CCT241533 - CAS 1262849-73-9
Catalog number: 1262849-73-9
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C23H27FN4O4
Molecular Weight:
442.48
COA:
Inquire
Targets:
Checkpoint Kinase (Chk)
Description:
CCT241533, a Chk2 inhibitor, has been found to improve the effect of genotoxic cancer therapies. IC50: 3 nM.
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Purity:
95%
Appearance:
Powder
Synonyms:
(6E)-4-fluoro-6-[4-[[(3S,4R)-4-(2-hydroxypropan-2-yl)pyrrolidin-3-yl]amino]-6,7-dimethoxy-1H-quinazolin-2-ylidene]cyclohexa-2,4-dien-1-one;UNII-79D8PWX59X;CHEMBL1236782;1262849-73-9;CCT241533;CCT-241533
Solubility:
10 mM in DMSO
Storage:
-20ºC Freeze
MSDS:
Inquire
Application:
CCT241533 is a Chk2 inhibitor that has been found to improve the effect of genotoxic cancer therapies.
Shelf Life:
As supplied, 2 years from the QC date provided on the Certificate of Analysis, when stored properly
Quantity:
Milligrams-Grams
InChIKey:
IXTQNANZDPZION-KFXCQKJJSA-N
InChI:
InChI=1S/C23H27FN4O4/c1-23(2,30)15-10-25-11-17(15)27-21-13-8-19(31-3)20(32-4)9-16(13)26-22(28-21)14-7-12(24)5-6-18(14)29/h5-9,15,17,25-26,30H,10-11H2,1-4H3,(H,27,28)/b22-14+/t15-,17-/m1/s1
Canonical SMILES:
CC(C)(C1CNCC1NC2=NC(=C3C=C(C=CC3=O)F)NC4=CC(=C(C=C42)OC)OC)O
1.CCT241533 is a potent and selective inhibitor of CHK2 that potentiates the cytotoxicity of PARP inhibitors.
Anderson VE1, Walton MI, Eve PD, Boxall KJ, Antoni L, Caldwell JJ, Aherne W, Pearl LH, Oliver AW, Collins I, Garrett MD. Cancer Res. 2011 Jan 15;71(2):463-72. doi: 10.1158/0008-5472.CAN-10-1252.
CHK2 is a checkpoint kinase involved in the ATM-mediated response to double-strand DNA breaks. Its potential as a drug target is still unclear, but inhibitors of CHK2 may increase the efficacy of genotoxic cancer therapies in a p53 mutant background by eliminating one of the checkpoints or DNA repair pathways contributing to cellular resistance. We report here the identification and characterization of a novel CHK2 kinase inhibitor, CCT241533. X-ray crystallography confirmed that CCT241533 bound to CHK2 in the ATP pocket. This compound inhibits CHK2 with an IC(50) of 3 nmol/L and shows minimal cross-reactivity against a panel of kinases at 1 μmol/L. CCT241533 blocked CHK2 activity in human tumor cell lines in response to DNA damage, as shown by inhibition of CHK2 autophosphorylation at S516, band shift mobility changes, and HDMX degradation. CCT241533 did not potentiate the cytotoxicity of a selection of genotoxic agents in several cell lines.
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Chemical Structure

CAS 1262849-73-9 CCT241533

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