ASTX029

ASTX029 is an ERK inhibitor (IC50 = 2.7 nM for ERK2). It is selective for ERK over a panel of 465 kinases. ASTX029 reduces phosphorylation of p90 ribosomal S6 kinase (RSK) in mutant B-RAF-expressing A375 melanoma and mutant K-Ras-expressing HCT116 colorectal cancer cells with IC50 values of 3.3 and 4 nM, respectively. It inhibits proliferation in a panel of cancer cell lines, including melanoma, colorectal, and lung cancer cells. ASTX029 reduces tumor growth in A375, Calu-6, and COLO 205 mouse xenograft models.Formal Name: (alphaR)-6-[5-chloro-2-[(tetrahydro-2H-pyran-4-yl)amino]-4-pyrimidinyl]-N-[(1S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]-1,3-dihydro-alpha-methyl-1-oxo-2H-isoindole-2-acetamide. CAS Number: 2095719-92-7. Molecular Formula: C29H31ClFN5O5. Formula Weight: 584.0. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 15 mg/ml. lambdamax: 223, 253 nm. SMILES: O=C1C2=CC(C3=NC(NC4CCOCC4)=NC=C3Cl)=CC=C2CN1[C@H](C)C(N[C@@H](C5=CC(OC)=CC(F)=C5)CO)=O. InChi Code: 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. InChi Key: BVRGQPJKSKKGIH-PUAOIOHZSA-N.