LRPPRC-IN-1
LRPPRC-IN-1 is a LRPPRC inhibitor. LRPPRC-IN-1 exerts dual effects of inhibiting LRPPRC activity and inducing its degradation by binding to the RNA-binding domain of LRPPRC. LRPPRC-IN-1 downregulates the expression of mitochondrial OXPHOS complex subunits and ATP synthase, inhibits oxidative phosphorylation, reduces ATP production, suppresses the proliferation and colony formation of various cancer cells, and inhibits tumor growth in vivo. LRPPRC-IN-1 can be used in studies related to lung cancer, pancreatic cancer, breast cancer, esophageal cancer, colorectal cancer, lymphoma, melanoma, cervical cancer, ovarian cancer, and prostate cancer.
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- Formel: C21H13Br2F3N2O4
- Molecular Weight:574.14
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
LRPPRC-IN-1 (compound 3o) (6.25-12.5 μM) potently inhibits the interaction between purified LRPPRC protein and its aptamer, with an inhibition rate of over 92.5%[1].
LRPPRC-IN-1 (5-10 μM) induces significant concentration-dependent degradation of LRPPRC protein in human lung adenocarcinoma cell line A549, with a maximum degradation rate of approximately 70%[1].
LRPPRC-IN-1 (120 h) exhibits potent and broad-spectrum antiproliferative activity against a variety of human cancer cell lines, with IC50 values ranging from 0.27 μM to 8.33 μM, including high activity against drug-resistant and refractory tumors[1].
LRPPRC-IN-1 (1.25-20 μM; 14 days) potently inhibits colony formation in a variety of human cancer cell lines[1].
LRPPRC-IN-1 (0.0-1.6 nM) inhibits the protein level of LRPPRC as well as the protein and transcription levels of the downstream mitochondrial OXPHOS signaling pathway in human lung adenocarcinoma cell line A549 at nanomolar concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Multiple human cancer cell lines: A549, PC9, A2780, MKN45, MDA-MB-231, SUM159, BXPC-3, ASPC-1
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Concentration:1.25 μM, 2.5 μM, 5 μM, 20 μM
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Incubation Time:14 days
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Result:Completely inhibited colony formation of A549, PC9, A2780, and MKN45 cells at 20 μM.
Significantly suppressed colony formation of MDA-MB-231, SUM159, BXPC-3, and ASPC-1 cells at concentrations of 1.25 μM, 2.5 μM, and 5 μM.
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Cell Line:A549 cells
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Concentration:0.0 nM, 0.4 nM, 0.8 nM, 1.6 nM
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Incubation Time:48 h
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Result:Significantly downregulated the transcription of OXPHOS-related genes, including COXI, COXII, and ATP6.
| Species | Dose | Route | Tmax | T1/2 | Cmax | AUC0-t | AUC0-∞ | MRT0-∞ | F | Vss | CL |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | i.v. | / | 4.26 h | / | 13400 ng·h/mL | 13600 ng·h/mL | 5.17 h | / | 1.90 L/kg | 6.12 mL/min/kg |
| Mice[1] | 5 mg/kg | i.p. | 0.5 h | 4.04 h | 6000 ng/mL | 22800 ng·h/mL | 23200 ng·h/mL | 5.89 h | 170.6 % | / | / |
| Mice[1] | 10 mg/kg | p.o. | 1.0 h | 4.35 h | 492 ng/mL | 4780 ng·h/mL | 4870 ng·h/mL | 6.31 h | 17.9 % | / | / |
LRPPRC-IN-1 (50 mg/kg; i.p.; daily; 10 days) exhibits significant in vivo antitumor activity against HCT116 xenografts, achieving a 49% tumor growth inhibition rate with a favorable safety profile[1].
LRPPRC-IN-1 (25-100 mg/kg; p.o.; daily; 10 days) exhibits a tolerable in vivo safety profile in healthy BALB/c mice at doses conferring antitumor efficacy, with only mild, dose-related alterations in select plasma biochemical markers at the highest tested dose[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-Nu nude mice (4-6 weeks old, male) were used to establish a xenograft model by inoculating PC9 cells.
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Dosage:50 mg/kg
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Administration:i.p.; daily; 18 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 73%.
Reduced tumor volume and tumor weight significantly.
Maintained stable mouse body weights throughout the treatment period.
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Animal Model:BALB/c-Nu nude mice (4-6 weeks old, male) were used to establish a xenograft model by inoculating HCT116 cells.[1]
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Dosage:50 mg/kg
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Administration:i.p.; daily; 10 days
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Result:Achieved a tumor growth inhibition (TGI) rate of 49%.
Suppressed tumor growth significantly.
Maintained stable mouse body weights across all treatment groups.
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Animal Model:BALB/c mice[1]
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Dosage:25 mg/kg; 50 mg/kg; 100 mg/kg
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Administration:p.o.; daily; 10 days
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Result:Showed favorable liver safety with no significant alterations in alanine aminotransferase (ALT), aspartate aminotransferase (AST), or albumin (ALB) levels at any dose.
Caused a slight decrease in γ-glutamyl transferase (GGT) in the 100 mg/kg group.
Induced mild increases in uric acid (UA) and lactate dehydrogenase (LDH) at 100 mg/kg.
Chemical Information
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Molecular Weight 574.14
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Formel C21H13Br2F3N2O4
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SMILES
O=C(C1=CC=C(C=C1O)C2=C(C=CC=C2)C(F)(F)F)N/N=C/C3=CC(Br)=C(C(Br)=C3O)O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
LRPPRC-IN-1 Related Classifications
HY-187350 Related Classifications
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