CAS No. 1370261-97-4

Molecular Formula: C19H24ClN9O
Molecular Weight: 429.90656

Molecular Weight: 429.91
Molecular Formula: C19H23N9O.HCl
Canonical SMILES: C1CCC(C(C1)N)NC2=NC=C(C(=N2)NC3=CC=CC(=C3)N4N=CC=N4)C(=O)N.Cl
InChI: InChI=1S/C19H23N9O.ClH/c20-15-6-1-2-7-16(15)26-19-22-11-14(17(21)29)18(27-19)25-12-4-3-5-13(10-12)28-23-8-9-24-28;/h3-5,8-11,15-16H,1-2,6-7,20H2,(H2,21,29)(H2,22,25,26,27);1H/t15-,16+;/m0./s1
InChIKey: RMNLLPXCNDZJMJ-IDVLALEDSA-N
Purity: 98%
Solubility: Soluble in DMSO, Water
Storage: Store at -20°C
Synonyms: 5-Pyrimidinecarboxamide, 2-[[(1R,2S)-2-aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-, hydrochloride (1:1); PRT2607 HCl; PRT-2607 HCl; PRT 2607 HCl; RPRT062607 HCl; PRT-062607 HCl; PRT 062607 HCl; P505-15 HCl; BIIB057 HCl; BIIB 057 HCl; 2-[[(1R,2S)-2-Aminocyclohexyl]amino]-4-[[3-(2H-1,2,3-triazol-2-yl)phenyl]amino]-5-pyrimidinecarboxamide hydrochloride
Description
PRT062607, also known as PRT2607, P505-15, and BIIB057, is a novel, highly selective, and orally bioavailable small molecule SYK inhibitor (SYK IC(50) = 1 nM) with anti-SYK activity that is at least 80-fold greater than its affinity for other kinases. PRT062607 successfully inhibited SYK-mediated B-cell receptor signaling and decreased cell viability in NHL and CLL. Oral dosing in mice prevented BCR-mediated splenomegaly and significantly inhibited NHL tumor growth in a xenograft model. In addition, combination treatment of primary CLL cells with PRT062607 plus fludarabine produced synergistic enhancement of activity at nanomolar concentrations. PRT062607 may be a therapeutic agent for B-cell malignancies. A dose finding study in healthy volunteers has been completed.


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