Tasisulam

Catalog No.S7326 Batch:S732601

Technical Data

Formula	C₁₁H₆BrCl₂NO₃S₂
Molecular Weight	415.11	CAS No.	519055-62-0
Solubility (25°C)*	In vitro	DMSO	83 mg/mL (199.94 mM)
		Ethanol	83 mg/mL (199.94 mM)
		Water	Insoluble
* <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.)

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Biological Activity

Description

Tasisulam (LY573636) is an antitumor agent and an apoptosis inducer via the intrinsic pathway. Phase 3.

Targets

Caspase ^[1]

In vitro

Tasisulam inhibits growth of various human leukemia and lymphoma cell lines with ED50 ranging from 7 to 40 μM. LY573636 also induces apoptosis in HL60, Reh, and MD901 cells, mainly by loss of mitochondrial membrane potential and induction of reactive oxygen species. ^[1] In addition, Tasisulam also produce antiproliferative activities in more than 70% of the 120 cell lines tested with EC50 of less than 50 μM. Tasisulam induces G2–M accumulation and subsequent apoptosis in Calu-6 and A-375 cells. In vitro, Tasisulam also inhibits VEGF-, FGF- and EGF-induced endothelial cord formation with EC50 of 47, 103, and 34 nM, respectively. ^[2]

In vivo

Tasisulam induces morphologic features of vascular normalization, including increased pericyte coverage and decreased hypoxia in vivo. Tasisulam (25 or 50 mg/kg, i.v.) displays dose-dependent antitumor activity, induces apoptosis, and normalizes tumor-associated vasculature in the Calu-6 non–small cell lung xenograft model. Besides, Tasisulam displays potent antitumor activity across a range of in vivo xenografts, including colorectal (HCT-116), melanoma (A-375), gastric (NUGC-3), leukemia (MV-4-11), and pancreatic (QGP-1). ^[2]

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines B-cell acute lymphocytic leukemia (Reh, RCH, BALL1), Burkitt’s lymphoma (Daudi), diffuse large B-cell lymphoma (MD901, LY4), myeloid leukemia cell lines (HL60 and U937), Mantle cell lymphoma cell lines (NCEB1, Jeko1, and SP49). Concentrations ~40 μM Incubation Time 96 hours Method Cells are treated with various concentrations of LY573636. 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.
Animal Study:^{^[2]}	Animal Models Calu-6 non–small cell lung xenograft model Dosages ~50 mg/kg Administration i.v.

Cell Assay:^{^[1]}

Cell lines
B-cell acute lymphocytic leukemia (Reh, RCH, BALL1), Burkitt’s lymphoma (Daudi), diffuse large B-cell lymphoma (MD901, LY4), myeloid leukemia cell lines (HL60 and U937), Mantle cell lymphoma cell lines (NCEB1, Jeko1, and SP49).
Concentrations
~40 μM
Incubation Time
96 hours
Method
Cells are treated with various concentrations of LY573636. 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.

Animal Study:^{^[2]}

Animal Models
Calu-6 non–small cell lung xenograft model
Dosages
~50 mg/kg
Administration
i.v.

References

Selleck's 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]	PubMed: 28013301

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]

PubMed: 28013301

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SHIPPING AND STORAGE
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