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ICG1101-OSI-906 (Linsitinib)
OSI-906 (Linsitinib),>99%
【英文同義名】:OSI-906, Kinome_3532, OSI-906AA, OSI906, ASP-7487, OSI-906, 867160-71-2
訂購信息:(*,常備現(xiàn)貨)
品 牌 | 產(chǎn)品名稱 | 產(chǎn)品貨號(hào) | 規(guī) 格 | 目錄價(jià)(元) |
Gene Operation | OSI-906 (Linsitinib) | ICG1101-0005MG | 5 mg | ¥1,159.00 |
ICG1101-0010MG | 10 mg | ¥1,929.00 | ||
ICG1101-0050MG | 50 mg | ¥5,329.00 | ||
ICG1101-0100MG | 100 mg | ¥8,519.00 |
產(chǎn)品描述
OSI-906 (Linsitinib) 是一種可以口服的、高效的IGF-IR和Ins R小分子抑制劑,其IC50分別為35 nM和75 nM。OSI-906通過抑制IGF-IR和IR,阻止配體誘導(dǎo)的激活下游信號(hào)通路,包括AKT,ERK1 / 2和p-p70S6K等,從而抑制多種腫瘤細(xì)胞的增殖。OSI-906 作用于IGF-IR驅(qū)動(dòng)的移植瘤鼠模型時(shí),顯示強(qiáng)力的抗腫瘤功效 [1]。OSI-906也能抑制NCI-H292小鼠移植瘤生長 [2]。OSI-906能阻斷LCC6移植瘤中IGF-1信號(hào)通路,OSI-906和doxorubicin聯(lián)用能顯著提高doxorubicin的抗腫瘤作用 [3]。OSI-906已進(jìn)入II期臨床試驗(yàn)用于治療多發(fā)性骨髓瘤。
靶點(diǎn)
靶點(diǎn) | IGF-IR | Ins R |
IC50(半數(shù)有效濃度) | 35 nM | 75 nM [1] |
化學(xué)特性
Cas No.: 867160-71-2 | M. Wt.: 421.49 |
Formula: C26H23N5O | Purity: >99% |
Synonym: OSI-906, Kinome_3532, OSI-906AA, OSI906, ASP-7487, OSI-906, 867160-71-2 | |
Chemical Name: (1s,3s)-3-(8-ami-(2-phenylquinolin-7-yl)imidazo[1,5-a]pyrazin-3-yl)-1-methylcyclobutanol | |
Appearance: White to off-white powder | |
Solubility: Soluble in DMSO (up to 199 mM) | |
Storage:Store powder at -20 ºC for the stability of three years |
儲(chǔ)存液配制
儲(chǔ)存液 (1 ml DMSO體系) | 1 mM | 5 mM | 10 mM | 25 mM | 50 mM | 100 mM |
質(zhì)量(mg) | 0.4215 | 2.1075 | 4.2149 | 10.5373 | 21.0745 | 42.1490 |
結(jié)構(gòu)式
使用濃度(僅作參考)
OSI-906 (Linsitinib)的具體使用濃度請(qǐng)參考相關(guān)文獻(xiàn),并根據(jù)自身實(shí)驗(yàn)條件(如實(shí)驗(yàn)?zāi)康?,?xì)胞種類,培養(yǎng)特性等)進(jìn)行摸索和優(yōu)化。
參考文獻(xiàn)
[1] Mulvihill, M. J. et al. Discovery of OSI-906: a selective and orally efficacious dual inhibitor of the IGF-1 receptor and insulin receptor. Future medicinal chemistry 1, 1153-1171 (2009).
[2] McKinley, E. T. et al. 18FDG-PET predicts pharmacodynamic response to OSI-906, a dual IGF-1R/IR inhibitor, in preclinical mouse models of lung cancer. Clinical cancer research : an official journal of the American Association for Cancer Research 17, 3332-3340 (2011).
[3] Zeng, X., Zhang, H., Oh, A., Zhang, Y. & Yee, D. Enhancement of doxorubicin cytotoxicity of human cancer cells by tyrosine kinase inhibition of insulin receptor and type I IGF receptor. Breast cancer research and treatment 133, 117-126(2012).