Tasisulam sodium

Research use only, not for human use.

Tasisulam (LY 573636) is a small molecule antitumor agent that induces apoptosis via the intrinsic pathway.

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.

Tasisulam sodium (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 sodium (25, 50 μM; 72 hours) induces a concentration-dependent increase in 4N DNA and G2-M accumulation. Tasisulam sodium (200 nM-200 μM; 48 hours) induces apoptosis in a broad range of in vitro cancer cell models. Tasisulam sodium 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 μMIncubation Time:48 hours Result:Induced an antiproliferative response across a wide range of tumor histologies with EC50s is 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.

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LY 573636 sodium

Proteasome/Ubiquitin

E3 Ubiquitin Ligase

E3 Ubiquitin Ligase

Cancer

Blood cancer

519055-63-1

437.09

C11H5BrCl2NNaO3S2

>98% (HPLC)

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C1=CC(=C(C=C1Cl)Cl)C(=O)[N-]S(=O)(=O)C2=CC=C(S2)Br.[Na+]

N-[(5-bromo-2-thienyl)sulfonyl]-2,4-dichloro-benzamide sodium salt

(-20℃)

With Ice Pack

≥ 2 years