CAS NO: | 926259-99-6 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
200mg | 电议 |
Cas No. | 926259-99-6 |
化学名 | (Z)-N-(2-aminophenyl)pyrazine-2-carbimidic acid |
Canonical SMILES | NC1=CC=CC=C1/N=C(O)/C2=CN=CC=N2 |
分子式 | C11H10N4O |
分子量 | 214.22 |
溶解度 | DMF: 5 mg/ml,DMSO: 30 mg/ml,Ethanol: 20 mg/ml,PBS (pH 7.2): 3 mg/ml |
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 | Description: IC50: 289 nM Histone deacetylases (HDACs) represent novel molecular targets for the treatment of various types of cancers including multiple myeloma (MM). Many HDAC inhibitors have already shown remarkable anti-tumor activities in the preclinical studies, however, their clinical utility is limited due to unfavorable toxicities associated with their broad range HDAC inhibitory effects. BG45 is a novel small molecule HDAC3-selective inhibitor. In vitro: BG45 is reported as an HDAC class I inhibitor with selectivity for HDAC3 over HDAC1, 2. Consistent with HDAC3 knockdown data, BG45 significantly inhibited MM cell growth dose-dependently. Importantly, BG45 also triggered a potent growth inhibitory effect against patient-derived MM cells, without affecting normal donor PBMCs [1]. In vivo: BG45 significantly inhibited MM tumor growth in a dose-dependent fashion. For example, significant differences were observed in control versus BG45 15 mg/kg, control versus BG45 50 mg/kg, and BG45 15 mg/kg versus BG45 50 mg/kg at day 22. Moreover, BG45 50 mg/kg in combination with bortezomib enhanced either single agent activity further. These results confirmed that BG45 triggers in vivo anti-MM activities [1]. Clinical trial: Up to now, BG45 is still in the preclinical development stage. Reference: |