A potent

CX-6258 – 1 mg

Brand:
Cayman
CAS:
1202916-90-2
Storage:
-20
UN-No:
Non-Hazardous - /

The family of Pim (Provirus Integration site for Moloney murine leukemia virus) proteins are serine/threonine kinases involved in cell survival and cell proliferation. CX-6258 is a potent, reversible inhibitor of Pim-1, -2, and -3 (IC50s = 5, 25, and 16 nM, respectively).{28838} It demonstrates excellent selectivity, inhibiting only FLT3 from a panel of 107 additional kinases. CX-6258 dose-dependently blocks the phosphorylation of the Pim targets Bad, 4E-BP1, and NKX3.1.{28838,28839} It acts synergistically with the chemotherapeutics doxorubicin and paclitaxel, presumably because CX-6258 impairs Pim-mediated enhanced expression of P-glycoprotein.{28838} CX-6258 is orally bioavailable and inhibits the growth of MV4-11 xenografts in mice.{28838}  

 

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Description

A potent, reversible, orally bioavailable inhibitor of Pim-1, -2, and -3 (IC50s = 5, 25, and 16 nM, respectively); dose-dependently blocks the phosphorylation of the Pim targets Bad, 4E-BP1, and NKX3.1; acts synergistically with chemotherapeutic drugs

Formal name: (3E)-5-chloro-3-[[5-[3-[(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)carbonyl]phenyl]-2-furanyl]methylene]-1,3-dihydro-2H-indol-2-one

Synonyms:  Pim-Kinase Inhibitor X

Molecular weight: 461.9

CAS: 1202916-90-2

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|PIMs||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|PIM Signaling

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