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PD0166285 dihydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PD0166285 dihydrochloride图片
CAS NO:212391-63-4
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
PD0166285 dihydrochloride是 P-gp 的一个底物,是WEE1抑制剂,也可微弱抑制Myt1IC50值分别为 24 和 72 nM。PD0166285 dihydrochloride 对 Chk1 的 IC50值为3.433 μM。
生物活性

PD0166285 dihydrochloride, a substrate of P-gp, is aWEE1inhibitor and a weakMyt1inhibitor withIC50values of 24 and 72 nM, respectively. PD0166285 dihydrochloride exhibits an IC50of 3.433 μM forChk1[1].

IC50& Target

IC50: 24 nM (WEE1), 72 nM (Myt1), 3.433 μM (Chk1)[1].

体外研究
(In Vitro)

PD0166285 (0.5 μM) dramatically inhibits irradiation-induced Cdc2 phosphorylation at the Tyr-15 and Thr-14 in seven of seven cancer cell lines[1].
PD0166285 sensitizes radiation-induced cell killing in p53 mutant HT29 cells and in the E6-transfected, p53-null ovarian cancer cell line PA-1 but to a lesser extent in p53 wild-type PA-1 cells. PD0166285 abrogates irradiation-induced G2 arrest and significantly increases mitotic cell populations[1].
PD0166285 acts as a radiosensitizer to sensitize cells to radiation-induced cell death with a sensitivity enhancement ratio of 1.23[1].

Western Blot Analysis[1]

Cell Line:Human and mouse cancer cell lines (HCT116, HT29, DLD-1, HCT8, H460, HeLa, C 26).
Concentration:0.5 μM.
Incubation Time:4 h.
Result:Inhibited Cdc2Y15 and CdcT14 phosphorylation.
体内研究
(In Vivo)
Animal Model:Wild-type, Abcg2-/-, Abcb1a/b-/-and Abcb1a/b;Abcg2-/-FVB mice[2].
Dosage:5 mg/kg.
Administration:IV.
Result:Cmaxis about 400 ng/mL.
P-gp, but not BCRP, limited the brain penetration of PD0166285.
分子量

585.35

Formula

C26H29Cl4N5O2

CAS 号

212391-63-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.