A potent and selective Syk inhibitor (IC50 = 4 nM); inhibits 92% of Syk activity

PRT060318 – 5 mg

Brand:
Cayman
CAS:
1194961-19-7
Storage:
-20
UN-No:
Non-Hazardous - /

PRT060318 is a potent and selective inhibitor of spleen tyrosine kinase (Syk; IC50 = 4 nM).{39127,39128} It is selective, inhibiting 92% of Syk activity, while other kinases retain >70% activity, at a concentration of 50 nM in a panel of 270 kinases.{39128} PRT060318 inhibits convulxin-induced aggregation of human platelet-rich plasma (IC50 = 2.5 μM) in vitro and prevents thrombosis in a transgenic mouse model of heparin-induced thrombocytopenia. It induces chronic lymphocytic leukemia (CLL) B cell apoptosis and inhibits the secretion of chemokines CCL3, CCL4, and CXCL13.{39219} PRT060318 also inhibits CLL B cell chemotaxis and pseudoemperipolesis.  

 

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Description

A potent and selective Syk inhibitor (IC50 = 4 nM); inhibits 92% of Syk activity, while other kinases retain >70% activity, at a concentration of 50 nM in a panel of 270 kinases; inhibits convulxin-induced aggregation of human platelet-rich plasma (IC50 = 2.5 μM); prevents thrombosis in a transgenic mouse model of heparin-induced thrombocytopenia; induces CLL B cell apoptosis and inhibits the secretion of chemokines CCL3, CCL4, and CXCL13; inhibits CLL B cell chemotaxis and pseudoemperipolesis,

Formal name: 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide

Synonyms:  P142-76|PRT318

Molecular weight: 340.4

CAS: 1194961-19-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Non-Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling||Research Area|Cardiovascular System|Blood|Thrombosis||Research Area|Cell Biology|Cell Signaling

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