I-PRT-060318; I-PRT318; P142–76

Igama Lekhemikhali:

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

Ikhodi ye-SMILES:

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

Ikhodi ye-InChi:

I-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- 3-2-7 -14(15)19/h4-6,9-10,14-15H,2-3,7-8,19H2,1H3,(H2,20,25)(H2,21,22,23,24)/ t14-,15+/m0/s1

I-InChi Key:

I-NZNTWOVDIXCHHS-LSDHHAIUSA-N

Igama elingukhiye:

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

Ukunyibilika:I-Soluble ku-DMSO

Isitoreji:0 - 4°C isikhathi esifushane (izinsuku ukuya emavikini), noma -20°C isikhathi eside (izinyanga)

Incazelo:

I-PRT060318 iyi-inhibitor enamandla futhi ekhethayo ye-spleen tyrosine kinase (Syk; IC50 = 4 nM). Iyakhetha, ivimbela u-92% womsebenzi we-Syk, kuyilapho amanye ama-kinase egcina umsebenzi ongu->70%, ekuhlanganiseni okungu-50 nM kuphaneli ye-Syk. 270 ama-kinases. I-PRT060318 ivimbela ukuhlangana kwe-convulxin-induced ye-plasma-rich platelet-rich (IC50 = 2.5 μM) ku-vitro futhi ivimbele i-thrombosis kumodeli yegundane ye-transgenic ye-heparin-induced thrombocytopenia. Idala i-lymphocytic leukemia (CLL) B cell apoptosis futhi ivimbele ukukhiqizwa kwama-chemokines CCL3, CCL4, kanye ne-CXCL13.3 PRT060318 futhi ivimbela i-CLL B cell chemotaxis kanye ne-pseudoemperipolesis.

Ithagethi: Syk