All Photos(1)
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
Empirical Formula (Hill Notation):
C18H24N6O
Recommended Products
Assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
SMILES string
N[C@H]1CCCC[C@H]1NC2=NC(NC3=CC=CC(C)=C3)=C(C=N2)C(N)=O
Biochem/physiol Actions
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).
Signal Word
Danger
Hazard Statements
Precautionary Statements
Hazard Classifications
Self-react. C
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
S Köhrer et al.
Leukemia, 30(6), 1246-1254 (2016-02-06)
Precursor-B-cell receptor (pre-BCR) signaling and spleen tyrosine kinase (SYK) recently were introduced as therapeutic targets for patients with B-cell acute lymphoblastic leukemia (B-ALL), but the importance of this pathway in B-ALL subsets and mechanism of downstream signaling have not fully
Marie-Blanche Onselaer et al.
Blood advances, 1(19), 1495-1504 (2018-01-04)
Fibrin has recently been shown to activate platelets through the immunoglobulin receptor glycoprotein VI (GPVI). In the present study, we show that spreading of human platelets on fibrin is abolished in patients deficient in GPVI, confirming that fibrin activates human
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
Pierre H Mangin et al.
Haematologica, 103(5), 898-907 (2018-02-24)
Glycoprotein VI, a major platelet activation receptor for collagen and fibrin, is considered a particularly promising, safe antithrombotic target. In this study, we show that human glycoprotein VI signals upon platelet adhesion to fibrinogen. Full spreading of human platelets on
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