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CCT244747

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Catalog No. T14904Cas No. 1404095-34-6
Alias CCT 244747

CCT244747 is a potent and highly selective CHK1 inhibitor that is orally active, ATP-competitive, and cytotoxic, abrogating drug-induced S and G2 blockade and inducing apoptosis in multiple tumor cell lines.

CCT244747

CCT244747

😃Good
Purity: 99.17%
Catalog No. T14904Alias CCT 244747Cas No. 1404095-34-6
CCT244747 is a potent and highly selective CHK1 inhibitor that is orally active, ATP-competitive, and cytotoxic, abrogating drug-induced S and G2 blockade and inducing apoptosis in multiple tumor cell lines.
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2 mg$76 5 days
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Purity:99.17%
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Product Introduction

Bioactivity
Description
CCT244747 is a potent and highly selective CHK1 inhibitor that is orally active, ATP-competitive, and cytotoxic, abrogating drug-induced S and G2 blockade and inducing apoptosis in multiple tumor cell lines.
Targets&IC50
Chk1:7.7 nM
In vitro
Methods: HT29 and SW620 colon cancer cell lines were treated with CCT244747 (0.01, 0.05, 0.1, 0.5, 1, 2, 5 μM) to characterize its effects on drug-induced changes in CHK1 and cell cycle biomarkers.
Results CCT244747 inhibited SN38- and gemcitabine-induced CHK1 activity in tumor cells, and this was associated with abrogation of cell cycle arrest, induction of DNA damage, and apoptosis. [4]
In vivo
Methods: Athymic mice bearing SW620 human colon cancer xenografts were treated with CCT244747 (100-300 mg/kg, oral) followed by gemcitabine (60 mg/kg, intravenous) 1 hour later to further analyze the pharmacodynamics of CCT244747.
Results: A single oral dose of CCT244747 (100-300 mg/kg) maintained inhibition of gemcitabine-induced pS296 CHK1 in HT29 colon tumor xenografts for up to 24 hours. [1]
AliasCCT 244747
Chemical Properties
Molecular Weight408.46
FormulaC20H24N8O2
Cas No.1404095-34-6
SmilesO(C)C=1C(=CN=C(NC2=NC(O[C@@H](CN(C)C)C)=C(C#N)N=C2)C1)C=3C=NN(C)C3
Relative Density.1.27 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 40 mg/mL (97.93 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.4482 mL12.2411 mL24.4822 mL122.4110 mL
5 mM0.4896 mL2.4482 mL4.8964 mL24.4822 mL
10 mM0.2448 mL1.2241 mL2.4482 mL12.2411 mL
20 mM0.1224 mL0.6121 mL1.2241 mL6.1206 mL
50 mM0.0490 mL0.2448 mL0.4896 mL2.4482 mL

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