| CAS NO: | 186497-07-4 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 186497-07-4 |
| 别名 | 齐泊腾坦,ZD4054 |
| 化学名 | N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide |
| Canonical SMILES | CC1=CN=C(C(=N1)OC)NS(=O)(=O)C2=C(N=CC=C2)C3=CC=C(C=C3)C4=NN=CO4 |
| 分子式 | C19H16N6O4S |
| 分子量 | 424.43 |
| 溶解度 | ≥ 7.2mg/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 |
| 半岛bd体育手机客户端 描述 | ZD4054 is a specific antagonist of the endothelin A receptor. The autocrine endothelin (ET)-1/endothelin A receptor (ETAR) pathway is an important regulator of several processes involved in ovarian cancer progression. In vitro: In the human ovarian cancer ETAR positive cell lines, ZD4054 effectively inhibited the basal and ET-1-induced cell proliferation, with the inhibition of AKT and p42/44MAPK phosphorylation, and increased apoptosis, through the inhibition of bcl-2 and activation of caspase-3 and poly(ADP-ribose) polymerase proteins. [1]. In vivo: In HEY ovarian cancer xenografts, ZD4054 inhibited tumor growth to the same degree as paclitaxel. Moreover, ZD4054-dependent tumor growth inhibition was associated with a reduction in proliferation index, MMP-2 expression, and microvessel microvessel density [2]. Clinical trial: The PK and safety profiles of ZD4054 determined in this Chinese patient population are similar to those previously reported. Findings suggest no clinically relevant inter-ethnic differences in ZD4054 disposition between the patient populations analyzed [3]. References: |
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