PRT-060318 (PRT318) is a novel selective Syk tyrosine kinase inhibitor with an IC50 of 4 nM. It is a treatment for heparin-induced thrombocytopenia.

 

Brand: BCM

 

Target: Syk

 

Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors

 

In Vitro: PRT318 inhibits platelet activation via GPVI/FcRγ, an ITAM receptor complex, but not via ADP or thrombin, which are G-protein coupled receptors. PRT318 effectively antagonizes CLL(chronic lymphocytic leukemia) cell survival after BCR triggering and in nurse-like cell-co-cultures. PRT318 inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering.

 

Melting Point: 152 - 155°C

 

Boiling Point: 602.1±65.0 °C(Predicted)

 

pKa: 14.10±0.50(Predicted)

 

Solubility: Soluble in DMSO; Soluble in Water. Insoluble in Ethanol.

 

GHS: GHS02

 

Isomeric SMILES: CC1=CC(=CC=C1)NC2=NC(=NC=C2C(=O)N)N[C@@H]3CCCC[C@@H]3N  

 

InChIKey: NZNTWOVDIXCHHS-LSDHHAIUSA-N  

 

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

 

Attribute
[Chem Name]	2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-(3-methylanilino)pyrimidine-5-carboxamide
[Synonym]	PRT-060318 2HCl; PRT318
[CAS No.]	1194961-19-7
[MDL No.]	MFCD28155088
[Formula]	C18H24N6O
[Molecular]	340.42
[Form]	Pale Brown Solid
[Storage]	Keep in dark place. Inert atmosphere. Room temperature

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