CHIR-124

SKU: orb1225103

Description

CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM, 2,000-fold selectivity over Chk2; displays 500- to 5,000-fold less active against other cell cycle kinases, such as CDK2/cyclin A , Cdc2/cyclin B, and CDK4/cyclin D; also potently inhibits PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM; interacts synergistically with topoisomerase poisons (e.g., camptothecin or SN-38) in causing growth inhibition in several p53-mutant solid tumor cell lines, abrogates the SN-38-induced S and G2-M checkpoints and potentiates apoptosis in MDA-MD-435 breast cancer cells, also restores the level of cdc25A protein; potentiates the growth inhibitory effects of irinotecan in breast cancer xenograft models.

Key Properties

• CAS Number: 405168-58-3
• MW: 419.91
• Purity: >98% (HPLC)
• Formula: C₂₃H₂₂ClN₅O
• SMILES: O=C1NC2=C(C=C(Cl)C=C2)C(N[C@@H]3C[N@]4CC[C@]3([H])CC4)=C1C5=NC6=CC=CC=C6N5
• Target: Chk
• Solubility: DMSO: 14 mg/mL

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CHIR124 | CHIR 124

Quick Database Links

Gene Symbol

Chk