Tasisulam (Synonyms: LY573636) |
| Katalog-Nr.GC10294 |
Tasisulam ist ein Antikrebsmittel und induziert Apoptose Über den intrinsischen Weg, was zur Freisetzung von Cytochrom c und Caspase-abhÄngigem Zelltod fÜhrt. Tasisulam hemmt die mitotische Progression und induziert eine vaskulÄre Normalisierung.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 519055-62-0
Sample solution is provided at 25 µL, 10mM.
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Tasisulam is an antitumor agent [1].
Tasisulam is an antitumor agent that induced growth arrest and apoptosis of human solid tumours. In human malignant hematopoietic cell lines, tasisulam inhibited cells growth with ED50 values of 5, 7, 12, 13, 21 and 31 μM for BALL1, HL60, RCH, NCEB1, SP49 and Daudi cell lines, respectively. Tasisulam induced growth arrest in a dose-dependent way. Also, tasisulam caused induction of ROS, loss of mitochondrial membrane potential and induction of apoptosis. In HL60 and U937 cells, tasisulam induce granulocytic/monocytic differentiation. In solid tumor cell lines, tasisulam induced apoptosis that was mediated by the mitochondrial-mediated cell death pathways [1]. Tasisulam increased phospho-histone H3 expression and cells with 4N DNA, and led to G2-M accumulation and apoptosis. Tasisulam also inhibited endothelial cell cord formation induced by epidermal growth factor, VEGF and fibroblast growth factor with EC50 values of 34, 47 and 103 nM, respectively.
In mice bearing the Calu-6 non-small cell lung xenograft model, tasisulam exhibited antitumor efficacy in a dose-dependent way and reduced tumor volume by 77%. Tasisulam caused G2-M accumulation and increased nuclear fragmentation. Also, tasisulam induced vascular normalization [2].
References:
[1]. Haritunians T, Gueller S, O'Kelly J, et al. Novel acyl sulfonamide LY573636-sodium: effect on hematopoietic malignant cells. Oncol Rep, 2008, 20(5): 1237-1242.
[2]. Meier T, Uhlik M, Chintharlapalli S, et al. Tasisulam sodium, an antitumor agent that inhibits mitotic progression and induces vascular normalization. Mol Cancer Ther, 2011, 10(11): 2168-2178.
| Cas No. | 519055-62-0 | SDF | |
| Überlieferungen | LY573636 | ||
| Chemical Name | N-(5-bromothiophen-2-yl)sulfonyl-2,4-dichlorobenzamide | ||
| Canonical SMILES | C1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br | ||
| Formula | C11H6BrCl2NO3S2 | M.Wt | 415.11 |
| Löslichkeit | ≥ 20.3mg/mL in DMSO | 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.409 mL | 12.045 mL | 24.09 mL |
| 5 mM | 0.4818 mL | 2.409 mL | 4.818 mL |
| 10 mM | 0.2409 mL | 1.2045 mL | 2.409 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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μL
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Calculation results:
Working concentration: mg/ml;
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 ddH2O, 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.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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