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Enzymes for Research, Diagnostic and Industrial Use

GSK1904529A

Cat No.
CEI-0072
Description
GSK1904529A can inhibit IGF-IR and IR with IC50 of 27 nM and 25 nM.
CAS No.
1089283-49-7
Molecular Weight
851.96
Purity
>99%
Storage
2 years at -20centigrade Powder
Targets
IGF-IR, IR
Molecular Formula
C44H47F2N9O5S
Chemical Name
N-(2,6-difluorophenyl)-5-(3-(2-(5-ethyl-2-methoxy-4-(4-(4-(methylsulfonyl)piperazin-1-yl)piperidin-1-yl)phenylamino)pyrimidin-4-yl)H-imidazo[1,2-a]pyridin-2-yl)-2-methoxybenzamide
Solubility
DMSO 124 mg/mL Water
In vitro
GSK1904529A selectively inhibits IGF-IR(insulin-like growth factor-I receptor) and IR (insulin receptor) with IC50 of 27 nM and 25 nM. GSK1904529A blocks receptor autophosphorylation and downstream signaling, leading to cell cycle arrest. For cell lines As insulin-like growth factor-I receptor is involved in development of many types of tumors, including prostate, colon, breast, pancreatic, ovarian, and sarcomas, GSK1904529A can inhibit many cancer cell lines. GSK1904529A can inhibits the proliferation of cell lines derived from solid and hematologic malignancies, with multiple myeloma and Ewings sarcoma cell lines being most sensitive.
In vivo
Oral administration of GSK1904529A decreases the growth of human tumor xenografts in mice, consistent with a reduction of IGF-IR phosphorylation in tumors.
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