For research use only. Not for therapeutic Use.
ASTX029 (Example 1) is a potent dual ERK1/2 inhibitor (IC50: 2.7 nM). ASTX029 has anti-cancer activity[1][2].
ASTX029 (96 h) inhibits the proliferation of human cancer cells with MAPK-activating mutations, with IC50 values of 1.8 to 380 nM[2].
ASTX029 (2 h) inhibits the phosphorylation of RSK in both A375 and HCT116 cells, with IC50 values of 3.3 and 4 nM respectively, and also reduces pERK level[2].
ASTX029 (10 and 100 nM, 0-72 h) induces cell-cycle to arrest in the G1-phase, and induces cell apoptosis in A375 and HCT116 cells[2].
ASTX029 (20-75 mg/kg, p.o.) inhibits tumor growth in Colo205 (BRAFV600E-mutant colorectal cancer) tumor-bearing mice[2].
ASTX029 (5 mg/kg, p.o., mice) shows AUC of 1600 ng h/mL, T1/2 of 2.9 h, F (%) of 42%[3].
| Catalog Number | I022566 |
| 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% |
| 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 | CC(C(=O)NC(CO)C1=CC(=CC(=C1)F)OC)N2CC3=C(C2=O)C=C(C=C3)C4=NC(=NC=C4Cl)NC5CCOCC5 |
| Reference | [1]. Michael Reader, et al. 6-pyrimidin-isoindole derivative as erk1/2 inhibitor. WO2018193410A1. [2]. Munck JM, et al. ASTX029, a Novel Dual-mechanism ERK Inhibitor, Modulates Both the Phosphorylation and Catalytic Activity of ERK. Mol Cancer Ther. 2021 Oct;20(10):1757-1768. |
