| CAS NO: | 310456-65-6 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 25mg | 电议 |
| 100mg | 电议 |
| Cas No. | 310456-65-6 |
| 别名 | [2-甲氧基-4-[(4-氧代-2-硫代-5-噻唑烷亚基)甲基]苯氧基]乙酸乙酯 |
| 化学名 | (E)-ethyl 2-(2-methoxy-4-((4-oxo-2-thioxothiazolidin-5-ylidene)methyl)phenoxy)acetate |
| Canonical SMILES | CCOC(COC1=C(OC)C=C(/C([H])=C(S2)\C(NC2=S)=O)C=C1)=O |
| 分子式 | C15H15NO5S2 |
| 分子量 | 353.41 |
| 溶解度 | ≥ 35.3mg/mL in DMSO |
| 储存条件 | Store at -20℃ |
| 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 |
| 产品描述 | IC50: 26 μmol/L IMR-1 is a inhibitor of Notch pathway. Aberrant Notch activity has been reported to play a important role in the initiation and maintenance of the neoplastic phenotype and in various cancer stem cells, which alludes to its additional involvement in metastasis and resistance. In vitro: In order to determine the effect of IMR-1 on the assembly of the Notch ternary complex (NTC) in cells, Notch-dependent cell lines OE33 and 786-0 were treated with IMR-1 or DAPT. Results showed that treatment of OE33 and 786-0 with IMR-1 could decrease the occupancy of Maml1 on the HES1 promoter but, in contrast to DAPT, IMR-1 treatment could not affect the occupancy of Notch1 on the HES1 promoter. In addition, western blot analyses indicated that IMR-1 treatment did not change the cellular levels of NICD [1]. In vivo: Animal study showed that treatment of mice with 15 mg/kg IMR-1 could readily block tumor establishment. Moreover, IMR-1 treatment at 15 mg/kg caused no observable adverse effects on the animal. In two independent PDX models, IMR-1 could significantly abrogate the tumor growth to a similar level achieved with DAPT treatment, without any significant weight loss or other visible signs of adverse effects in the treated mice [1]. Clinical trial: Up to now, IMR-1 is still in the preclinical development stage. Reference: |
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