PRT-060318 (PRT318, P142–76)
$100.00 – $1,000.00
PRT-060318 (PRT318, P142–76) (CAS No.: 1194961-19-7), a potent and selective inhibitor of spleen tyrosine kinase (Syk; IC50 = 4 nM). 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. >98% Purity.
Synonyms: PRT060318, PRT318, P142–76, PRT-318, Syk inhibitor, spleen tyrosine kinase inhibitor
For Research Use Only.
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Description
APIM050415: PRT-060318 (PRT318, P142–76) is a potent and selective inhibitor of spleen tyrosine kinase (Syk; IC50 = 4 nM). 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.
CAS No.: 1194961-19-7
IUPAC/Chemical Name: 2-(((1R,2S)-2-aminocyclohexyl)amino)-4-(m-tolylamino)pyrimidine-5-carboxamide
Molecular Formula: C18H24N6O
Molecular Weight: 340.42
Purity: >98% Purity
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report
Solubility: Soluble in DMSO
Storage: Dry, dark and at 0 – 4 C for short term (days to weeks) or -20 C for long term (months to years).
Note: Please contact us for COA, Spectra, and SDS information.
Background Information:
PRT-060318 (PRT318, P142–76) (CAS No. 1194961-19-7) is a potent and selective inhibitor of spleen tyrosine kinase (Syk; IC50 = 4 nM).1,2 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. PRT-060318 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. PRT-060318 also inhibits CLL B cell chemotaxis and pseudoemperipolesis.
Target: Syk
IC50: 4 nM
In Vitro: PRT-060318 (PRT318) is a potent inhibitor of purified Syk kinase with an IC50 of 4 nM. Syk kinase is inhibited by 92%, whereas all other kinases retains more than 70% at a concentration of 50 nM of PRT-060318 (PRT318). PRT-060318 and P505-15 effectively antagonize CLL cell survival after B-cell receptor (BCR) triggering and in nurse-like cell-co-cultures. They inhibit BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT318 and P505-15 inhibit Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering. [1]
In Vivo: PRT-060318 (PRT318) completely inhibits HIT immune complex-induced aggregation of both human and transgenic HIT mouse platelets. Pretreatment of mice with PRT-060318 markedly reduces HIT IC-induced thrombosis in the lungs. The Thrombosis Score is significantly lower for PRT318-treated mice compared with control. [2]
What is the solubility of PRT-060318 (PRT318) in vitro?
H2O: > 5.6 mg/mL
Reference:
[1]. Hoellenriegel, J. et al. “Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration”, Leukemia, 2012, 26, 1576-1583
[2]. Reilly, M. P. et al. “PRT-060318, a novel Syk inhibitor, prevents heparin-induced thrombocytopenia and thrombosis in a transgenic mouse model”, Blood, 2011, 117, 2241-2246.
[3]. Pollitt, A. Y. et al. “Syk and Src Family Kinases Regulate C-type Lectin Receptor 2 (CLEC-2)-mediated Clustering of Podoplanin and Platelet Adhesion to Lymphatic Endothelial Cells”, J. Biol. Chem., 2014, 289, 35695–35710.
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Additional information
| Size | 10 mg, 100 mg, 5 mg, 50 mg |
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