AG-012986
AG-012986 is a multitargeted cyclin-dependent kinase (CDK) inhibitor active against CDK1, CDK2, CDK4/6, CDK5, and CDK9, with selectivity over a diverse panel of non-CDK kinases. AG-012986 showed antiproliferative activities in vitro with IC(50)s of <100 nmol/L in 14 of 18 tumor cell lines. In vivo, significant antitumor efficacy induced by AG-012986 was seen (tumor growth inhibition, >83.1%) in 10 of 11 human xenograft tumor models. AG-012986 also showed dose-dependent retinoblastoma Ser(795) hypophosphorylation, cell cycle arrest, decreased Ki-67 tumor staining, and apoptosis in conjunction with antitumor activity. (
1: Lee DU, Jessen B. 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. doi: 10.1002/jbt.20415. Epub 2011 Nov 16. PubMed PMID: 22095879.
2: Zhang C, Lundgren K, Yan Z, Arango ME, Price S, Huber A, Higgins J, Troche G, Skaptason J, Koudriakova T, Nonomiya J, Yang M, O'Connor P, Bender S, Los G, Lewis C, Jessen B. Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy. Mol Cancer Ther. 2008 Apr;7(4):818-28. doi: 10.1158/1535-7163.MCT-07-0440. PubMed PMID: 18413795.
3: Jessen BA, Lee L, Koudriakova T, Haines M, Lundgren K, Price S, Nonomiya J, Lewis C, Stevens GJ. Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors. J Appl Toxicol. 2007 Mar-Apr;27(2):133-42. PubMed PMID: 17211896.
4: Illanes O, Anderson S, Niesman M, Zwick L, Jessen BA. Retinal and peripheral nerve toxicity induced by the administration of a pan-cyclin dependent kinase (cdk) inhibitor in mice. Toxicol Pathol. 2006;34(3):243-8. PubMed PMID: 16698721.
2: Zhang C, Lundgren K, Yan Z, Arango ME, Price S, Huber A, Higgins J, Troche G, Skaptason J, Koudriakova T, Nonomiya J, Yang M, O'Connor P, Bender S, Los G, Lewis C, Jessen B. Pharmacologic properties of AG-012986, a pan-cyclin-dependent kinase inhibitor with antitumor efficacy. Mol Cancer Ther. 2008 Apr;7(4):818-28. doi: 10.1158/1535-7163.MCT-07-0440. PubMed PMID: 18413795.
3: Jessen BA, Lee L, Koudriakova T, Haines M, Lundgren K, Price S, Nonomiya J, Lewis C, Stevens GJ. Peripheral white blood cell toxicity induced by broad spectrum cyclin-dependent kinase inhibitors. J Appl Toxicol. 2007 Mar-Apr;27(2):133-42. PubMed PMID: 17211896.
4: Illanes O, Anderson S, Niesman M, Zwick L, Jessen BA. Retinal and peripheral nerve toxicity induced by the administration of a pan-cyclin dependent kinase (cdk) inhibitor in mice. Toxicol Pathol. 2006;34(3):243-8. PubMed PMID: 16698721.
| Chemical | |
|---|---|
| CAS Num | 486414-35-1 |
| Chemical Formula | C22H23F2N5O2S |
| Molecular Weight | 459.51 |
| IUPAC Chemical Name | 4-[[4-Amino-5-(2,6-difluorobenzoyl)thiazol-2-yl]amino]-N-((R)-2-dimethylamino-1-methylethyl)benzamide |
| Exact Mass | 459.15405 |
| Elemental Analysis | C, 57.50; H, 5.05; F, 8.27; N, 15.24; O, 6.96; S, 6.98 |
| Synonym | AG012986; AG 012986; AG-012986. |
| Solubility | Soluble in DMSO, not in water |
| SMILES Code | O=C(N[C@H](C)CN(C)C)C1=CC=C(NC2=NC(N)=C(C(C3=C(F)C=CC=C3F)=O)S2)C=C1 |
| Biological | |
| Targets and Effects | cyclin-dependent kinase (CDK) inhibitor |
| Pathways | Apoptosis |
| Physical | |
| Appearance | Solid powder |
| Purity | >98% (or refer to the Certificate of Analysis) |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| Storage Condition | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Shelf Life | >5 years if stored properly |
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