215655-21-3

215655-21-3 structure

Name: ICT5040
Chemical Name: 2-(methylthio)-5-[2-methyl-6-(trifluoromethyl)-3-pyridyl]-1,3,4-oxadiazole
CAS Number: 215655-21-3
Molecular Formula: C₁₀H₈F₃N₃OS
Molecular Weight: 275.250
Catalog: Signaling Pathways GPCR/G Protein CXCR
Create Date: 2021-09-12 21:51:52
Modify Date: 2024-03-31 13:43:54
ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells[1].

Name	2-(methylthio)-5-[2-methyl-6-(trifluoromethyl)-3-pyridyl]-1,3,4-oxadiazole
Synonyms	Pyridine, 2-methyl-3-[5-(methylthio)-1,3,4-oxadiazol-2-yl]-6-(trifluoromethyl)- 2-(methylthio)-5-[2-methyl-6-(trifluoromethyl)-3-pyridyl]-1,3,4-oxadiazole 2-Methyl-3-[5-(methylsulfanyl)-1,3,4-oxadiazol-2-yl]-6-(trifluoromethyl)pyridine 2-Methyl-3-[5-(methylthio)-1,3,4-oxadiazol-2-yl]-6-(trifluoromethyl)pyridine

Description	ICT5040 is a small molecule CXCR4 antagonist (IC50=3.8 μM). ICT5040 inhibits CXCL12-mediated proliferation and migration, and suppresses CXCL12-induced intracellular calcium mobilisation in U87 glioma cells[1].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> CXCR Signaling Pathways >> Immunology/Inflammation >> CXCR
Target	CXCR4:3.8 μM (IC50)
In Vitro	ICT5040 (1-100 μM; 0-4 d) 剂量依赖性地抑制 CXCL12 诱导的 U87 胶质瘤细胞的增殖和迁移[1]。 ICT5040 在 U87 胶质瘤细胞中降低 CXCL12 诱导的细胞内钙动员[1]。 Cell Migration Assay [1] Cell Line: U87-glioma cells Concentration: 1 μM, 10 μM, 100 μM; with 100 ng/mL CXCL12 Incubation Time: 0, 1, 2, 3, and 4 days Result: Resulted reduction of CXCL12 induced proliferation and migration of U87 cells at day 3.
References	[1]. Vinader V, et al. Discovery and computer aided potency optimization of a novel class of small molecule CXCR4 antagonists. PLoS One. 2013 Oct 18;8(10):e78744.