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Formula | C23H22ClN5O |
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Molecular Weight | 419.91 | CAS No. | 405168-58-3 | |
Solubility (25°C)* | In vitro | DMSO | 7 mg/mL (16.67 mM) | |
Water | Insoluble | |||
Ethanol | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | CHIR-124 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2. | ||||||||
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In vitro | CHIR-124 is a quinolone-based small molecule that is structurally unrelated to other known inhibitors of Chk1. CHIR-124 interacts synergistically with topoisomerase poisons (e.g., Camptothecin or SN-38) in causing growth inhibition in a variety of cancer cell lines, including breast carcinoma (MDA-MB-231 and MDA-MB-435) and colon carcinoma (SW-620 and Colo205), all of which contains the mutant p53 gene. CHIR-124 abrogates the SN-38-induced S and G2-M checkpoints and potentiates apoptosis in MDA-MD-435 breast cancer cells. The abrogation of the G2-Mcheckpoint and induction of apoptosis by CHIR-124 are enhanced by the loss of p53. [1] CHIR-124 also potently targets other kinases such as PDGFR and Flt3 with IC50 of 6.6 nM and 5.8 nM, respectively. [2] | ||||||||
In vivo | CHIR-124 potentiates the growth inhibitory effects of Irinotecan by abrogating the G2-M checkpoint and increasing tumor apoptosis in an orthotopic breast cancer xenograft model. |
Kinase Assay:[1] |
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Cell Assay:[1] |
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Animal Study:[1] |
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Data from [Oncotarget, 2014, 5(3), 667-78]
Data from [Data independently produced by , , J Pathol, 2015, 236: 348-359]
Data from [Data independently produced by , , J Virol, 2016, 90(20):9433-45]
Data from [Data independently produced by , , Transl Oncol, 2018, 11(1):140-146]
p53-independent tumor suppression by cell-cycle arrest via CREB/ATF transcription factor OASIS [ Cell Rep, 2023, S2211-1247(23)00490-4] | PubMed: 37178686 |
The MRN complex maintains the biliary-derived hepatocytes in liver regeneration through ATR-Chk1 pathway [ NPJ Regen Med, 2023, 8(1):20] | PubMed: 37024481 |
The MRN complex maintains the biliary-derived hepatocytes in liver regeneration through ATR-Chk1 pathway [ npj Regenerative Medicine, 2023, 20-2023)] | PubMed: None |
Alternative Lengthening of Telomeres in Pediatric High-Grade Glioma and Therapeutic Implications [ Cancers (Basel), 2023, 15(12)3070] | PubMed: 37370681 |
The Autonomous Parvovirus Minute Virus of Mice Localizes to Cellular Sites of DNA Damage Using ATR Signaling [ Viruses, 2023, 15(6)1243] | PubMed: 37376543 |
ATR inhibition overcomes platinum tolerance associated with ERCC1- and p53-deficiency by inducing replication catastrophe [ NAR Cancer, 2023, 5(1):zcac045] | PubMed: 36644397 |
Deregulation and epigenetic modification of BCL2-family genes cause resistance to venetoclax in hematologic malignancies [ Blood, 2022, blood.2021014304] | PubMed: 35704690 |
Syntaxin 18 regulates the DNA damage response and epithelial-to-mesenchymal transition to promote radiation resistance of lung cancer [ Cell Death Dis, 2022, 13(6):529] | PubMed: 35668077 |
The SKP2-p27 axis defines susceptibility to cell death upon CHK1 inhibition [ Mol Oncol, 2022, 16(15):2771-2787] | PubMed: 35673965 |
Identification of New Vulnerabilities in Conjunctival Melanoma Using Image-Based High Content Drug Screening [ Cancers (Basel), 2022, 14(6)1575] | PubMed: 35326726 |
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