ALK

下级目录

CEP-28122
ASP-3026
Entrectinib
GSK1838705A
AZD-3463
Ensartinib
PF-03671148
CEP-37440
Etalocib
GW6604
CEP-14083
CEP-14513
A-83-01
SB-505124 hydrochloride hydrate
NVP-TAE684

目录项下的产品

1022958-60-6
1097917-15-1
1108743-60-7
1116235-97-2
1116235-97-2 / MFCD216235972
GSK1838705A is a small-molecule kinase inhibitor that inhibits IGF-IR and IR (insulin receptor) with IC50s of 2.0 and 1.6 nM, respectively . GSK1838705A blocks the in vitro proliferation of cell lines derived from solid and hematologic malignancies, including multiple myeloma and Ewing's sarcoma, and retards the growth of human tumor xenografts in vivo. Despite the inhibitory effect of GSK1838705A on insulin receptor, minimal effects on glucose homeostasis were observed at efficacious doses. GSK1838705A also inhibits the anaplastic lymphoma kinase (ALK), which drives the aberrant growth of anaplastic large-cell lymphomas, some neuroblastomas, and a subset of non-small cell lung cancers. GSK1838705A inhibits ALK, with an IC(50) of 0.5 nmol/L, and causes complete regression of ALK-dependent tumors in vivo at well-tolerated doses. GSK1838705A is therefore a promising antitumor agent for therapeutic use in human cancers. (source: Mol Cancer Ther. 2009 Oct;8(10):2811-20. ).
1356962-20-3
1370651-20-9
1378524-25-4
1391712-60-9
161172-51-6
452342-37-9
452342-37-9 / MFCD52342379
GW6604 is a potent and selective ALK-5 inhibitor with potent anticancer activity. GW6604 is also a TGF-beta signaling pathway inhibitor. In vitro, GW6604 inhibited autophosphorylation of ALK5 with an IC(50) of 140 nM and in a cellular assay inhibited TGF-beta-induced transcription of PAI-1 (IC(50): 500 nM). In vivo, GW6604 (40 mg kg(-1) p.o.) increased liver regeneration in TGF-beta-overexpressing mice, which had undergone partial hepatectomy. In an acute model of liver disease, GW6604 reduced by 80% the expression of collagen IA1. Inhibition of ALK5 could be an attractive new approach to treatment of liver fibrotic diseases by both preventing matrix deposition and promoting hepatocyte regeneration. ( Br J Pharmacol. 2005 May;145(2):166-77. ).
856692-39-2
856693-04-4
909910-43-6
694433-59-5
761439-42-3