For research use only. Not for therapeutic Use.
BAY-1143572（Cat No.:I013702）is a potent and selective inhibitor of the enzyme CDK7 (cyclin-dependent kinase 7), which plays a crucial role in regulating the cell cycle and transcription. By inhibiting CDK7, BAY-1143572 disrupts the phosphorylation of RNA polymerase II and cell cycle progression, leading to reduced proliferation and increased apoptosis in cancer cells. This compound has shown promise in preclinical studies for treating various cancers, particularly those with high transcriptional activity, such as triple-negative breast cancer. BAY-1143572 is being investigated as a potential therapeutic agent in oncology, with a focus on combination therapies to enhance treatment efficacy.
| Catalog Number | I013702 |
| CAS Number | 1414943-88-6 |
| Molecular Formula | C₁₈H₁₈FN₅O₂S |
| Purity | ≥95% |
| Target | CDK |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | 4-(4-fluoro-2-methoxyphenyl)-N-[3-[(methylsulfonimidoyl)methyl]phenyl]-1,3,5-triazin-2-amine |
| InChI | InChI=1S/C18H18FN5O2S/c1-26-16-9-13(19)6-7-15(16)17-21-11-22-18(24-17)23-14-5-3-4-12(8-14)10-27(2,20)25/h3-9,11,20H,10H2,1-2H3,(H,21,22,23,24) |
| InChIKey | ACWKGTGIJRCOOM-UHFFFAOYSA-N |
| SMILES | COC1=C(C=CC(=C1)F)C2=NC(=NC=N2)NC3=CC=CC(=C3)CS(=N)(=O)C |
| Reference | [1]. Scholz A, et al. BAY 1143572, a first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, shows convincing anti-tumor activity in preclinical models of acute myeloid leukemia (AML). [abstract]. In: Proceedings of the 107th Annual Meeting of the American Association for Cancer Research; 2016 Apr 16-20; New Orleans, LA. Philadelphia (PA): AACR; Cancer Res 2016;76(14 Suppl):Abstract nr 3022.<br>[2]. Scholz A, et al. BAY 1143572: A first-in-class, highly selective, potent and orally available inhibitor of PTEFb/CDK9 currently in Phase I, inhibits MYC and shows convincing anti-tumor activity in multiple xenograft models by the induction of apoptosis. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr DDT02-02. doi:10.1158/1538-7445.AM2015-DDT02-02 |
