CHIR-124 | B3069

CHIR-124 is a quinolone-based inhibitor of Checkpoint kinase-1 (Chk1). It potently and selectively inhibits Chk1 in vitro with an IC₅₀ of 0.3 nM. It interacts synergistically with topoisomerase poisons (e.g., camptothecin) in inhibiting the growth of several p53-mutant solid tumor cell lines. CHIR-124 potentiates the growth inhibitory effects of irinotecan by abrogating the G2-M checkpoint and increasing tumor apoptosis in a breast cancer xenograft model.

CHIR-124 is a quinolone-based inhibitor of Checkpoint kinase-1 (Chk1). It potently and selectively inhibits Chk1 in vitro with an IC₅₀ of 0.3 nM. It interacts synergistically with topoisomerase poisons (e.g., camptothecin) in inhibiting the growth of several p53-mutant solid tumor cell lines. CHIR-124 potentiates the growth inhibitory effects of irinotecan by abrogating the G2-M checkpoint and increasing tumor apoptosis in a breast cancer xenograft model.

B3069 | CHIR-124 DataSheet

Alternate Name/Synonyms: 4-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-6-chloro-1H-quinolin-2-one; (S)-3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4-(quinuclidin-3-ylamino)quinolin-2(1H)-one

Appearance: Brown Solid

Formulation:

CAS Number: 405168-58-3

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₂₃H₂₂ClN₅O

Molecular Weight: 419.91

Cell-Permeable?: TRUE

Purity: ≥98%

Solubilities: ~10 mg/ml in DMSO; ~3 mg/ml in DMF

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: An inhibitor of Checkpoint kinase-1

MDL Number: MFCD31656992

PubChem CID: 135399748

SMILES: C1CN2CCC1C(C2)NC3=C(C(=O)NC4=C3C=C(C=C4)Cl)C5=NC6=CC=CC=C6N5

InChi: InChI=1S/C23H22ClN5O/c24-14-5-6-16-15(11-14)21(25-19-12-29-9-7-13(19)8-10-29)20(23(30)28-16)22-26-17-3-1-2-4-18(17)27-22/h1-6,11,13,19H,7-10,12H2,(H,26,27)(H2,25,28,30)/t19-/m1/s1

InChi Key: MOVBBVMDHIRCTG-LJQANCHMSA-N