WEE1-IN-5

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

WEE1-IN-5 

WEE1-IN-5 (Debio 0123) 是一种口服有效的高特异性 WEE1 抑制剂，IC50 值在低纳摩尔范围内。WEE1-IN-5 抑制磷酸化 CDC2。Debio 0123 可增强 Carboplatin 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

WEE1-IN-5 Chemical Structure

CAS No. : 2243882-74-6

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生物活性

WEE1-IN-5 (Debio 0123) is a potent, orally available and highly specific WEE1 inhibitor with an IC50 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 antitumoral activity of Carboplatin in vivo where neither agent was active alone[1].

IC50 & Target

IC50: 0.8 nM (WEE1)[1]
体外研究
(In Vitro)

WEE1-IN-5 exhibits an EC50 of 188 nM in pCDC2 and an IC50 shift for CYP3A4/5[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

511.45

Formula

C26H28Cl2N6O
CAS 号

2243882-74-6
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.
参考文献

  • [1]. H. Gelderblom, et al. 601TiP First-in-human phase I study of a novel oral Wee1 inhibitor (Debio 0123) in combination with carboplatin in patients with advanced solid tumours. Ann Oncol. 2020 Sep; 31: S501-S502.

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