SML2505
PRT-060318
≥95% (HPLC)
Synonym(s):
2-((1R,2S)-2-Aminocyclohexylamino)-4-(m-tolylamino)pyrimidine-5-carboxamide, 2-[[(1R,2S)-2-Aminocyclohexyl]amino]-4-[(3-methylphenyl)amino]-5-pyrimidinecarboxamide, P142-76, PRT060318, PRT318
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About This Item
Empirical Formula (Hill Notation):
C18H24N6O
CAS Number:
Molecular Weight:
340.42
UNSPSC Code:
12352200
MDL number:
NACRES:
NA.21
InChI key
NZNTWOVDIXCHHS-LSDHHAIUSA-N
SMILES string
N[C@H]1CCCC[C@H]1NC2=NC(NC3=CC=CC(C)=C3)=C(C=N2)C(N)=O
assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Related Categories
Biochem/physiol Actions
Orally active, highly potent and selective Syk inhibitor with in vivo efficacy in animal models of thrombosis and B-cell acute lymphoblastic leukemia (B-ALL).
PRT-060318 (PRT318; P142-76) is a highly potent and selective Syk inhibitor (IC50 = 4 nM; much reduced potency against 138 other kinases) that blocks BCR-dependent signaling in chronic lymphocytic leukemia (CCL) cultures (2-3 μM) and specifically inhibits platelets activation via ITAM receptor complex GPVI/FcRγ, but not P2Y1/12 or PAR1, stimulation (IC50 = 2.5 μM; aggregation by 8 ng/mL convulxin). PRT318 demonstrates in vivo efficacy in animal models of thrombosis (30 mg/kg mouse bis p.o.; 5.1675 mg/3.1 mL/kg/rabbit/15 min then 7.33 mg/4.4 mL/kg/h i.v.; 8.90 mg/mL/kg pig/h i.v.) and B-cell acute lymphoblastic leukemia (30 mg /kg bis p.o.; human B-ALL xenograft mice).
signalword
Danger
hcodes
Hazard Classifications
Self-react. C
Storage Class
5.2 - Organic peroxides and self-reacting hazardous materials
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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Patrick Andre et al.
Blood, 118(18), 5000-5010 (2011-09-02)
Although current antiplatelet therapies provide potent antithrombotic effects, their efficacy is limited by a heightened risk of bleeding and failure to affect vascular remodeling after injury. New lines of research suggest that thrombosis and hemorrhage may be uncoupled at the
Michael P Reilly et al.
Blood, 117(7), 2241-2246 (2010-11-23)
Heparin-induced thrombocytopenia (HIT) is a major cause of morbidity and mortality resulting from the associated thrombosis. Extensive studies using our transgenic mouse model of HIT have shown that antibodies reactive with heparin-platelet factor 4 complexes lead to FcγRIIA-mediated platelet activation
J Hoellenriegel et al.
Leukemia, 26(7), 1576-1583 (2012-03-01)
Syk is a protein tyrosine kinase that couples B-cell receptor (BCR) activation with downstream signaling pathways, affecting cell survival and proliferation. Moreover, Syk is involved in BCR-independent functions, such as B-cell migration and adhesion. In chronic lymphocytic leukemia (CLL), Syk
Callum N Watson et al.
Platelets, 27(6), 535-540 (2016-03-31)
Gram-negative Escherichia coli cause diseases such as sepsis and hemolytic uremic syndrome in which thrombotic disorders can be found. Direct platelet-bacterium interactions might contribute to some of these conditions; however, mechanisms of human platelet activation by E. coli leading to
Rachit Badolia et al.
International journal of molecular sciences, 18(6) (2017-06-10)
The binding of von Willebrand factor (VWF) to the platelet membrane glycoprotein 1b-IX (GP1b-IX) leads to activation of platelets. GP1b was shown to signal via the FcRγ-ITAM (Fc Receptor γ-Immunoreceptor tyrosine-based activation motif) pathway, activating spleen tyrosine kinase (Syk) and
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