SW044248
Based on 1 Customer Validation
SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
For research use only. We do not sell to patients.
- Purity: 98.92%
- CAS No.: 522650-83-5
- Formula: C22H23N5O2S
- Molecular Weight:421.52
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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All Topoisomerase Isoforms
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Biological Activity
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Topoisomerase I |
SW044248 is a non-canonical Top1 inhibitor, and is selectively toxic for certain NSCLC cell lines. SW044248 shows no effect on Top2. SW044248 (2, 5, 10 μM) rapidly inhibits transcription, translation and DNA synthesis in sensitive cells (HCC4017 and H292 cells) but not insensitive cells (HBEC30KT cells and HCC44 cells). SW044248 (10 μM) rapidly activates the integrated stress response through kinases GCN2 and PKR. The inhibition of Top1 in HCC4017 cells is helpful to the toxicity of SW044248. SW044248 (5, 10 μM) shows no effect on HBEC30KT and HCC44 cell lines due to the up-regulation of p21CDKN1A[1]. SW044248 is selectively toxic in 18/74 NSCLC lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 522650-83-5
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Appearance Solid
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Molecular Weight 421.52
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Formula C22H23N5O2S
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Color Light yellow to yellow
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SMILES
CCC(SC1=NN=C2C(N(CC)C3=C2C=CC=C3)=N1)C(NC4=CC=CC=C4OC)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Solvent & Solubility
DMSO : 12.5 mg/mL (29.65 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Protocol
100 μL of 50,000 cells/mL cell suspensions of individual cell lines are added in wells in 96-well plates. The next day, 100 μL of cell medium substituted with 2X concentration of SW044248 or camptothecin or DMSO in triplicates is added to each well. After 96 and 120 hours the ATP concentration in the wells is measured with CelTiter-Glo. The luminescence is measured with an plate reader[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Zubovych IO, et al. A Novel Inhibitor of Topoisomerase I Is Selectively Toxic for a Subset of Non-Small Cell Lung Cancer Cell Lines. Mol Cancer Ther. 2016 Jan;15(1):23-36. [Content Brief]
[2]. Kim HS, et al. Systematic identification of molecular subtype-selective vulnerabilities in non-small-cell lung cancer. Cell. 2013 Oct 24;155(3):552-66. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3724 mL | 11.8618 mL | 23.7237 mL | 59.3092 mL |
| 5 mM | 0.4745 mL | 2.3724 mL | 4.7447 mL | 11.8618 mL | |
| 10 mM | 0.2372 mL | 1.1862 mL | 2.3724 mL | 5.9309 mL | |
| 15 mM | 0.1582 mL | 0.7908 mL | 1.5816 mL | 3.9539 mL | |
| 20 mM | 0.1186 mL | 0.5931 mL | 1.1862 mL | 2.9655 mL | |
| 25 mM | 0.0949 mL | 0.4745 mL | 0.9489 mL | 2.3724 mL |
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