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Chemical Structure : ASTX029
CAS No.: 2095719-92-7
Catalog No.: PC-72401Not For Human Use, Lab Use Only.
ASTX029 (ASTX-029) is a highly potent, selective dual-mechanism ERK inhibitor with IC50 of <3 nM for ERK1/2, inhibits both ERK catalytic activity and the phosphorylation of ERK by MEK.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $158 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | $428 | In stock | |
| 100 mg | Get quote |
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ASTX029 (ASTX-029) is a highly potent, selective dual-mechanism ERK inhibitor with IC50 of <3 nM for ERK1/2, inhibits both ERK catalytic activity and the phosphorylation of ERK by MEK.
ASTX029 displayed high selectivity against a broad panel of kinases, and only 5 of a further 460 kinases (MAP2K6, MAP2K6S207E/T211E, PRKCN, PRKD1 and MAPK15) with IC50 of <100 nM.
ASTX029 inhibited the phosphorylation of ERK substrate RSK in a dose-dependent manner in both A375 (BRAF V600E-mutant melanoma) and HCT116 (KRAS G13D-mutant colorectal) cells with IC50 of 3.3 and 4 nM, respectively.
ASTX029 decreased pERK levels with a maximum inhibition of 93% and 94% in A375 and HCT116 cells, ASTX029 treatment also inhibited phosphorylation of the ERK substrate, CRAF.
ASTX02 caused a dose-dependent cell-cycle arrest in the G1-phase with an increase in apoptotic markers such as cleaved PARP and Bim.
ASTX029 (75 mg/kg, oral) modulated pharmacodynamic markers of MAPK signaling in a Colo205 subcutaneous xenograft model.
ASTX029 inhibited the proliferation of human cancer cell lines harboring MAPK-activating mutations (BRAF, KRAS, or NRAS.) with IC50 of 1.8-380 nM (A375: 3.4 nM, HCT116: 28 nM).
ASTX029 demonstrated in vivo antitumor activity in a range of MAPK-activated xenograft models.
| M.Wt | 584.045 | |
| Formula | C29H31ClFN5O5 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
100 mM in DMSO |
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| Chemical Name/SMILES |
(2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1-oxo-2,3-dihydro-1H-isoindol-2-yl)-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide |
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1. Munck JM, et al. Mol Cancer Ther. 2021 Oct;20(10):1757-1768.
2. Heightman TD, et al. J Med Chem. 2021 Aug 26;64(16):12286-12303.
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