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IGF-1R
Insulin and IGF are peptides pivotal to numerous functions such as cellular growth, proliferation, metabolism, glucose homeostasis, cell differentiation, and apoptosisInsulin and IGF are peptides having 40–80 % homology making it challenging, although not impossible, to explain insulin and IGF-1 ligand receptor interaction. Insulin/IGF signaling system mainly comprises of three ligands—IGF-1, IGF-2, and insulin, which in turn interact with at least six receptors: the type I IGF receptor (IGF-1R), the IRA (IR-A), the IRB (IR-B), hybrid receptors of IGF and IR-A, hybrid receptors of IGF and IR-B, and hybrid receptors of IR-A and IR-B. In vivo and in vitro experimental models have highlighted increased insulin, IGF-1 and IGF-2 signaling to be responsible for enhancing tumorigenesis. Signaling of IGF as growth hormone plays a fundamental role in regulating embryonic growth as well as specific differentiation in most adult tissues. The activated IR tyrosine kinase activates several substrates including IR substrate proteins (IRS1-4), Gab-1, Cbl, and Shc, Phosphatidyl Inositol 3-Kinase (PIK3), Akt, mTOR, MAPK, and signal regulatory protein family.
References
1.Singh P,et al. Med Oncol. 2014 Jan;31(1):805.
References
1.Singh P,et al. Med Oncol. 2014 Jan;31(1):805.
Angiogenesis
IGF-1R
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Insulin efsitora alfa
产品货号 : M36800
cas no: 2131038-11-2
Insulin efsitora alfa (LY-3209590) 是一种胰岛素受体 (insulin receptor，IR) 的选择性激动剂。Insulin efsitora alfa 是一种融合蛋白，由与人免疫球蛋白 G2 (IgG2) 片段可结晶 (Fc) 结构域融合人胰岛素受体 (IR) 激动剂组成，分子量为 64.1 kDa。Insulin efsitora alfa 耐受性良好，在糖尿病中有潜在的应用。
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Ganitumab
产品货号 : M36729
cas no: 905703-97-1
Ganitumab (AMG 479) 是一种重组人1型胰岛素样生长因子受体 (IGF1R) 单克隆抗体。Ganitumab 识别具有亚纳米摩尔亲和力的小鼠 IGF1R (KD=0.22 nM)，并抑制小鼠 IGF1R 与 IGF1 和 IGF2 的相互作用。Ganitumab 可用于癌症研究。
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Protonstatin-1
产品货号 : M36384
cas no: 521972-99-6
Protonstatin-1 is used as a hypoglycemic agent and as a compound for the treatment of Alzheimer's disease, inhibits IGFIR kinase activity and can be used in cancer research.
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KW-2450 free base
产品货号 : M36254
cas no: 904899-25-8
KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.
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Tyrphostin AG 538
产品货号 : M35935
cas no: 133550-18-2
AG 538 是一种有效的 IGF-1 受体激酶竞争性抑制剂，IC50 为 400 nM。
