AGL-2263

An inhibitor of IGF-1R

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库存: 现货

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1mg

￥812.00

650.00

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5mg

￥2375.00

1900.00

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10mg

￥3737.00

2990.00

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25mg

￥7487.00

5990.00

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50mg

￥12712.00

10170.00

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Background

AGL 2263 is an inhibitor of the insulin-like growth factor 1 receptor (IGF-1R; IC₅₀ = 0.43 μM).¹ It also inhibits the insulin receptor (IR), protein kinase B (PKB), and Src in a cell-free assay (IC₅₀s = 0.4, 55, and 2.2 μM, respectively). AGL 2263 inhibits IGF-1R autophosphorylation and phosphorylation of the downstream elements IRS-1, PKB, and ERK2 in an ATP-independent manner. It inhibits colony formation of PC3 and LNCaP prostate and MCF-7 and MDA-MB-468 breast cancer cells in soft agar (IC₅₀s = 4.3, 9, 17, and 6 μM, respectively).

1.Blum, G., Gazit, A., and Levitzki, A.Development of new insulin-like growth factor-1 receptor kinase inhibitors using catechol mimicsJ. Biol. Chem.278(42)40442-40454(2003)

Protocol

Cell experiment:

Trophoblast cells are prepared from normal or GDM placentas. They are incubated in the presence of stimulants, insulin (100 nM) or both insulin and AGL-2263 (AGL, 5 μM) IR blocker, together for 24 hr[1].

参考文献:

[1]. Li Y, et al. GDM-associated insulin deficiency hinders the dissociation of SERT from ERp44 and down-regulates placental 5-HT uptake. Proc Natl Acad Sci U S A. 2014 Dec 30;111(52):E5697-705.