Atrasentan hydrochloride
- ABT-627, ABT627, ABT 627
货号: abs811604
货号-规格 | 货期 | 价格 | 数量 |
abs811604-10mg | 4周 | ¥3791.00 | - + |
abs811604-50mg | 4周 | ¥10219.00 | - + |

产品描述 | ||
描述 | Atrasentan hydrochloride is an endothelin antagonist receptor (IC50=0.0551 nM, ETA) being developed for the treatment of prostate cancer. | |
纯度 | >98% | |
储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. | |
基本信息 | ||
别名 | ABT-627, ABT627, ABT 627 | |
可溶性/溶解性 | 10 mM in DMSO | |
生物活性 | ||
靶点 | Endothelin Receptor | |
In vitro(体外研究) | Atrasentan (ABT-627, 0-50 μM) significantly inhibits LNCaP and C4-2b prostate cancer cell growth. ABT-627 in conbination with Taxotere elicits a significantly greater loss of viable prostate cancer cells relative to either agent alone and shows greater degree of down-regulation of the NF-κB DNA binding activity. Atrasentan profoundly induces several CYPs and drug transporters (e.g. 12-fold induction of CYP3A4 at 50 μM). It is a moderate P-gp inhibitor (IC50 in P388/dx cells=15.1±1.6 μM) and a weak BCRP inhibitor (IC50 in MDCKII-BCRP cells=59.8±11 μM). | |
In vivo(体内研究) | Atrasentan (3 mg/kg, p.o.) inhibits the pressor response induced by big endothelin-1 (1 nmol/kg) in pithed rats. Aatrasentan (ABT-627, 10 mg/kg, i.p.) as well as Taxotere alone inhibited the C4-2b tumor growth within the bone environment to some extent in the SCID-hu model. | |
温馨提示:本产品仅作科研实验使用,不支持临床等研究 |
- 实验方法 实验条件
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