货号	规格	价格	上海	北京	珠海	武汉
S81548-1mg	≥99%	￥120.00 S81548-1mg ￥120.00 现货	1 0 1	-	-	-
S81548-5mg	≥99%	￥300.00 S81548-5mg ￥300.00 现货	8 8	1	-	-
S81548-10mg	≥99%	￥530.00 S81548-10mg ￥530.00 现货	7 7	2	-	-
S81548-50mg	≥99%	￥1530.00 S81548-50mg ￥1530.00 现货	4 0 4	-	-	-
S81548-100mg	≥99%	￥2150.00 S81548-100mg ￥2150.00 现货	3 0 3	-	-	-

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产品描述：

Linsitinib (OSI-906) is a potent, selective and orally bioavailable dual inhibitor of the IGF-1 receptor and insulin receptor (IR) with IC50s of 35 and 75 nM, respectively

靶点：

IC50: 35 nM (IGF-1R), 75 nM (InsR);IGF-1R

体内研究：

Linsitinib inhibits tumor growth in an IGF-1R-driven xenograft mouse model, with 100% TGI and 55% regression at a dose of 75 mg/kg and 60% TGI and no regression at a dose of 25 mg/kg. Linsitinib administration induces different elimination half-lives of itself in dog, rat and mice, the elimination half-lives are 1.18 hours, 2.64 hours and 2.14 hours, respectively. Linsitinib administration at different single dose once-daily in femal Sprague-Dawley rat and femal CD-1 mouse reveal that the Vmax is not dose-proportional to Linsitinib dose. Linsitinib elevates the blood glucose levels at a dose of 25 mg/kg after 12 days administration. Linsitinib administration at a single dose of 75 mg/kg in IGF-1R-driven full-length human IGF-1R (LISN) xenograft mouse model achieve maximal inhibition of IGF-1R phosphorylation (80%) between 4 and 24 hours with plasma drug concentrations of 26.6-4.77 μM. Linsitinib administered as a single dose of at 60 mg/kg in NCI-H292 xenografts mice inhibits uptake of glucose at 2, 4, and 24 hours post-treatment in vivo. Linsitinib inhibits the growth of tumors in NCI-H292 xenograft mouse model

参考文献：

1. Mulvihill MJ, et al. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and IR. Future Med Chem. 2009 Sep;1(6):1153-71. 2. McKinley ET, et al. 18FDG-PET predicts pharmacodynamic response to OSI-906, a dual IGF-1R/IR inhibitor, in preclinical mouse models of lung cancer. Clin Cancer Res. 2011 May 15;17(10):3332-40. 3. Li W, et al. Effectiveness of inhibitor rapamycin, saracatinib, linsitinib and JNJ-38877605 against human prostate cancer cells. Int J Clin Exp Med. 2015 Apr 15;8(4):6563-7.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.372 ml	11.862 ml	23.724 ml
5 mM	0.474 ml	2.372 ml	4.745 ml
10 mM	0.237 ml	1.186 ml	2.372 ml
50 mM	0.047 ml	0.237 ml	0.474 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

OSI-906(Linsitinib),双重IGF-1R和胰岛素受体激酶抑制剂

OSI-906 (Linsitinib)

参考文献

质检证书(COA)

如何获取质检证书(COA)?

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)