Welcome to ProbeChem!Global Supplier of Chemical Probes, Inhibitors & Agonists.
Chemical Structure : CHIR-124
CAS No.: 405168-58-3
Catalog No.: PC-43443Not For Human Use, Lab Use Only.
CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM, 2,000-fold selectivity over Chk2.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $128 | In stock | |
| 25 mg | $198 | In stock | |
| 50 mg | $328 | In stock | |
| 100 mg | Get quote |
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
CHIR-124 is a potent, selective Chk1 inhibitor with in vitro IC50 of 0.3 nM, 2,000-fold selectivity over Chk2.
CHIR-124 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.
CHIR-124 also potently inhibits PDGFR and FLT3 with IC50s of 6.6 nM and 5.8 nM.
CHIR-124 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.
CHIR-124 potentiates the growth inhibitory effects of irinotecan in breast cancer xenograft models.
| M.Wt | 419.91 | |
| Formula | C23H22ClN5O | |
| Appearance | Solid | |
| Storage |
|
|
| Solubility |
DMSO: 14 mg/mL |
|
| Chemical Name/SMILES |
2(1H)-Quinolinone, 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylamino]-3-(1H-benzimidazol-2-yl)-6-chloro- |
|
1. Tse AN, et al. Clin Cancer Res. 2007 Jan 15;13(2 Pt 1):591-602.
2. Tao Y, et al. Cell Cycle. 2009 Apr 15;8(8):1196-205.
3. Lee JH, et al. Proc Natl Acad Sci U S A. 2011 Dec 6;108(49):19629-34.
4. Seiler JA, et al. Mol Cell Biol. 2007 Aug;27(16):5806-18.
Copyright © 2022 probechem.com. All Rights Reserved. probechem Copyright
