For research use only. Not for therapeutic Use.
ASTX029（Cat No.:I022566）is an oral, selective dual-mechanism inhibitor of extracellular signal-regulated kinases 1 and 2 (ERK1/2), key components of the MAPK signaling pathway often dysregulated in cancers with RAS or RAF mutations. Developed by Astex Pharmaceuticals, ASTX029 aims to block both ERK catalytic activity and its phosphorylation of downstream targets, effectively inhibiting tumor growth and survival. Preclinical models have shown potent anti-tumor activity, particularly in cancers resistant to upstream MEK inhibitors. Currently in clinical trials, ASTX029 holds promise as a targeted therapy for MAPK-driven malignancies such as melanoma and colorectal cancer.
| CAS Number | 2095719-92-7 |
| Synonyms | (2R)-2-[5-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]-3-oxo-1H-isoindol-2-yl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide |
| Molecular Formula | C29H31ClFN5O5 |
| Purity | ≥95% |
| IUPAC Name | (2R)-2-[5-[5-chloro-2-(oxan-4-ylamino)pyrimidin-4-yl]-3-oxo-1H-isoindol-2-yl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide |
| InChI | InChI=1S/C29H31ClFN5O5/c1-16(27(38)34-25(15-37)19-9-20(31)12-22(10-19)40-2)36-14-18-4-3-17(11-23(18)28(36)39)26-24(30)13-32-29(35-26)33-21-5-7-41-8-6-21/h3-4,9-13,16,21,25,37H,5-8,14-15H2,1-2H3,(H,34,38)(H,32,33,35)/t16-,25-/m1/s1 |
| InChIKey | BVRGQPJKSKKGIH-PUAOIOHZSA-N |
| SMILES | C[C@H](C(=O)N[C@H](CO)C1=CC(=CC(=C1)F)OC)N2CC3=C(C2=O)C=C(C=C3)C4=NC(=NC=C4Cl)NC5CCOCC5 |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
