Wee1-IN-5 (Debio 0123) 是一种口服有效且高度特异性的Wee1抑制剂，IC50值在低纳摩尔范围内。Wee1-IN-5 抑制磷酸化 CDC2。Wee1-IN-5可增强卡铂在体内的抗肿瘤活性，而这两种药物单独使用都没有活性。

WEE1-IN-5 (Debio 0123) is a potent, orally available and highly specific WEE1 inhibitor with an IC 50 in the low nanomolar range. WEE1-IN-5 inhibits phospho-CDC2 which translated into an increase in DNA damage and premature entry into mitosis. WEE1-IN-5 increases the antitumoral activity of Carboplatin in vivo whereas neither agent was active alone [1].

WEE1-IN-5 shows an EC 50 of 188 nM in pCDC2 and an IC 50 shift for CYP3A4/5 [1].

WEE1-IN-5 (5mg/kg for PO; 1 mg/kg for IV; single dosage) shows a CL of 14 mL/min/kg, an AUC int 1324 h·ng/mL and bioavailability of 35% in SD rats [1].

2243882-74-6

C26H28Cl2N6O

511.45

WEE1-IN-5

DMSO:18mg/mL (35.2mM),ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years