产品信息
抗原名称
Wee1；Myt1；Chk1
商品描述
PD0166285 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations.PD0166285 is a novel G2 checkpoint abrogator.
分子量
512.43
纯度
＞98%
可溶性
DMSO : 65 mg/mL (126.85 mM; Need ultrasonic)
In vitro(体外研究)
PD0166285 is identified to inhibit Wee1 activity at nanomolar concentrations. The inhibitor abrogates G2/M checkpoint inducing early cell division. At the cellular level, 0.5 μM PD0166285 dramatically inhibits irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in seven of seven cancer cell lines tested. This G2 checkpoint abrogation by PD0166285 is demonstrated to kill cancer cells.PD0166285 does not inhibit Cdc2/cyclin B but inhibits Chk1 kinase at a much higher concentration (3433 nM). the treatment of cells with the inhibitor is related to microtubule stabilization and decrease in cyclin D transcription. Thus, PD0166285 may be a potentially useful anti-cancer therapy.
In vivo(体内研究)
PD0166285 at 0.5 μM concentration can inhibit Cdc2Y15 /T14 phosphorylation in all cell lines tested, regardless of their p53 status and pharmacological targeting of WEE1 by PD0166285 sensitizes U251-FM GBM tumors to IR in vivo.
背景
别名
PD 0166285; PD-0166285
分子式
C26H27Cl2N5O2
CAS号
185039-89-8
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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