For research use only. Not for therapeutic Use.
PF-4136309（Cat No.:I001304）is a selective and potent inhibitor of the dual-specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A), which is implicated in various neurological disorders and cancer. By inhibiting DYRK1A, PF-4136309 has potential applications in treating conditions such as Down syndrome, Alzheimer’s disease, and other neurodegenerative diseases, as it may enhance neurogenesis and synaptic function. Additionally, its effects on cell cycle regulation suggest possible roles in cancer therapy. Ongoing research aims to elucidate its pharmacokinetics, safety, and efficacy in preclinical and clinical studies, positioning it as a promising candidate in drug development.
| Catalog Number | I001304 |
| CAS Number | 1341224-83-6 |
| Synonyms | N-(2-(3-((4-hydroxy-4-(5-(pyrimidin-2-yl)pyridin-2-yl)cyclohexyl)amino)pyrrolidin-1-yl)-2-oxoethyl)-3-(trifluoromethyl)benzamide |
| Molecular Formula | C29H31F3N6O3 |
| Purity | ≥95% |
| Target | Immunology/Inflammation |
| Solubility | DMSO: ≥ 32 mg/mL |
| Storage | -20°C |
| IUPAC Name | N-[2-[(3S)-3-[[4-hydroxy-4-(5-pyrimidin-2-ylpyridin-2-yl)cyclohexyl]amino]pyrrolidin-1-yl]-2-oxoethyl]-3-(trifluoromethyl)benzamide |
| InChI | InChI=1S/C29H31F3N6O3/c30-29(31,32)21-4-1-3-19(15-21)27(40)36-17-25(39)38-14-9-23(18-38)37-22-7-10-28(41,11-8-22)24-6-5-20(16-35-24)26-33-12-2-13-34-26/h1-6,12-13,15-16,22-23,37,41H,7-11,14,17-18H2,(H,36,40)/t22?,23-,28?/m0/s1 |
| InChIKey | ZNSVOHSYDRPBGI-CBQRAPNFSA-N |
| SMILES | C1CN(C[C@H]1NC2CCC(CC2)(C3=NC=C(C=C3)C4=NC=CC=N4)O)C(=O)CNC(=O)C5=CC(=CC=C5)C(F)(F)F |
| Reference | 1:ACS Med Chem Lett. 2011 Oct 5;2(12):913-8. doi: 10.1021/ml200199c. eCollection 2011 Dec 8. Discovery of INCB8761/PF-4136309, a Potent, Selective, and Orally Bioavailable CCR2 Antagonist.Xue CB,Wang A,Han Q,Zhang Y,Cao G,Feng H,Huang T,Zheng C,Xia M,Zhang K,Kong L,Glenn J,Anand R,Meloni D,Robinson DJ,Shao L,Storace L,Li M,Hughes RO,Devraj R,Morton PA,Rogier DJ,Covington M,Scherle P,Diamond S,Emm T,Yeleswaram S,Contel N,Vaddi K,Newton R,Hollis G,Metcalf B, PMID: 24900280 PMCID: PMC4018168 DOI: 10.1021/ml200199c </br><span>Abstract:</span> We report the discovery of a new (S)-3-aminopyrrolidine series of CCR2 antagonists. Structure-activity relationship studies on this new series led to the identification of 17 (INCB8761/PF-4136309) that exhibited potent CCR2 antagonistic activity, high selectivity, weak hERG activity, and an excellent in vitro and in vivo ADMET profile. INCB8761/PF-4136309 has entered human clinical trials. |
