2488761-18-6
Chemical Structure
TMX-3013
- CAS No.: 2488761-18-6
- Formula:C17H14BrFN6O3S
- Molecular Weight:481.30
IUPAC Name: 2-((5-bromo-2-((2-methyl-4-sulfamoylphenyl)amino)pyrimidin-4-yl)amino)-6-fluorobenzamide
InChIKey: VCPYDRGRPKSEOJ-UHFFFAOYSA-N
SMILES: NC(C1=C(C=CC=C1NC2=NC(NC3=CC=C(C=C3)S(N)(=O)=O)=NC=C2Br)F)=O
Biological Activity: TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs)[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
TMX-3013 | 98.02% | TMX-3013 is a CDK inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be used as a target protein ligand, conjugated with the PROTAC linker and the CRBN ligand Thalidomide (HY-14658) for the synthesis of PROTAC TMX-2138 (HY-164906). TMX-3013 can also act as an effector ligand, binding to target proteins HaloTag or FKBP, and can be used in the synthesis of regulated induced proximity targeting chimeras (RIPTACs). | ||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Raina K, et al. Regulated induced proximity targeting chimeras-RIPTACs-A heterobifunctional small molecule strategy for cancer selective therapies. Cell Chem Biol. 2024;31(8):1490-1502.e42. [Content Brief]
- [2]. Teng M, et al. Exploring Ligand-Directed N-Acyl-N-alkylsulfonamide-Based Acylation Chemistry for Potential Targeted Degrader Development. ACS Med Chem Lett. 2021 Jul 21;12(8):1302-1307. [Content Brief]
- [3]. Teng M, et al. Development of CDK2 and CDK5 Dual Degrader TMX-2172. Angew Chem Int Ed Engl. 2020;59(33):13865-13870. [Content Brief]
Keywords
