TCS ERK 11e (TCS Extracellular Signal-Related Kinase 11e, VX-11e, 4-[2-[(2-chloro-4-fluorophenyl)amino]-5-methyl-4-pyrimidinyl]-N-[(1S)-1-(3-chlorophenyl)-2-hydroxyethyl]-1H-pyrrole-2-carboxamide)

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£550.00

SKU:: 217345
Molekulargewicht:: 500.4
Lagerbedingungen:: 4°C
Hersteller:: United States Biological
CAS Number:: 896720-20-0
Weitere Details:: A cell-permeable pyrimidylpyrrole compound that acts as an active site-targeting, highly potent and selective ERK1/2 inhibitor (KI <2nM against Erk2; [ATP] = 65uM), while inhibiting GSK-3, Aurora A, Cdk2 only at much higher concentrations (KI = 395, 540, and 852nM, respectively) and exhibiting much reduced or little potency toward a panel of more than 130 other kinases (KI ≥1.4uM; IC50 ≥1uM). Shown to effectively inhibit human colon carcinoma HT-29 proliferation (IC50 = 48nM) and restore EGFR inhibitor WZ4002 antiproliferation activity in WZR10 cultures (84% and no inhibition, respectively, by 100nM WZ4002 with or without 1uM Erk Inhibitor VIII co-treatment). Orally available in both mice and rats in vivo. Synonyms: VX-11e, (S)-4-(2-(2-Chloro-4-fluorophenylamino)-5-methylpyrimidin-4-yl)-N-(1-(3-chlorophenyl)-2-hydroxyethyl)-1H-pyrrole-2-carboxamide CAS No: 896720-20-0 Molecular Weight: 500.4 Molecular Formula: C₂₄H₂₀Cl₂FN₅O₂ Solubility: DMSO, DMF, Ethanol Purity: ≥98% Storage and Stability: Store at 4°C°C under inert atmosphere. For maximum recovery of product, centrifuge the original vial prior to removing the cap.