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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].
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $96 | In Stock | |
5 mg | $239 | In Stock | |
10 mg | $378 | In Stock | |
25 mg | $639 | In Stock | |
50 mg | $913 | In Stock | |
100 mg | $1,230 | In Stock | |
1 mL x 10 mM (in DMSO) | $269 | In Stock |
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]. |
Alias | WEE1-IN-5 |
Molecular Weight | 511.45 |
Formula | C26H28Cl2N6O |
Cas No. | 2243882-74-6 |
Smiles | CN1CCC(CC1)c1ccc(Nc2ncc3C(=O)N(CN(C)c3n2)c2c(Cl)cccc2Cl)cc1C |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 18 mg/mL (35.2 mM), Sonication and heating to 60℃ are recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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