For research use only. Not for therapeutic Use.
R547（Cat No.:I004755）is a selective inhibitor of the protein kinase CDK7, which plays a crucial role in regulating transcription and cell cycle progression. By inhibiting CDK7, R547 disrupts the phosphorylation of RNA polymerase II and key cell cycle proteins, leading to reduced cell proliferation and induction of apoptosis in cancer cells. It has shown promise in preclinical studies, particularly against various tumor types, including breast and lung cancers. R547’s specificity for CDK7 may provide a targeted therapeutic approach, minimizing effects on normal cells while effectively combating malignancies.
| Catalog Number | I004755 |
| CAS Number | 741713-40-6 |
| Synonyms | [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone |
| Molecular Formula | C18H21F2N5O4S |
| Purity | ≥95% |
| Target | Cyclin-Dependent Kinases |
| Solubility | DMSO 60 mg/mL; Water <1 mg/mL |
| Storage | Store at -20°C |
| IC50 | 2 nM(Ki for CDK1); 3 nM(Ki for CDK2); 1 nM(Ki for CDK4) |
| IUPAC Name | [4-amino-2-[(1-methylsulfonylpiperidin-4-yl)amino]pyrimidin-5-yl]-(2,3-difluoro-6-methoxyphenyl)methanone |
| InChI | InChI=1S/C18H21F2N5O4S/c1-29-13-4-3-12(19)15(20)14(13)16(26)11-9-22-18(24-17(11)21)23-10-5-7-25(8-6-10)30(2,27)28/h3-4,9-10H,5-8H2,1-2H3,(H3,21,22,23,24) |
| InChIKey | JRNJNYBQQYBCLE-UHFFFAOYSA-N |
| SMILES | COC1=C(C(=C(C=C1)F)F)C(=O)C2=CN=C(N=C2N)NC3CCN(CC3)S(=O)(=O)C |
| Reference | </br>1:In vitro and in vivo activity of R547: a potent and selective cyclin-dependent kinase inhibitor currently in phase I clinical trials. DePinto W, Chu XJ, Yin X, Smith M, Packman K, Goelzer P, Lovey A, Chen Y, Qian H, Hamid R, Xiang Q, Tovar C, Blain R, Nevins T, Higgins B, Luistro L, Kolinsky K, Felix B, Hussain S, Heimbrook D.Mol Cancer Ther. 2006 Nov;5(11):2644-58. PMID: 17121911 Free Article</br>2:Discovery of [4-Amino-2-(1-methanesulfonylpiperidin-4-ylamino)pyrimidin-5-yl](2,3-difluoro-6- methoxyphenyl)methanone (R547), a potent and selective cyclin-dependent kinase inhibitor with significant in vivo antitumor activity. Chu XJ, DePinto W, Bartkovitz D, So SS, Vu BT, Packman K, Lukacs C, Ding Q, Jiang N, Wang K, Goelzer P, Yin X, Smith MA, Higgins BX, Chen Y, Xiang Q, Moliterni J, Kaplan G, Graves B, Lovey A, Fotouhi N.J Med Chem. 2006 Nov 2;49(22):6549-60. PMID: 17064073 |
