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SW044248

Katalog-Nr.GC19342 Copy One-Click Copy Product Info

SW044248 ist ein nicht-kanonischer Topoisomerase-I-Inhibitor und selektiv toxisch fÜr bestimmte Zelllinien von nicht-kleinzelligem Lungenkrebs (NSCLC).

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SW044248 Chemische Struktur

Cas No.: 522650-83-5

Größe Preis Lagerbestand Menge
10mM (in 1mL DMSO)
46,00 $
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5mg
50,00 $
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10mg
86,00 $
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25mg
164,00 $
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50mg
242,00 $
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100mg
335,00 $
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Sample solution is provided at 25 µL, 10mM.



Description of SW044248

SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.

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 uM) 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 uM) 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 uM) 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].

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.
[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.

Protocol of SW044248

Cell experiment:

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].

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.
[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.

Chemical Properties of SW044248

Cas No. 522650-83-5 SDF
Canonical SMILES CCC(SC1=NN=C2C(N(CC)C3=C2C=CC=C3)=N1)C(NC4=CC=CC=C4OC)=O
Formula C22H23N5O2S M.Wt 421.52
Löslichkeit DMSO : ≥ 30 mg/mL (71.17 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of SW044248

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.3724 mL 11.8618 mL 23.7237 mL
5 mM 474.5 μL 2.3724 mL 4.7447 mL
10 mM 237.2 μL 1.1862 mL 2.3724 mL
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In vivo Formulation Calculator (Clear solution) of SW044248

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Review for SW044248

Average Rating: 5 ★★★★★ (Based on Reviews and 22 reference(s) in Google Scholar.)

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