An orally bioavailable pyrazolopyrimidine compound that acts as a potent, reversible and ATP-competitive inhibitor of Mer receptor tyrosine kinase (IC50=2.9nM, Ki=4.3nM) with ~10-fold greater selectivity over other TAM family kinases (IC50=37 and 48nM for Axl and Tyro3, respectively). Also shown to affect the activities of Flt3, MAPKAPK2, RET and Ret-Y791F at 30nM by 82%, 92%, 59% and 56% in a 72 kinase panel, and block Mer auto-phosphorylation in human Pre-B leukemia 697 cells with an IC50 of 141nM. Exhibits desirable pharmacokinetic profile and efficacy in mice. Synonyms: 1-((trans-4-Aminocyclohexyl)methyl)-N-butyl-3-(4-fluorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-6-amine, MERTK Inhibitor I, RP38 Inhibitor I, TAM Family RTK Inhibitor I CAS No: 1350547-65-7 Molecular Formula: C22H29FN6 Molecular Weight: 396.5 Purity: 98% (LCMS) Appearance: White to yellow solid Solubility: DMSO (10%): 2.5mg/ml Method for Determining Identity: 1H NMR Spectrum and Liquid Chromatograpty Mass Spectrometry Analysis Storage and Stability: Lyophilized powder may be stored at -20C. Stable for 6 months after receipt at -20C. Reconstitute with sterile DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20C. For maximum recovery of product, centrifuge the original vial after thawing and prior to removing the cap. Further dilutions can be made in assay buffer.
Molecular Weight:
396.5
CAS Number:
[1350547-65-7]
* VAT and and shipping costs not included. Errors and price changes excepted
