959754-85-9

959754-85-9 structure

Name: GLPG-0259
Chemical Name: 4-[8-[4-(4-tert-butylpiperazin-1-yl)anilino]-[1,2,4]triazolo[1,5-a]pyrazin-5-yl]furan-2-carboxamide
CAS Number: 959754-85-9
Molecular Formula: C₂₄H₂₈N₈O₂
Molecular Weight: 460.53200
Catalog: Research Areas Cancer
Create Date: 2016-07-27 03:05:09
Modify Date: 2024-01-09 16:59:17
GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells[1][2].

Name	4-[8-[4-(4-tert-butylpiperazin-1-yl)anilino]-[1,2,4]triazolo[1,5-a]pyrazin-5-yl]furan-2-carboxamide

Description	GLPG0259 is a ATP-competitive inhibitor of MAPK-activated protein kinase 5 (MK5) with oral activity. GLPG0259 reduces inflammation and bone destruction in a mouse model of collagen-induced arthritis. GLPG0259 also inhibited the metastasis of prostate cancer (PCa) cells[1][2].
Related Catalog	Research Areas >> Cancer Signaling Pathways >> Others >> Others
Target	MAPK-activated protein kinase 5 (MK5)[1]
In Vitro	GLPG0259 能够减少炎症和骨降解介质的释放，但不影响 c-jun NH(2)-末端蛋白激酶 (JNK)、ERK 和 p38 MAP 激酶的磷酸化[1]。 GLPG0259 (1-5 μM; 48 h) 导致前列腺癌 (PCa) 细胞株 LNCaP 和 PC3 中，肌动蛋白丝状减少和重塑[2]。
In Vivo	GLPG0259 (2 mg/kg, 10 mg/kg;腹腔注射; 每周 2 次, 共 7 周) 在携带有前列腺癌细胞系 P3 细胞 (i.v.) 的 SCID 米色小鼠中，抑制肿瘤细胞在肺转移[2].
References	[1]. Westhovens R, et al. Oral administration of GLPG0259, an inhibitor of MAPKAPK5, a new target for the treatment of rheumatoid arthritis: a phase II, randomised, double-blind, placebo-controlled, multicentre trial. Ann Rheum Dis. 2013 May;72(5):741-4. [2]. Khalil MI, et al. The TLK1-MK5 Axis Regulates Motility, Invasion, and Metastasis of Prostate Cancer Cells. Cancers (Basel). 2022 Nov 22;14(23):5728.