Biological Activity
Potent Chk2 inhibitor (IC50 = 3 nM). Shows >63-fold selectivity for Chk1 over Chk2 and a panel of 84 other kinases. Inhibits Chk2 activation in response to etoposide-induced DNA damage in HT29 cells. Blocks ionizing radiation-induced apoptosis of mouse thymocytes.
External Portal Information
Chemicalprobes.org is a portal that offers independent guidance on the selection and/or application of small molecules for research. The use of CCT 241533 is reviewed on the chemical probes website.
Technical Data
| M. Wt | 515.41 |
| Formula | C23H27FN4O4.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| PubChem ID | 49867844 |
| InChI Key | IXTQNANZDPZION-GSOOIIRJSA-N |
| Smiles | FC1=CC(C3=NC2=CC(OC)=C(OC)C=C2C(N[C@H]4[C@H]([C@](C)(O)C)CNC4)=N3)=C(O)C=C1.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 51.54 | 100 | |
| water | 5.15 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 515.41. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.94 mL | 9.7 mL | 19.4 mL |
| 5 mM | 0.39 mL | 1.94 mL | 3.88 mL |
| 10 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 50 mM | 0.04 mL | 0.19 mL | 0.39 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Caldwell et al (2011) Structure-based design of potent and selective 2-(quinazolin-2-yl)phenol inhibitors of checkpoint kinase 2. J.Med.Chem. 54 580 PMID: 21186793
Keywords: CCT 241533 dihydrochloride, supplier, checkpoint, kinase, 2, CHK, inhibitors, inhibits, radioprotectant, potent, selective, Checkpoint, Kinases, Checkpoint, Control, Kinases, Checkpoint, Kinases, Tocris Bioscience
