Tasisulam

SKU: orb1224828

Description

Tasisulam (LY 573636) is a small molecule antitumor agent that induces apoptosis via the intrinsic pathway, resulting in cytochrome c release and caspase-dependent cell death; shows antiproliferative effect against a variety of human hematopoietic malignancies, including AML, B-ALL, large B-cell and mantle cell lymphoma cell lines; promotes the recruitment of RBM39 to the CUL4-DCAF15 E3 ubiquitin ligase, leading to RBM39 polyubiquitination and proteasomal degradation; causes aberrant pre-mRNA splicing.Blood Cancer Phase 1 Discontinued(In Vitro):Tasisulam (200 nM-200 μM; 48 hours) induces an antiproliferative response across a wide range of tumor histologies with EC50s of 10 μM and 25 μM for Calu-6 and A-375 cell lines, respectively.Tasisulam (25, 50 μM; 72 hours) induces a concentration-dependent increase in 4N DNA and G2-M accumulation.Tasisulam (200 nM-200 μM; 48 hours) induces apoptosis in a broad range of in vitro cancer cell models.Tasisulam also blocks VEGF, epidermal growth factor, and fibroblast growth factor-induced endothelial cell cord formation.

Key Properties

• CAS Number: 519055-62-0
• MW: 415.1
• Purity: >98% (HPLC)
• Formula: C₁₁H₆BrCl₂NO₃S₂
• SMILES: O=S(C1=CC=C(Br)S1)(NC(C2=CC=C(Cl)C=C2Cl)=O)=O
• Target: E3 Ubiquitin Ligase
• Solubility: DMSO: 77 mg/mL (185.5 mM); Ethanol: 77 mg/mL (185.5 mM); Water: <1 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vitro:
  Tasisulam (200 nM-200 μM; 48 hours) induces an antiproliferative response across a wide range of tumor histologies with EC50s of 10 μM and 25 μM for Calu-6 and A-375 cell lines, respectively. Tasisulam (25, 50 μM; 72 hours) induces a concentration-dependent increase in 4N DNA and G2-M accumulation. Tasisulam (200 nM-200 μM; 48 hours) induces apoptosis in a broad range of in vitro cancer cell models. Tasisulam also blocks VEGF, epidermal growth factor, and fibroblast growth factor-induced endothelial cell cord formation. Cell Proliferation Assay Cell line: Calu-6 non-small cell lung carcinoma and A-375 melanoma models. Concentration: 200 nM-200 μM. Incubation time: 48 hours. Result: Induced an antiproliferative response across a wide range of tumor histologies with EC50s are 10 μM and 25 μM, respectively. Cell Cycle Analysis Cell line: Calu-6 and A-375 cell lines. Concentration: 25, 50 μM. Incubation time: 72 hours. Result: Induced a concentration-dependent increase in 4N DNA and G2-M accumulation. Apoptosis Analysis Cell line: Calu-6 non-small cell lung carcinoma and A-375 melanoma models. Concentration: 200 nM-200 μM. Incubation time: 48 hours. Result: Induced apoptosis in a broad range of in vitro cancer cell models.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LY 573636

Quick Database Links

Gene Symbol

E3 Ubiquitin Ligase