Mer RTK Inhibitor, UNC569

Blue Ice

396, 5

Supplied as a beige powder.

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 -20°C. Stable for 6 months after receipt at -20°C. Reconstitute with sterile DMSO. Aliquot to avoid repeated freezing and thawing. Store at -20°C. 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.