PRT-060318; PRT318; P142-76

Nomen chemicum:

2-(((1R,2S)-2-aminocyclohexyl)amino) -4-(m-tolylamino) pyrimidine-5-carboxamide

SMILES Code:

O=C(C1=CN=C(N[C@H]2[C@@H](N)CCCC2)N=C1NC3=CC=CC(C)=C3)N

InChi Code:

InChI=1S/C18H24N6O/c1-11-5-4-6-12(9-11)22-17-13(16(20)25)10-21-18(24-17)23-15-8- 19/h4-6,9-10,14-15H,2-3,7-8,19H2,1H3(H2,21,22; 23,24)/t14-,15+/m0/s1

InChi Key:

NZNTWOVDIXCHHS-LSDHHAIUSA-N

Keyword:

PRT-060318, PRT318, P142–76, PRT060318, PRT 060318, PRT318, PRT-318, PRT 318, 1194961-19-7

Solubilitas:Solutum in DMSO

Repono:0 - 4° C pro brevi termino (dies ad hebdomades), vel -20° C ad terminum longum (menses)

Descriptio:

PRT060318 vehemens et selectivus inhibitor lienis tyrosini kinasi (Syk; IC50 = 4 nM). Est selectiva, inhibens 92% de Syk activitatem, dum aliae kinases retinent >70% actionem, ad collationem 50 nM in decuria. 270 kinases. PRT060318 vetat aggregatio convulxin-plasmatis humani dives plasmatis (IC50 = 2.5 µM) in vitro et prohibet thrombosin in muse transgenico exemplari thrombocytopenia-heparin inducto. Inducit chronica lymphocytica leukemia (CLL) B cellam apoptosim et secretionem chemokinorum CCL3, CCL4, et CXCL13.3 PRT060318 vetat etiam CLL B cellam chemotaxis et pseudoemperipolesis.

Target: Syk