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Submit ReviewCCT 241533 dihydrochloride
Description: Potent Chk2 inhibitor
Chemical Name: (3R,4S)-4-[[2-(5-Fluoro-2-hydroxyphenyl)-6,7-dimethoxy-4-quinazolinyl]amino]-α,α-dimethyl-3-pyrrolidinemethanol dihydrochloride
Purity: ≥98% (HPLC)
Biological Activity for CCT 241533 dihydrochloride
CCT 241533 dihydrochloride is a 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.
Licensing Information
Sold under license from Cancer Research Technology Ltd (Ximbio).
External Portal Information for CCT 241533 dihydrochloride
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.
Compound Libraries for CCT 241533 dihydrochloride
CCT 241533 dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for CCT 241533 dihydrochloride
| M. Wt | 515.41 |
| Formula | C23H27FN4O4.2HCl |
| Storage | Desiccate at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 1962925-28-5 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for CCT 241533 dihydrochloride
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 5.15 | 10 with gentle warming | |
| DMSO | 51.54 | 100 |
Preparing Stock Solutions for CCT 241533 dihydrochloride
The following data is based on the product molecular weight 515.41. Batch specific molecular weights may vary from batch to batch due to the degree 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 |
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Product Datasheets for CCT 241533 dihydrochloride
References for CCT 241533 dihydrochloride
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for CCT 241533 dihydrochloride, please let us know.
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Keywords: CCT 241533 dihydrochloride, CCT 241533 dihydrochloride supplier, checkpoint, kinase, 2, CHK, inhibitors, inhibits, radioprotectant, potent, selective, Checkpoint, Kinases, Control, 4968, Tocris Bioscience
Citations for CCT 241533 dihydrochloride
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Cell Cycle & DNA Damage Repair Poster
In normal cells, each stage of the cell cycle is tightly regulated, however in cancer cells many genes and proteins that are involved in the regulation of the cell cycle are mutated or over expressed. This poster summarizes the stages of the cell cycle and DNA repair. It also highlights strategies for enhancing replicative stress in cancer cells to force mitotic catastrophe and cell death.