A selective inhibitor of Mer kinase activity

UNC2250 – 10 mg

Brand:
Cayman
CAS:
1493694-70-4
Storage:
-20
UN-No:
Non-Hazardous - /

Tyro3, Axl, and Mer are members of the TAM family of receptor tyrosine kinases that have signaling roles in normal and malignant cells.{30868} UNC2250 is an inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM.{30869} It is selective for Mer over a panel of both tyrosine and serine-threonine kinases, including Tyro3 and Axl. UNC2250 also inhibits ligand-dependent phosphorylation of a chimeric EGFR-Mer protein and blocks colony formation in soft agar cultures of BT-12 rhabdoid tumor and Colo699 NSCLC cell lines.{30869} UNC2250 displays good pharmacokinetic properties in mice following intravenous or oral administration.{30869}  

 

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Description

A selective inhibitor of Mer kinase activity, blocking the steady-state phosphorylation of endogenous Mer in 697 B-ALL cells with an IC50 value of 9.8 nM; inhibits Mer activity in cells and displays good pharmacokinetic properties in mice following intravenous or oral administration

Formal name: trans-4-[[2-(butylamino)-5-[5-(4-morpholinylmethyl)-2-pyridinyl]-4-pyrimidinyl]amino]-cyclohexanol

Synonyms: 

Molecular weight: 440.6

CAS: 1493694-70-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling

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