UNC2250 is a potent and selective Mer Kinase inhibitor. When applied to live cells, UNC2250 inhibited steady-state phosphorylation of endogenous Mer with an IC50 of 9.8 nM and blocked ligand-stimulated activation of a chimeric EGFR-Mer protein. Treatment with UNC2250 also resulted in decreased colony-forming potential in rhabdoid and NSCLC tumor cells, thereby demonstrating functional antitumor activity. The results provide a rationale for further investigation of UNC2250 for therapeutic application in patients with cancer.

MedKoo Cat#: 406396 Name: UNC2250 CAS#: 1493694-70-4 Chemical Formula: C24H36N6O2 Exact Mass: 440.28997 Molecular Weight: 440.58 Elemental Analysis: C, 65.43; H, 8.24; N, 19.07; O, 7.26

Synonym: UNC2250, UNC-2250, UNC 2250

IUPAC/Chemical Name: (1r,4r)-4-((2-(butylamino)-5-(5-(morpholinomethyl)pyridin-2-yl)pyrimidin-4-yl)amino)cyclohexanol

InChi Key: HSYSSKFCQHXOBP-MXVIHJGJSA-N

InChi Code: InChI=1S/C24H36N6O2/c1-2-3-10-25-24-27-16-21(23(29-24)28-19-5-7-20(31)8-6-19)22-9-4-18(15-26-22)17-30-11-13-32-14-12-30/h4,9,15-16,19-20,31H,2-3,5-8,10-14,17H2,1H3,(H2,25,27,28,29)/t19-,20-

SMILES Code: O[C@H]1CC[C@H](NC2=NC(NCCCC)=NC=C2C3=NC=C(CN4CCOCC4)C=C3)CC1

Technical Data

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Certificate of Analysis: View CoA: current batch, Lot#BBC60304

QC Data: View QC data: current batch, Lot#BBC60304

Safety Data Sheet (MSDS): View Material Safety Data Sheet (MSDS)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code: 293490

References

1: Zhang W, Zhang D, Stashko MA, Deryckere D, Hunter D, Kireev D, Miley MJ, Cummings C, Lee M, Norris-Drouin J, Stewart WM, Sather S, Zhou Y, Kirkpatrick G,  Machius M, Janzen WP, Earp HS, Graham DK, Frye SV, Wang X. Pseudo-Cyclization through Intramolecular Hydrogen Bond Enables Discovery of Pyridine Substituted Pyrimidines as New Mer Kinase Inhibitors. J Med Chem. 2013 Nov 20. 56(23): 9683–9692. PubMed PMID: 24195762.