PRT-060318; PRT318; P142–76

Ingoa matū:

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

Waehere SMILES:

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

Waehere InChi:

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

Kī InChi:

NZNTWOVDIXCHHS-LSDHHAIUSA-N

Kupumatua:

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

Wairewa:Wairewa i roto i te DMSO

Rokiroki:0 - 4°C mo te wa poto (ra ki nga wiki), -20°C ranei mo te wa roa (marama)

Whakaahuatanga:

Ko te PRT060318 he kaha me te whiriwhiri i te aukati tyrosine kinase (Syk; IC50 = 4 nM) .He mea whiriwhiri, he whakakore i te 92% o te mahi Syk, i etahi atu kinase e pupuri ana i te mahi> 70%, i te kukū o 50 nM i roto i te röpü o 270 kinase. Ka whakakorehia e te PRT060318 te whakahiato-a-convulxin o te plasma platelet-taonga tangata (IC50 = 2.5 μM) in vitro me te aukati i te thrombosis i roto i te tauira kiore transgenic o te heparin-induced thrombocytopenia. Ka whakaawehia te mate pukupuku lymphocytic tawhito (CLL) B apoptosis pūtau me te aukati i te hunanga o nga chemokines CCL3, CCL4, me te CXCL13.3 PRT060318 ka aukati hoki i te CLL B cell chemotaxis me te pseudoemperipolesis.

Whāinga: Syk