13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
在線訂購 免費訂購熱線：021-59541103 021-60443211
聯系人:高小姐
電話:021-59541103 021-60443211
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Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mM (in 1mL DMSO) 5mg 10mg 25mg 100mg |
| CAS | 1236699-92-5 |
| 別名 |
|
| 化學名 | N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)pyridine-4-carboxamide |
| 分子式 | C15H15FIN3O3 |
| 分子量 | 431.2 |
| 溶解度 | ≥ 21.55mg/mL in DMSO, ≥ 10.36 mg/mL in EtOH with ultrasonic |
| 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：
IC50: ranging from 0.005 to 2 μM for the growth of MM cell lines
The MEK/ERK pathway transmits mitogenic signals to the nucleus and thus regulates the expression of genes that are critical for survival, proliferation, and differentiation. This pathway is often upregulated in cancer as result of oncogenic mutations. MEK is a crucial kinase in this pathway and has been targeted for the therapeutic agents development that block the MEK/ERK signaling cascade. AS 703026 is a novel small molecule MEK inhibitor.
In vitro: AS 703026 binds to the distinctive MEK allosteric site and therefore exhibits exquisite kinase selectivity. The AS 703026 binding to MEK is independent of ATP, and results in enzyme inhibition by prevention of activation. This inhibitor shows strong antiproliferative effect on tumor cell lines bearing oncogenic mutations or amplifications along the MEK/ERK pathway [1].
In vivo: In relevant mouse xenograft models, AS 703026 inhibits tumor growth after oral administration. The effect on tumor growth is dose-dependant and correlates with target modulation in both tumors and blood [1].
Clinical trial: 16 patients were enrolled in the trial. 10 and 6 patients were treated daily with 45 and 60 mg of AS 703026 plus FOLFIRI, respectively. The MTD was considered to be 45 mg/day. Of the 15 patients in the efficacy analysis group, 2 patients had partial response, 9 patients had stable disease, 3 patients had progressive disease as their best overall response and 1 patient could not be evaluated.
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原創作者：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部
賬 號：2169 2341 6278
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