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.
For research use only. We do not sell to patients.
- Formula: C21H13Br2F3N2O4
- Molecular Weight:574.14
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
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].
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.
Parmacokinetics
| 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 % | / | / |
In Vivo
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].
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.
- Kinase activity and phosphorylation assays
- RNA extraction experimental
- Western Blot
- Patient-Derived Xenograft (PDX)
- Patient-Derived Orthotopic Xenograft (PDOX)
- Protocol for Kinase activity and phosphorylation assays
- Soft Agar Colony Formation Assay
- Colony Formation (Clonogenic) Assay
- Subcutaneous Cell-Line-Derived Xenograft
- Breast Cancer Modeling
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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Molecular Weight 574.14
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Formula 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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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)
LRPPRC-IN-1 Related Classifications
HY-187350 Related Classifications
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