UM-164 (C007B-304853)

InformationUM-164 is a highly potent, dualc-Src/p38inhibitor ofc-Srcwith a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.Targetsp38α ; p38β ; c-Src (Cell-free assay) ; 2.7 nM(Kd)In vitroUM-164 binds the inactive kinase conformation of c-Src. UM-164 alters the cell localization of c-Src in TNBC (anti-triple-negative breast cancer) cells. It has potent antiproliferative activity (average GI50 = 160 nmol/L) in all TNBC cell lines tested. UM-164 is a potent inhibitor of p38α and p38β. p38 MAPK phosphorylation is completely absent in SUM 149 cells treated with 50 nmol/L of UM-164. UM-164 can suppress both cell motility and invasion of MDA-MB 231 and SUM 149 cell lines with an IC50 = 50 nmol/L. FAK phosphorylation is inhibited by UM-164 in SUM 149 cells. UM-164 also efficiently reduces activation of EGFR (at both Tyr-845 and Tyr-1068), AKT, and ERK1/2, all of which are not direct targets of UM-164..In vivoIn xenograft models of TNBC (anti-triple-negative breast cancer), UM-164 results in a significant decrease of tumor growth compared with controls, with limited in vivo toxicity.Cell Research(from reference)Cell lines：MDA-MB 468 cells Concentrations：5 μM Incubation Time：4 h. Specification: 0.99 Molecular Formula: C30H31F3N8O3S Molecular Weight: 640.68 PubChem CID: 11714353 Isomeric SMILES: CC1=C(C=C(C=C1)NC(=O)C2=CC(=CC=C2)C(F)(F)F)NC(=O)C3=CN=C(S3)NC4=CC(=NC(=N4)C)N5CCN(CC5)CCO Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/U414125-SCI_d0b03828c3b96f025ff59144936d9cbf.pdf