生物活性
Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.
体外研究
(In Vitro)
Centrinone (LCR-263) exhibits more than 1000-fold selectivity for Plk4 over Aurora A/B and does not affect cellular Aurora A or B substrate phosphorylation at concentrations that deplete centrosomes. Centrinone (LCR-263) treatment of HeLa human cervical carcinoma cells leads to a progressive reduction in foci containing centriolar and pericentriolar material markers at each round of cell division, until most cells lack centrioles and centrosomes. Treatment with Centrinone (LCR-263) reduces centriole number in multiciliated Xenopus epithelial cells, which indicates that Plk4 also controls centriole amplification in differentiated cells. Centrinone (LCR-263) treatment causes centrosome depletion in human and other vertebrate cells. Centrosome loss irreversibly arrests normal cells in a senescence-like G1 state by a p53-dependent mechanism that is independent of DNA damage, stress, Hippo signaling, extends mitotic duration, or segregation errors[1].
分子量
633.65
性状
Solid
Formula
C26H25F2N7O6S2
CAS 号
1798871-30-3
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro:
DMSO : ≥ 31 mg/mL (48.92 mM)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度溶剂体积质量 1 mg 5 mg 10 mg
1 mM 1.5782 mL 7.8908 mL 15.7816 mL
5 mM 0.3156 mL 1.5782 mL 3.1563 mL
10 mM 0.1578 mL 0.7891 mL 1.5782 mL
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂: