CHIR-124 , 99% , 405168-58-3

CAS NO.：405168-58-3

Empirical Formula: C23H22ClN5O

Molecular Weight: 419.91

MDL number: MFCD14636453

PRODUCT Properties

• Density: 1.46
• storage temp.: Store at -20°C
• solubility: insoluble in H2O; ≥10.5 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming
• form: solid
• pka: 9.00±0.70(Predicted)
• color: Light yellow to brown
• InChIKey: MOVBBVMDHIRCTG-LJQANCHMSA-N
• SMILES: N1C2=C(C=C(Cl)C=C2)C(N[C@H]2C3CCN(CC3)C2)=C(C2NC3=CC=CC=C3N=2)C1=O

Description and Uses

Checkpoint kinase 1 (Chk1) regulates S and G₂-M phase cell cycle checkpoints in response to DNA damage. CHIR124 is a cell-permeable, quinolone-based inhibitor of Chk1 (IC₅₀ = 0.3 nM in vitro). It demonstrates high selectivity for Chk1 by displaying inhibitory values 2,000-fold higher against Chk2 (IC₅₀ = 0.7 μM). In synergy with topoisomerase I poisons or ionizing radiation, CHIR124 can inhibit the growth of p53-mutant solid tumor cells both in vitro and in a xenograft model, potentiating tumor apoptosis.

CHIR 124 is a cell-permeable molecule with a quinolone-based structure. It inhibits checkpoint kinase 1 (Chk1) which regulates S and G2-M cekk cycle checkpoints in response to DNA damage. Application towards inhibition of tumor cell growth.

Safety

• Symbol(GHS): GHS07
• Signal word: Warning
• Hazard statements: H302
• Precautionary statements: P280-P305+P351+P338