WSB1 Degrader 1

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

WSB1 Degrader 1 是一种有效的口服活性 WD 重复序列和包含 1 个 SOCS 盒的降解剂。 WSB1 Degrader 1 具有抗癌转移作用。

WSB1 Degrader 1 is a poten and orally active?WD repeat and SOCS box-containing 1 degrader. WSB1 Degrader 1 has anticancer metastatic effects.

WSB1 Degrader 1 (compound 4; 0.25-2500 nM; 2-24 hours; H1299-WSB1 cells) treatment indues WSB1 degradation in time-dependent and dose-dependent manners.WSB1 Degrader 1 (compound 4) exhibits potent antimigration efficacy in both KHOS and H460 cell lines with IC50 values of 39.1 μM and 24.47 μM, respectively.WSB1 Degrader 1 (compound 4) significantly inhibits cancer cell migration under normoxia and hypoxia in KHOS cells. WSB1 Degrader 1 (5 μM) treatment elevates the levels of the RhoGDI2 protein in KHOS cells under hypoxia.The wound-healing of H1299-WSB1 cells is significantly inhibited by treating with WSB1 Degrader 1. WSB1 Degrader 1 can only block the wound-healing capability of wild-type A2780 (A2780-WT) cells but not the A2780-WSB1/KO cells. Western Blot Analysis Cell Line:H1299-WSB1 cells Concentration:0.25 nM, 2.5 nM, 25 nM, 250 nM, 2500 nM Incubation Time:2 hours, 4 hours, 6 hours, 8 hours, 12 hours, 24 hours Result:Induced WSB1 degradation in time-dependent and dose-dependent manners.

WSB1 Degrader 1 (compound 4; 100 mg/kg; p.o.; daily; for 28 days) treatment can effectively inhibit the pulmonary metastasis of cancer cells.In rats, after 100 mg/kg oral dosing or 160 mg/kg intraperitoneal dosing of WSB1 Degrader 1 (compound 4), the two ways of administration are observed with quick absorption (Tmax), but the former dosing displayed a fast clearance (T1/2). Moreover, Cmax and AUC0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups showed acceptable blood exposure. Animal Model:Balb/c (nu/nu) mice bearing highly metastatic 4T1 breast cancer cells.Dosage:100 mg/kg/day.Administration:p.o.; daily; for 28 days Result:Effectively inhibited the pulmonary metastasis of cancer cells.

——

Others

Other Targets

WSB1

——

——

2306039-66-5

334.41

C21H22N2O2

>98% (HPLC)

DMSO:24 mg/mL?(71.76 mM;?Need ultrasonic)

NC1=NC(C2=CC=C(OC)C(C)=C2)=C(C3=CC=C(OC)C(C)=C3)C=C1

——

(-20℃)

With Ice Pack

≥ 2 years