规格

价格

库存

数量

25 mg

待询

5日内发货

50 mg

待询

5日内发货

100 mg

待询

5日内发货

生物活性

产品描述	CFI-400945 is an orally active, potent, and selective inhibitor of polo-like kinase 4.
靶点活性	AURKB/INCENP:98 nM, TRKA:6 nM, TIE2/TEK:22 nM, AURKA:140 nM, PLK4:2.8 nM, TRKB:9 nM
体外活性	In an assay using recombinant human PLK4, CFI-400945 inhibited PLK4 (IC50: 2.8 ± 1.4 nM and Ki: 0.26 ± 0.1 nM in an ATP competitive manner). CFI-400945 inhibited autophosphorylation of PLK4 at serine 305 (EC50: 12.3 nM in cells overexpressing PLK4). CFI-400945 showed no significant inhibitory activity against other PLK family members (PLK1, PLK2, and PLK3 with the IC50s of > 50 μM). In transfected HCT116 cells with TRKA, TRKB, and Tie2/TEK, the EC50 values were 84 nM, 88 nM, and 117 nM, respectively. CFI-400945 inhibited the activity of AURKA and AURKB with the EC50 value of 510 nM and 102 nM. CFI-400945 (≥ 200 nM) decreased the mean centriole number in asynchronous U2OS cells. CFI-400945 inhibited a panel of breast cancer cell growth with the GI50 of 14-165 nM [1].
体内活性	In mice, the maximum tolerated dose (MTD) of CFI-400945 for once-daily oral administration was estimated to be 7.5-9.5 mg/kg [1].

化学信息

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 10 mg/mL (15.37 mM), Sonication is recommended.

Ethanol: ≤12 mg/mL, Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 1 mg/mL (1.54 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO

CFI-400945