Biodegradable polymeric micelles encapsulated JK184 suppress tumor growth through inhibiting Hedgehog signaling pathway was written by Zhang, Nannan;Liu, Shichang;Wang, Ning;Deng, Senyi;Song, Linjiang;Wu, Qinjie;Liu, Lei;Su, Weijun;Wei, Yuquan;Xie, Yongmei;Gong, Changyang. And the article was included in Nanoscale in 2015.Product Details of 315703-52-7 The following contents are mentioned in the article:
JK184 can specially inhibit Gli in the Hedgehog (Hh) pathway, which showed great promise for cancer therapeutics. For developing aqueous formulation and improving anti-tumor activity of JK184, we prepared JK184 encapsulated MPEG-PCL micelles by the solid dispersion method without using surfactants or toxic organic solvents. The cytotoxicity and cellular uptake of JK184 micelles were both increased compared with the free drug. JK184 micelles induced more apoptosis and blocked proliferation of Panc-1 and BxPC-3 tumor cells. In addition, JK184 micelles exerted a sustained in vitro release behavior and had a stronger inhibitory effect on proliferation, migration and invasion of HUVECs than free JK184. Furthermore, JK184 micelles had stronger tumor growth inhibiting effects in s.c. Panc-1 and BxPC-3 tumor models. Histol. anal. showed that JK184 micelles improved anti-tumor activity by inducing more apoptosis, decreasing microvessel d. and reducing expression of CD31, Ki67, and VEGF in tumor tissues. JK184 micelles showed a stronger inhibition of Gli expression in Hh signaling, which played an important role in pancreatic carcinoma. Furthermore, circulation time of JK184 in blood was prolonged after entrapment in polymeric micelles. Our results suggested that JK184 micelles are a promising drug candidate for treating pancreatic tumors with a highly inhibitory effect on Hh activity. This study involved multiple reactions and reactants, such as N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine (cas: 315703-52-7Product Details of 315703-52-7).
N-(4-Ethoxyphenyl)-4-(2-methylimidazo[1,2-a]pyridin-3-yl)thiazol-2-amine (cas: 315703-52-7) belongs to thiazole derivatives. The higher aromaticity of thiazole is due to delocalization of a lone pair of sulfur electrons across the ring, which is evidenced by chemical shifts of ring hydrogen at δ 7.27 and 8.77 ppm (C2 and C4), indicating diamagnetic ring current. Various laboratory methods exist for the organic synthesis of thiazoles. Prominent is the Hantzsch thiazole synthesis is a reaction between haloketones and thioamides.Product Details of 315703-52-7
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica