Tasisulam

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tasisulam (LY 573636) 是一种小分子抗肿瘤剂，可通过内在途径诱导细胞凋亡，导致细胞色素 c 释放和 caspase 依赖性细胞死亡。

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.

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.

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LY 573636

Proteasome/Ubiquitin

E3 Ubiquitin Ligase

Caspase

Cancer

Blood cancer

519055-62-0

415.1

C11H6BrCl2NO3S2

>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

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

(-20℃)

With Ice Pack

≥ 2 years