=C%26C(OC)=O)=O)=O)C)(C(OCCNC(/C(C)=C/C=C/C(C)(OC%27=O)C(C%28(CC%29)OC(C)=O)CCC%27%28CC=C%29C(OC)=O)=O)=O)C)(C(OCCNC(/C(C)=C/C=C/C(C)(OC%30=O)C(C%31(CC%32)OC(C)=O)CCC%30%31CC=C%32C(OC)=O)=O)=O)C)(C(OCCNC(/C(C)=C/C=C/C(C)(OC%33=O)C(C%34(CC%35)OC(C)=O)CCC%33%34CC=C%35C(OC)=O)=O)=O)C)(C(OCCNC(/C(C)=C/C=C/C(C)(OC%36=O)C(C%37(CC%38)OC(C)=O)CCC%36%37CC=C%38C(OC)=O)=O)=O)C)(C(OCCNC(/C(C)=C/C=C/C(C)(OC%39=O)C(C%40(CC%41)OC(C)=O)CCC%39%40CC=C%41C(OC)=O)=O)=O)C)(C(OCCNC(/C(C)=C/C=C/C(C)(OC%42=O)C(C%43(CC%44)OC(C)=O)CCC%42%43CC=C%44C(OC)=O)=O)=O)C)(C(OCCNC(/C(C)=C/C=C/C(C)(OC%45=O)C(C%46(CC%47)OC(C)=O)CCC%45%46CC=C%47C(OC)=O)=O)=O)C)=S
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)