In Vivo (Add solvents to the product individually and in order.)
Homogeneous suspension
CMC-NA
≥5mg/ml
Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
Biological Activity
Description
Tasisulam (LY573636) is an antitumor agent and an Apoptosis inducer via the intrinsic pathway. Phase 3.
Targets
Caspase
In vitro
Tasisulam inhibits growth of various human leukaemia and lymphoma cell lines with ED50 ranging from 7 to 40 μM. This compound also induces Apoptosis in HL60, Reh, and MD901 cells, mainly by loss of mitochondrial membrane potential and induction of reactive oxygen species. In addition, this chemical also produces antiproliferative activities in more than 70% of the 120 cell lines tested with EC50 of less than 50 μM. It induces G2–M accumulation and subsequent Apoptosis in Calu-6 and A-375 cells. In vitro, this agent also inhibits VEGF-, FGF- and EGF-induced endothelial cord formation with EC50 of 47, 103, and 34 nM, respectively.
In Vivo
Tasisulam induces morphologic features of vascular normalisation, including increased pericyte coverage and decreased hypoxia in vivo. This compound (25 or 50 mg/kg, i.v.) displays dose-dependent antitumor activity, induces Apoptosis, and normalises tumour-associated vasculature in the Calu-6 non–small cell lung xenograft model. Besides, it displays potent antitumor activity across a range of in vivo xenografts, including colorectal (HCT-116), melanoma (A-375), gastric (NUGC-3), leukaemia (MV-4-11), and pancreatic (QGP-1).
Cells are treated with various concentrations of this compound. 3-(4,5-Dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay is performed. Briefly, MTT is dissolved in phosphate-buffered saline (PBS) at 5 mg/mL. Approximately 1,000 cells per well are incubated in culture medium for 96 hours in 96-well plates; and then, 10 μL of the MTT solution is added. After a 4-hour incubation, 100 μL of solubilization solution (20 % sodium dodecyl sulfate [SDS]) is added, and the mixture was incubated at 37 °C for 16 hours. In this assay, MTT is cleaved to an orange formazan dye by metabolically active cells; and the absorbance of the formazan product is measured with an enzyme-linked immunoabsorbent assay (ELISA) reader at 540 nm.
Sellecks Tasisulam Has Been Cited by 1 Publication
Synthesis of a Sulfonimidamide-Based Analog of Tasisulam and Its Biological Evaluation in the Melanoma Cell Lines SKMel23 and A375
[Steinkamp AD, et al. Skin Pharmacol Physiol, 2016, 29(6):281-290]
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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