Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H12N4O2 |
| Molecular Weight | 340.3349 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)C1=CC=C2C(=C1)N=C(NC3=CC=CC(=C3)C#C)C4=NC=NC=C24
InChI
InChIKey=HJGFPNFAFSFDNN-UHFFFAOYSA-N
InChI=1S/C20H12N4O2/c1-2-12-4-3-5-14(8-12)23-19-18-16(10-21-11-22-18)15-7-6-13(20(25)26)9-17(15)24-19/h1,3-11H,(H,23,24)(H,25,26)
| Molecular Formula | C20H12N4O2 |
| Molecular Weight | 340.3349 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
DescriptionCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/26919095
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/pubmed/26919095
CX-5011, which was synthesized by Cylene Pharmaceutical, possesses an unprecedented selectivity towards the casein kinase II (CK2) versus other kinases. CK2 is a pleiotropic protein kinase, which regulates many survival pathways and plays a global anti-apoptotic function. It is highly expressed in tumor cells, and is presently considered a promising therapeutic target. Recently was discovered, that the ternary mixture containing CX-5011, imatinib and U0126 represents the most effective synergistic combination to counteract chronic myeloid leukaemia CML cell viability. Co-targeting CK2 and MEK protein kinases is a promising strategy to restore responsiveness of resistant CML cells to imatinib.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| Unprecedented selectivity and structural determinants of a new class of protein kinase CK2 inhibitors in clinical trials for the treatment of cancer. | 2011 Oct 4 |
|
| Effects of the CK2 inhibitors CX-4945 and CX-5011 on drug-resistant cells. | 2012 |
|
| Inhibition of protein kinase CK2 by CX-5011 counteracts imatinib-resistance preventing rpS6 phosphorylation in chronic myeloid leukaemia cells: new combined therapeutic strategies. | 2016 Apr 5 |
Sample Use Guides
CX-5011 acts as a pro-apoptotic agent and the inhibitor concentration required to induce apoptosis in imatinib-resistant KCL22 cells is much lower than that effective in sensitive cell line. R-KCL22 cells were treated with DMSO (Ctrl) or the indicated concentrations of CX-5011 (2-10 uM) for 4 h.
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 09:34:34 GMT 2023
by
admin
on
Sat Dec 16 09:34:34 GMT 2023
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| Record UNII |
GY6276ICQJ
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| Record Status |
Validated (UNII)
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| Record Version |
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1009821-06-0
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