P505-15 | Highly selective Syk inhibitor

CAS:
 1370261-97-4
Catalog Number:
 10-4650

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P505-15 (1370261-97-4) is a highly selective and potent (IC50 = 1-2 nM) inhibitor of spleen tyrosine kinase (Syk).1 It potently inhibited B cell antigen receptor-mediated B cell signaling/activation and basophil degranulation. It displayed anti-inflammatory activity in rodent models of rheumatoid arthritis. P505-15 displayed efficacy in vitro and in vivo in non-Hodgkin lymphoma and chronic lymphocytic leukemia models.2,3 It protected against toxin-induced hepatic fibrosis, associated hepatocellular injury, and hepatocarcinogenesis.4 P505-15 was also found to inhibit PINK1 (IC50 = 0.5-3 µM) in HeLa cells and dopaminergic neurons.5

References/Citations:

  1. Coffey et al. (2012), Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis; J. Pharmacol. Exp. Ther. 340 350
  2. Hoellenriegel et al. (2012), Selective, novel spleen tyrosine kinase (Syk) inhibitors suppress chronic lymphocytic leukemia B-cell activation and migration; Leukemia 26 1576
  3. Spurgeon et al. (2013), The selective SYK inhibitor P505-15 (PRT062607) inhibits B cell signaling and function in vitro and in vivo and augments the activity of fludarabine in chronic lymphocytic leukemia; J. Pharmacol. Exp. Ther. 344 378
  4. Torres-Hernandex et al. (2019), Targeting SYK signaling in myeloid cells protects against liver fibrosis and hepatocarcinogenesis; Oncogene 38 4512
  5. Rasool et al. (2024), Identification and structural characterization of small molecule inhibitors of PINK1; Sci. Rep. 14 7739
CAS:
1370261-97-4
Catalog Number:
10-4650
Activity:
Highly selective Syk inhibitor
Chemical Names:
2-[[(1R,2S)-2-Aminocyclohexyl]amino]-4-[3-(triazol-2-yl)anilino]pyrimidine-5-carboxamide hydrochloride
Alternate Name:
PRT062607; BIIB-057
Molecular Weight:
429.91
Molecular Formula:

C19H23N9O·HCl

Solubility:
Soluble in DMSO (25 mg/mL); Water (>25 mg/mL)
Physical Properties:
White solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO or water may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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