Tasisulam

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.

519055-62-0

LY 573636

>98% (HPLC)

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)

O=S (C1=CC=C (Br) S1) (NC (C2=CC=C (Cl) C=C2Cl) =O) =O

C11H6BrCl2NO3S2

415.1

Storage temperature: -20°C. Stability: ≥ 2 years

For research use only.