486414-32-8
Chemical Structure
AG-012986 dihydrochloride
- CAS No.: 486414-32-8
- Formula:C22H25Cl2F2N5O2S
- Molecular Weight:532.43
InChIKey: MCUINVYSCWLFGD-CURYUGHLSA-N
SMILES: O=C(C1=C(C=CC=C1F)F)C2=C(N)N=C(NC3=CC=C(C=C3)C(N[C@H](C)CN(C)C)=O)S2.Cl.Cl
Biological Activity:
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AG-012986 dihydrochloride | AG-012986 (dihydrochloride) is a pan-CDK inhibitor with Ki values of 44 nM (CDK1), 9.2 nM (CDK4), 94 nM (CDK2), and IC50 values of 22 nM (CDK5), 4 nM (CDK9). AG-012986 (dihydrochloride) causes apoptosis of T-cells by targeting upstream kinases in the p38 Mitogen-activated protein kinase (MAPK) pathway and impairing cellular survival. AG-012986 (dihydrochloride) induces cell cycle arrest, retinoblastoma protein hypophosphorylation, and reduces Ki-67 expression. AG-012986 (dihydrochloride) exerts antiproliferative activity in tumor cells, demonstrates antitumor efficacy in human xenograft models, and causes retinal and peripheral neurotoxicity, plus immune cell toxicity. AG-012986 (dihydrochloride) can be used for the research of colon carcinoma, non-small cell lung carcinoma, lung carcinoma, breast carcinoma, ovarian tumor, pancreatic carcinoma, osteosarcoma, lymphoma, leukemia, retinotoxicity. |
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References
- [1]. Zhang C, et al. Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy. Mol Cancer Ther. 2008 Apr;7(4):818-28. [Content Brief]
- [2]. Wright P, et al. Differential expression of cyclin-dependent kinases in the adult human retina in relation to CDK inhibitor retinotoxicity. Arch Toxicol. 2019;93(3):659-671. [Content Brief]
- [3]. Lee DU, et al. Off-target immune cell toxicity caused by AG-012986, a pan-CDK inhibitor, is associated with inhibition of p38 MAPK phosphorylation. J Biochem Mol Toxicol. 2012 Mar;26(3):101-8. [Content Brief]
