Debio-0123 [2243882-74-6]

Cat# T9864-5mg

Size : 5mg

Brand : TargetMol

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Debio-0123

(Synonyms: WEE1-IN-5) Copy Product Info
Debio-0123 (WEE1-IN-5) is a potent, orally available and highly specific WEE1 inhibitor with an IC 50 in the low nanomolar range. Debio-0123 inhibits phospho-CDC2 which translated into an increase in DNA damage and premature entry into mitosis. Debio-0123 increases the antitumoral activity of Carboplatin in vivo whereas neither agent was active alone [1].
Debio-0123
Cas No. 2243882-74-6
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.93%
Appearance:Solid
Color:White
COA LCMS HNMR

Product Introduction

Bioactivity
Description
Debio-0123 (WEE1-IN-5) is a potent, orally available and highly specific WEE1 inhibitor with an IC 50 in the low nanomolar range. Debio-0123 inhibits phospho-CDC2 which translated into an increase in DNA damage and premature entry into mitosis. Debio-0123 increases the antitumoral activity of Carboplatin in vivo whereas neither agent was active alone [1].
In vitro
WEE1-IN-5 shows an EC 50 of 188 nM in pCDC2 and an IC 50 shift for CYP3A4/5 [1].
In vivo
WEE1-IN-5, administered as a single dose of 5mg/kg orally (PO) and 1mg/kg intravenously (IV), demonstrates a clearance rate (CL) of 14 mL/min/kg, an area under the curve (AUC) of 1324 h·ng/mL, and a bioavailability of 35% in SD rats [1].
SynonymsWEE1-IN-5
Chemical Properties
Molecular Weight511.45
FormulaC26H28Cl2N6O
Cas No.2243882-74-6
SmilesCN1CCC(CC1)c1ccc(Nc2ncc3C(=O)N(CN(C)c3n2)c2c(Cl)cccc2Cl)cc1C
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (97.76 mM), Sonication and heating to 60℃ are recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 1 mg/mL (1.96 mM), Sonication is recommended.
10% DMSO+90% Saline: 5 mg/mL (9.78 mM), Suspension.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9552 mL9.7761 mL19.5523 mL97.7613 mL
5 mM0.3910 mL1.9552 mL3.9105 mL19.5523 mL
10 mM0.1955 mL0.9776 mL1.9552 mL9.7761 mL
20 mM0.0978 mL0.4888 mL0.9776 mL4.8881 mL
50 mM0.0391 mL0.1955 mL0.3910 mL1.9552 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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