P505-15 | Highly selective Syk inhibitor

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

Available Options

Size:PriceQuantity 
5 mg$75.00
25 mg$250.00

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:

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