405168-58-3

Basic information

• Product Name: CHIR-124
• Synonyms: CHIR-124;2(1H)-Quinolinone, 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylaMino]-3-(1H-benziMidazol-2-yl)-6-chloro-;4-[((3S)-1-Azabicyclo[2.2.2]oct-3-yl)amino]-3-(1H-benzimidazol-2-yl)-6-chloroquinolin-2(1H)-one
• CAS NO: 405168-58-3
• Molecular Formula: C23H22ClN5O
• Molecular Weight: 419.90668
• Product Categories: Inhibitors
• Mol File: 405168-58-3.mol
• Article Data: 0

Chemical Properties

• Appearance: /
• Density: 1.46
• Solubility: insoluble in H2O; ≥10.5 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming
• CAS DataBase Reference: CHIR-124(CAS DataBase Reference)
• NIST Chemistry Reference: CHIR-124(405168-58-3)
• EPA Substance Registry System: CHIR-124(405168-58-3)

Safety Data

• Hazardous Substances Data: 405168-58-3(Hazardous Substances Data)

Usage

Description

CHIR-124, also known as a cell-permeable, quinolone-based inhibitor, is a potent and selective inhibitor of checkpoint kinase 1 (Chk1). It plays a crucial role in regulating the S and G2-M phase cell cycle checkpoints in response to DNA damage. With its high selectivity for Chk1 and its ability to inhibit the growth of p53-mutant solid tumor cells, CHIR-124 has emerged as a promising pharmaceutical candidate for various applications.

Uses

Used in Oncology:
CHIR-124 is used as an inhibitor of checkpoint kinase 1 (Chk1) for the inhibition of tumor cell growth. It demonstrates high selectivity for Chk1, with inhibitory values 2,000-fold higher against Chk2. CHIR-124 can effectively inhibit the growth of p53-mutant solid tumor cells both in vitro and in a xenograft model, leading to potentiated tumor apoptosis.
Used in Combination Therapy:
CHIR-124 is used in combination with topoisomerase I poisons or ionizing radiation to enhance the therapeutic effects against cancer. This synergistic approach can improve the efficacy of conventional treatments and overcome resistance in certain cases, making it a valuable tool in the fight against cancer.
Used in Drug Development:
CHIR-124 serves as a key component in the development of novel drug delivery systems and therapeutic strategies. Its potent inhibitory effects on Chk1 make it an attractive candidate for further research and development, with the potential to improve the delivery, bioavailability, and therapeutic outcomes of cancer treatments.

references

[1]. tse an, rendahl kg, sheikh t, et al. chir-124, a novel potent inhibitor of chk1, potentiates the cytotoxicity of topoisomerase i poisons in vitro and in vivo. clinical cancer research, 2007, 13(2): 591-602.[2]. tao yg, leteur c, yang cy, et al. radiosensitization by chir-124, a selective chk1 inhibitor effects of p53 and cell cycle checkpoints. cell cycle, 2007, 8(8): 1196-1205.