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ICG1102-NVP-AEW541
NVP-AEW541,≥98%
【英文同義名】:AEW-541, AEW541, AEW 541, 475489-16-8, SureCN94862, SureCN1441421, SureCN1987652
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 | ICG1102-0002MG | 2 mg | ¥1,679.00 | |
ICG1102-0005MG | 5 mg | ¥2,989.00 | ||
ICG1102-0010MG | 10 mg | ¥5,279.00 | ||
ICG1102-0050MG | 50 mg | ¥16,039.00 |
產(chǎn)品描述
是一種高效的IGF-1R抑制劑,其IC50為86 nM。在細(xì)胞水平對(duì)IGF-1R的選擇性是InsR的27倍以上。能夠抑制移植瘤IGF-1R信號(hào)傳導(dǎo)在并能顯著降低IGF-IR的誘導(dǎo)纖維肉瘤在體內(nèi)的生長 [1]。特異性的抑制TC-71細(xì)胞中IGF-I介導(dǎo)的細(xì)胞生長和信號(hào)傳導(dǎo),并抑制肉瘤細(xì)胞系細(xì)胞周期進(jìn)程并誘導(dǎo)G1期阻滯 [2]。抑制IGF-Ⅱ介導(dǎo)的IGF-IR和Akt通路, 除了抑制細(xì)胞生長外,也能誘導(dǎo)體外細(xì)胞的凋亡??诜?/span>能抑制成神經(jīng)細(xì)胞移植瘤裸鼠腫瘤的生長 [3]。以時(shí)間和劑量依賴的方式抑制PC3,DU145和22RV1細(xì)胞系細(xì)胞增殖并減弱細(xì)胞活力,也能增強(qiáng)電離輻射對(duì)PTEN野生型前列腺癌細(xì)胞的作用,而對(duì)PTEN缺失細(xì)胞沒有效果 [4]。 和??afatinib聯(lián)用能協(xié)同抑制多數(shù)胰腺癌細(xì)胞的生長 [5]。
靶點(diǎn)
靶點(diǎn) | IGF-IR |
IC50(半數(shù)有效濃度) | 86 nM [1] |
化學(xué)特性
Cas No.: 475489-16-8 | M. Wt.: 439.55 |
Formula: C27H29N5O | Purity: ≥98% |
Synonym: AEW-541, AEW541, AEW 541, 475489-16-8, SureCN94862, SureCN1441421, SureCN1987652 | |
Chemical Name: 7-((1s,3s)-3-(azetidin-1-ylmethyl)cyclobutyl)-5-(3-(benzyloxy)phenyl)-7H-pyrrolo[2,3-d]pyrimidin-4- amine | |
Appearance: white solid 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) | 0.4396 | 2.1978 | 4.3955 | 10.9888 | 21.9775 | 43.9550 |
結(jié)構(gòu)式
使用濃度(僅作參考)
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)康模?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] Garcia-Echeverria, C. et al. In vivo antitumor activity of -A novel, potent, and selective inhibitor of the IGF-IR kinase. Cancer cell 5, 231-239 (2004).
[2] Scotlandi, K. et al. Antitumor activity of the insulin-like growth factor-I receptor kinase inhibitor in musculoskeletal tumors. Cancer research 65, 3868-3876(2005).
[3] Tanno, B. et al. Down-regulation of insulin-like growth factor I receptor activity by has an antitumor effect on neuroblastoma cells in vitro and in vivo. Clinical cancer research : an official journal of the American Association for Cancer Research 12, 6772-6780(2006).
[4] Isebaert, S. F., Swinnen, J. V., McBride, W. H. & Haustermans, K. M. Insulin-like growth factor-type 1 receptor inhibitor enhances radiosensitivity of PTEN wild-type but not PTEN-deficient human prostate cancer cells. International journal of radiation oncology, biology, physics 81, 239-247 (2011).
[5] Ioannou, N., Seddon, A. M., Dalgleish, A., Mackintosh, D. & Modjtahedi, H. Treatment with a combination of the ErbB (HER) family blocker afatinib and the IGF-IR inhibitor, induces synergistic growth inhibition of human pancreatic cancer cells. BMC cancer 13, 41 (2013).