13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
標簽:GSK2126458
聯(lián)系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區(qū)嘉羅公路1661
化學性質：
| 規(guī)格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg |
| CAS | 1086062-66-9 |
| 別名 | GSK212; GSK-2126458; GSK 2126458; GSK-212; GSK 212 |
| 化學名 | 2,4-difluoro-N-[2-methoxy-5-(4-pyridazin-4-ylquinolin-6-yl)pyridin-3-yl]benzenesulfonamide |
| 分子式 | C25H17F2N5O3S |
| 分子量 | 505.5 |
| 溶解度 | ≥ 25.3mg/mL in DMSO |
| 儲存條件 | 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 |
產品描述：
GSK2126458 is an inhibitor of PI3K/mTOR with Ki value of 19 pM for PI3K [1].
PI3K (phosphoinositide 3-kinase) plays an important role in regulating cell growth and transformation, and mTOR (mammalian target of rapamycin) which works as a class IV PI3K protein kinase, is also a crucial regulator of cell growth [2]. It has been shown that up-regulation of PI3K/mTOR (phosphatidylinositol-3' kinase/mammalian target of rapamycin) signaling is widespread in carcinoma which may be worked as a biomarker used in clinic [3].
GSK2126458 is a highly potent inhibitor of PI3K/mTOR. When subjected to colorectal cancer cell lines, GSK2126458 could potentiate the cells antiproliferative activity via combining with DDR1-IN-1[4]. In BT474 breast cancer lines, treated with GSK2126458 could be the arrest of G1 cell cycle and thus inhibit cell proliferation [5]. GSK2126458 also could improve the sensitivity of NPC cells to radiation and suppress tumor progression [1].
In a 5-8F xenograft model with NPC, treated the mouse with GSK2126458 combining of IR significantly inhibited the tumor growth [1]. In mice injected with cancer cells from melanoma patient resisted to the combination of divergent and trametinib, GSK2126458 combined with dabrafenib, trametinib treatment resulted in sustained inhibition of tumor growth[3].
GSK2126458 may play a significant role in regulating autophagy [6].
特別提醒：
1. 本產品僅供科研使用。請勿用于醫(yī)藥、臨床診斷或治療，食品及化妝品等用途。請勿存放于普通住宅區(qū)。
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原創(chuàng)作者：上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名：上海生物
開 戶 行：中國銀行山東省分行營業(yè)部
賬 號：2169 2341 6278
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