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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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
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
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
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
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