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MedChemExpressModel WEE1-IN-5 -2243882-74-6

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WEE1-IN-5 is a potent WEE1 inhibitor with an IC50 value of 0.8 nM. WEE1-IN-5 inhibits phospho-CDC2. WEE1-IN-5 abrogates the G2 check point, increasing sensitivity to DNA damaging agents in cancer cells. WEE1-IN-5 can be used for researching anticancer[1].
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WEE1-IN-5

MCE China:WEE1-IN-5

Brand:MedChemExpress (MCE)

Cat. No.HY-147054

CAS:2243882-74-6

Purity:99.46%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:WEE1-IN-5 is a potent WEE1 inhibitor with an IC50 value of 0.8 nM. WEE1-IN-5 inhibits phospho-CDC2. WEE1-IN-5 abrogates the G2 check point, increasing sensitivity to DNA damaging agents in cancer cells. WEE1-IN-5 can be used for researching anticancer.

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

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].

IC50 & Target:IC50: 0.8 nM (WEE1), 188 nM (CDC2)[1] In Vitro WEE1-IN-5 exhibits an EC50 of 188 nM in pCDC2 and an IC50 shift for CYP3A4/5[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> WEE1-IN-5 Related Antibodies

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References:

[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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