1449578-65-7
1449578-65-7 結(jié)構(gòu)式
基本信息
中文別名
化合物 T10428 英文別名
AZ82KIFC1 inhibitor AZ82
KIFC1 Inhibitor, AZ82 - CAS 1449578-65-7 - Calbiochem
3-Pyridinepropanamide, α-[[(5-methyl-4-propyl-2-thienyl)carbonyl]amino]-N-(3R)-3-pyrrolidinyl-6-[3-(trifluoromethoxy)phenyl]-, (αR)-
5-methyl-N-[(2R)-1-oxo-1-[[(3R)-pyrrolidin-3-yl]amino]-3-[6-[3-(trifluoromethoxy)phenyl]pyridin-3-yl]propan-2-yl]-4-propylthiophene-2-carboxamide
物理化學(xué)性質(zhì)
沸點(diǎn)707.9±60.0 °C(Predicted)
密度1.32±0.1 g/cm3(Predicted)
儲(chǔ)存條件+2C to +8C
溶解度DMF: 20 mg/ml; DMSO: 20 mg/ml; Ethanol: 20 mg/ml; Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml
酸度系數(shù)(pKa)13.25±0.46(Predicted)
形態(tài)黃色薄膜
顏色White to off-white
常見問題列表
生物活性
AZ82 是一種驅(qū)動(dòng)蛋白樣蛋白 KIFC1 (HSET/KIFC1) 的選擇性抑制劑，其 Ki 值和 IC50 值分別為 43 nM 和 300 nM。靶點(diǎn)
|
HSET/KIFC1 300 nM (IC 50 ) |
HSET/KIFC1 43 nM (Ki) |
體外研究
AZ82 is shown to specifically induce multipolar spindles in BT-549 cells, but not in cancer cells with normal centrosome number, such as HeLa. AZ82 binds specifically to KIFC1/MT complex but not to KIFC1 or MT alone. Treatment with AZ82 caused centrosome declustering in BT-549 breast cancer cells with amplified centrosomes. AZ82 inhibits both processes with an IC 50 of 0.90 ± 0.09 μM for mant-ATP binding and 1.26 ± 0.51 μM for mant-ADP releasing.