Tasisulam

SKU: orb1300994

Description

Tasisulam (LY573636) is a small molecule antitumor agent that induces apoptosis through the intrinsic mitochondrial pathway. It has demonstrated activity in preclinical in vitro and in vivo studies against various cancer models, supporting its investigation as a chemotherapeutic candidate.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 519055-62-0
• MW: 415.11
• Purity: >99.99% (May vary between batches)
• Formula: C₁₁H₆BrCl₂NO₃S₂
• SMILES: Clc1ccc(C(=O)NS(=O)(=O)c2ccc(Br)s2)c(Cl)c1
• Target: Apoptosis,Caspase,Molecular Glues
• Solubility: Ethanol:77 mg/mL (185.49 mM);DMSO:77 mg/mL (185.49 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.82 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• 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).
• 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. 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.
• Cell Research:
  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. (Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Tasisulam, Apoptosis, Caspase, LY 573636, LY573636, LY-573636, inhibit, Inhibitor

Compound Identifiers

PubChem CID

10160238