Oncrasin-72
Based on 1 Customer Validation
Oncrasin-72 (NSC-743380) is an RNA polymerase II inhibitor with activity in inhibiting growth and inducing cell death in human cancer cells. Oncrasin-72 exhibits antitumor activity through JNK activation and STAT3 inhibition. Analytical method development and validation for Oncrasin-72 is essential for quantifying its concentration in biological fluids for pharmacokinetic studies. This method was able to successfully quantify Oncrasin-72 in different dose groups when applied in rat plasma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 97.61%
- CAS. Nr.: 92407-90-4
- Formel: C16H14ClNO
- Molecular Weight:271.74
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biologische Aktivität
Beschreibung
IC50 & Target
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RNA Polymerase |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H157 | IC50 |
<=0.2 μM
Compound: 34
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Antitumor activity against human NCI-H157 cells assessed as cell viability after 3 days by sulforhodamine B assay
Antitumor activity against human NCI-H157 cells assessed as cell viability after 3 days by sulforhodamine B assay
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[PMID: 21443218] |
| NCI-H460 | IC50 |
<=0.2 μM
Compound: 34
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Antitumor activity against human H460 cells assessed as cell viability after 3 days by sulforhodamine B assay
Antitumor activity against human H460 cells assessed as cell viability after 3 days by sulforhodamine B assay
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[PMID: 21443218] |
| NCI-H460 | IC50 |
0.019 μM
Compound: 34
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Cytotoxicity against human H460 cells assessed as cell viability after 3 days by sulforhodamine B assay
Cytotoxicity against human H460 cells assessed as cell viability after 3 days by sulforhodamine B assay
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[PMID: 21443218] |
Chemical Information
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CAS. Nr. 92407-90-4
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Appearance Solid
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Molecular Weight 271.74
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Formel C16H14ClNO
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Color White to off-white
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SMILES
ClC1=CC=CC(CN2C=C(CO)C3=C2C=CC=C3)=C1
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Synonyms
NSC-743380
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (368.00 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
Reinheit & Dokumentation
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Data Sheet (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
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 | 3.6800 mL | 18.3999 mL | 36.7999 mL | 91.9997 mL |
| 5 mM | 0.7360 mL | 3.6800 mL | 7.3600 mL | 18.3999 mL | |
| 10 mM | 0.3680 mL | 1.8400 mL | 3.6800 mL | 9.2000 mL | |
| 15 mM | 0.2453 mL | 1.2267 mL | 2.4533 mL | 6.1333 mL | |
| 20 mM | 0.1840 mL | 0.9200 mL | 1.8400 mL | 4.6000 mL | |
| 25 mM | 0.1472 mL | 0.7360 mL | 1.4720 mL | 3.6800 mL | |
| 30 mM | 0.1227 mL | 0.6133 mL | 1.2267 mL | 3.0667 mL | |
| 40 mM | 0.0920 mL | 0.4600 mL | 0.9200 mL | 2.3000 mL | |
| 50 mM | 0.0736 mL | 0.3680 mL | 0.7360 mL | 1.8400 mL | |
| 60 mM | 0.0613 mL | 0.3067 mL | 0.6133 mL | 1.5333 mL | |
| 80 mM | 0.0460 mL | 0.2300 mL | 0.4600 mL | 1.1500 mL | |
| 100 mM | 0.0368 mL | 0.1840 mL | 0.3680 mL | 0.9200 mL |