CHIR-124_product_DataBase

Bioactivity

CHIR-124 is a potent and selective Chk1 inhibitor with IC50 of 0.3 nM, and also potently targets PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.

Invitro

CHIR-124 is 500- to 5,000-fold less active against other cell cycle kinases, such as cyclin-dependent kinase 2/cyclin A (0.19 μM), cdc2/cyclin B (0.51 μM), and cyclin-dependent kinase 4/cyclin D (2.1 μM). CHIR-124 (≥0.9 nM) in combination with SN-38 (≥0.42 nM) causes significant synergy or >10% deviation from additivity in human cancer cell lines expressing mutant p53, and these values overlap and fall below the IC50s for SN-38 (1.2×10-7 M) and CHIR-124 (2.2×10-7 M), respectively. Moreover, CHIR-124 (100 nM) abrogates the SN-38-induced S and G2-M phase cell cycle checkpoints. CHIR-124 (200 nM) leads to a 2.5-fold elevated level of cdc25A above that of the untreated HCT116 p53−/− cells. The down-regulation of cdc25A induced by SN-38 is completely restored by concurrent or sequential treatment with CHIR-124, proving that CHIR-124 inhibits the Chk1-mediated destruction of cdc25A in whole cells[1]. CHIR-124 occupies the ATP-binding site, inhibits Chk1 (IC50, 0.3 nM) 2,000-fold more potently than Chk2 (IC50, 0.7 μM)[2].

Name

CHIR-124

CAS

405168-58-3

Formula

C23H22ClN5O

Molar Mass

419.91

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

PeptideDB

CHIR-124

CAS: 405168-58-3 F: C23H22ClN5O W: 419.91