產(chǎn)品屬性：
產(chǎn)品名稱 | 規(guī)格 | CAS號(hào) | 型號(hào) |
AXL1717 | 10mM (in 1mL DMSO) 10mg 50mg 250mg | 477-47-4 | EY-Y0165132 |
Cas No.477-47-4
別名 Picropodophyllotoxin;Picropodophyllin;PPP;AXL-1717;AXL 1717
化學(xué)名 (5R,5aR,8aS,9R)-5-hydroxy-9-(3,4,5-trimethoxyphenyl)-5a,6,8a,9-tetrahydro-5H-[2]benzofuro[5,6-f][1,3]benzodioxol-8-one
分子式 C22H22O8
分子量 414.41
溶解度 ≥ 20.7 mg/mL in DMSO
儲(chǔ)存條件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產(chǎn)品描述：
AXL1717 (Picropodophyllotoxin) is a selective inhibitor of IGF-1R with IC50 value rangs from 0.24-0.33 μM [1].
IGF-1R (type 1 insulin-like growth factor receptor) is a transmembrane receptor that activated by IGF-1 and plays an important role in cell growth and anabolic effects in adults. It has been reported that over-expression of IGF-1R is correlated with a variety of cancers and its inhibitors has been revealed to anti-cancer in clinical study [1] [2].
AXL 1717 is a potent IGF-1RTK inhibitor and has ability to inhibit tumor cells combined with HDAC inhibitor LBH589. When tested with 4 human myeloma cells (RPMI 8226, Karpas707, LP-1, and OPM-2) and 1 murine cell (5T33MM), AXL1717 treatment markedly decreased cell survival in a dose-dependent manner, arrested cell cycle in G2-M phase and induced cell apoptosis by inhibiting IGF-1RTK [1]. In four colon carcinoma cell lines (HT-29, HCT-116, DLD-1 and CaCO-2), AXL1717 treatment showed high ability to inhibit cell proliferation and migration in a dose-dependent manner [2].
In mouse model with 5TMM subcutaneous xenograft, administration of AXL 1717 (1.5 mg/d) resulted in a prolonged survival in combination with LBH (2.5 mg/kg/d) compared with control group [1].
AXL1717 has been tested to treat non-small cell lung cancer patients in a Phase I/II clinically [3].
References:
[1].Lemaire, M., et al., The HDAC inhibitor LBH589 enhances the antimyeloma effects of the IGF-1RTK inhibitor picropodophyllin. Clin Cancer Res, 2012. 18(8): p. 2230-9.
[2].Feng, X., et al., Multiple antitumor effects of picropodophyllin in colon carcinoma cell lines: clinical implications. Int J Oncol, 2012. 40(4): p. 1251-8.
[3].Ekman, S., et al., Clinical Phase I study with an Insulin-like Growth Factor-1 receptor inhibitor: experiences in patients with squamous non-small cell lung carcinoma. Acta Oncol, 2011. 50(3): p. 441-7.
關(guān)鍵字： 477-47-4;C22H22O8;AXL1717;
上海一研生物科技有限公司Shanghai yiyan bio-technology Co. Ltd.主要從事免疫學(xué)、分子生物學(xué)和常規(guī)生化試劑等為一體的科研產(chǎn)品銷售企業(yè)，公司自成立以來(lái)，秉承""全心全意服務(wù)于科研工作者""的企業(yè)理念，立足生物科技領(lǐng)域，運(yùn)用生物技術(shù)和科研試劑，發(fā)展現(xiàn)代生物科技，為各類大中小醫(yī)院及其它醫(yī)療機(jī)構(gòu)、高等院校、科研院所、企事業(yè)單位提供優(yōu)質(zhì)的產(chǎn)品，服務(wù)生物科技領(lǐng)域的科學(xué)研究人員。
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