Sabizabulin 是一种有效且具有口服生物利用度的 α 和 β 微管蛋白抑制剂,可对抗黑色素瘤和前列腺癌细胞系。 Sabizabulin 通过靶向 HPV E6 和 E7 抑制宫颈癌细胞的肿瘤生长和转移表型。 Sabizabulin 显示出抗增殖活性,可用于前列腺癌研究。
产品描述
Sabizabulin is an effective and orally bioavailable inhibitor of α and β tubulin against panels of melanoma and prostate cancer cell lines. Sabizabulin inhibits tumor growth and metastatic phenotypes of cervical cancer cells via targeting HPV E6 and E7. Sabizabulin shows antiproliferative activity and can be used in prostate cancer studies.
体外活性
Sabizabulin (2.5-80 nM) inhibits Panc-1, AsPC-1 and HPAF-II cells growth in a dose and time-dependent manner with IC50s of 25, 35 and 35 nM for 24 hours and 11.8, 15.5, and 25 nM for 48 hours. Sabizabulin (5-20 nM) inhibits pro-Caspase 3 and 9 and activates Caspase-3 and 9 in a dose-dependent manner. Sabizabulin (5-20 nM) induces the expression of Bax and Bad and inhibits the expression of Bcl-2 and Bcl-xl proteins. Sabizabulin (5-20 nM) dose-dependently arrests Panc-1 and AsPC-1 cells in G2/M phase[4].
体内活性
Sabizabulin (50 μg/mouse; intra-tumorally) potently inhibits tumor growth and shows no apparent toxicity[4].
Cas No.
1332881-26-1
分子式
C21H19N3O4
分子量
377.39
别名
VERU-111;ABI-231
储存和溶解度
DMSO:18mg/mL (47.7mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years