13585831301
021-59541103 021-60443211
3004967995
13585831301021-59541103 021-604432113004967995
聯系人:高小姐
電話:021-59541103 021-60443211
手機:13585831301
Q Q： 3004967995
Email:3004967995@qq.com
詳細地址：上海嘉定區嘉羅公路1661
化學性質：
| 規格 | 10mM (in 1mL DMSO) 5mg 10mg 50mg |
| CAS | 5608-24-2 |
| 別名 |
|
| 化學名 | 2,2-bis(hydroxymethyl)-1-azabicyclo[ |
| 分子式 | C9H15NO3 |
| 分子量 | 185.22 |
| 溶解度 | DMF: 30 mg/ml,DMSO: 30 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 50 mg/ml |
| 儲存條件 | Store at 4°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: The value varied among different tumor type. In Saos-2-His-273 cells, PRIMA-1 induced cell death with an IC50 of over 15 M.
PRIMA-1, a novel low molecular weight compound, rescues the tumor-suppressing function of mutant p53 proteins and shows anti-tumor activity in vivo. P53 severs as a crucial tumor suppressor and mutant p53 is expressed at high levels in many tumors. PRIMA-1 is considered as a lead compound for the development of anticancer drugs targeting mutant p53. [1]
In vitro: The substantial increase in Saos-2-His-273-cells death could be noticed after being treated with 125 μM PRIMA-1 for 48 hours. TUNEL staining revealed that such tumor-cell death was primarily triggered by apoptosis. PRIMA-1 could also restore the transcriptional transactivation function to mutant p53 in vitro. [2]
In vivo: To assess the effect of PRIMA-1 on human tumor xenografts, mice were inoculated with Saos-2-His-273 cells expressing mutant p53. The mice then received PRIMA-1 treatment at intra-tumor does of 20 mg/kg or i.v. doses of 20 and 100 mg/kg twice a day for three days. Compared with the control group, the average tumor volume decreased from 555.7 mm3 to 11.7 (100 mg/kg) and 53 (20 mg/kg) mm3 after i.v. injections of PRIMA-1. Intra-tumor injections of PRIMA-1 also decreased the average tumor volume to 5.3 mm3. [2]
Clinical trial: The methylated form of PRIMA-1, PRIMA-1MET was tested on 22 patients with hematologic malignancies and prostate cancer. Based on the clinical data, PRIMA-1MET was safe at predicted therapeutic dose, had a favorable pharmacokinetic profile and could lead to apoptosis of tumor cells in the p53–dependent manner. [3]
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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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