UCI-LC0019
Based on 1 Customer Validation
UCI-LC0019 is a mutant p53 reactivator. UCI-LC0019 binds to mutant p53, induces wild-type-like conformational change, restores sequence-specific DNA binding activity, activates p53-dependent transcription programs, and does not act via thiol reactivity or glutathione depletion. UCI-LC0019 inhibits proliferation and induces apoptosis in cancer cells harboring mutant p53, with no significant effect on p53null or wild-type p53 tumors cells. UCI-LC0019 exhibits anti-tumor activity in xenograft mouse models carrying p53R175H mutant tumors. UCI-LC0019 can be used for the research of cancer, such as ovarian cancer.
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- Pureté : 98.63%
- CAS No.: 1372406-51-3
- Formule: C17H14N2O2
- Masse moléculaire:278.31
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCT-116 | IC50 |
0.58 μM
Compound: A9
|
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay
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[PMID: 27017265] |
In Vitro
UCI-LC0019 potently inhibits proliferation of p53G245S-expressing Saos-2 cells (IC50 = 16.5 μM) and p53R175H-expressing TOV112D cells (IC50 = 15.2 μM) with reduced activity against p53null Saos-2 cells (IC50 = 24.1 μM)[1].
UCI-LC0019 (0-30 μM; 3-72 h) rapidly reduces proliferation and induces apoptosis in p53R175H-expressing TOV112D cells[1].
UCI-LC0019 (25-30 μM; 3 days) inhibits proliferation of p53R175H-expressing TOV112D cells via a mechanism independent of thiol reactivity, as co-treatment with 5 mM NAC (HY-B0215) does not reverse its antiproliferative effects[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:p53R175H-expressing TOV112D cells
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Concentration:30 μM
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Incubation Time:3, 12, 24 h
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Result:Induced rapid cell death time-dependently.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice with p53R175H-expressing TOV112D Xenografts[1]
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Dosage:10 mg/kg
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Administration:i.p.; daily for 10 days
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Result:Reduced tumor volume.
Increased GSH levels.
Did not result in weight loss or any obvious toxic effects.
- Protocol for Electrophoretic Mobility Shift Assay (EMSA)
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Cell Viability Determination by MTT Colorimetric Assay
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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CAS No. 1372406-51-3
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Appearance Solid
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Masse moléculaire 278.31
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Formule C17H14N2O2
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Color Light yellow to yellow
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SMILES
COC1=CC=CC(/C=C/C(C2=NC3=CC=CC=C3N2)=O)=C1
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (359.31 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5931 mL | 17.9656 mL | 35.9312 mL | 89.8279 mL |
| 5 mM | 0.7186 mL | 3.5931 mL | 7.1862 mL | 17.9656 mL | |
| 10 mM | 0.3593 mL | 1.7966 mL | 3.5931 mL | 8.9828 mL | |
| 15 mM | 0.2395 mL | 1.1977 mL | 2.3954 mL | 5.9885 mL | |
| 20 mM | 0.1797 mL | 0.8983 mL | 1.7966 mL | 4.4914 mL | |
| 25 mM | 0.1437 mL | 0.7186 mL | 1.4372 mL | 3.5931 mL | |
| 30 mM | 0.1198 mL | 0.5989 mL | 1.1977 mL | 2.9943 mL | |
| 40 mM | 0.0898 mL | 0.4491 mL | 0.8983 mL | 2.2457 mL | |
| 50 mM | 0.0719 mL | 0.3593 mL | 0.7186 mL | 1.7966 mL | |
| 60 mM | 0.0599 mL | 0.2994 mL | 0.5989 mL | 1.4971 mL | |
| 80 mM | 0.0449 mL | 0.2246 mL | 0.4491 mL | 1.1228 mL | |
| 100 mM | 0.0359 mL | 0.1797 mL | 0.3593 mL | 0.8983 mL |