| Identification | Back Directory | [Name]
PRT062607 acetate | [CAS]
1370261-98-5 | [Synonyms]
P50515 Acetate
P505-15 Acetate
P505 15 Acetate
PRT062607 acetate
4-((3-(2H-1,2,3-Triazol-2-yl)phenyl)amino)-2-(((1R,2S)-2-aminocyclohexyl)amino)pyrimidine-5-carboxamide acetate | [Molecular Formula]
C21H27N9O3 | [MDL Number]
MFCD23105961 | [MOL File]
1370261-98-5.mol | [Molecular Weight]
453.51 |
| Hazard Information | Back Directory | [Uses]
PRT062607 (P505-15) acetate is an orally available Syk inhibitor (IC50: 1 nM) that inhibits inflammation and induction Apoptosis. PRT062607 acetate exerts potent antitumor activity in tumor xenograft mouse models[1].[2]. | [in vivo]
PRT062607 acetate produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. PRT062607 acetate (15, 30 mg/kg; po; bid; 5 d) causes SYK inhibition in mice and prevents BCR-induced splenomegaly in mice[1].
PRT062607 acetate (15 mg/kg; po ; bid; 5 d) SYK inhibition in mice prevents Ramos tumor formation in mouse xenograft models[1].
PRT062607 acetate (10-20 mg/kg; po; bid) prevents BCR mediated splenomegaly and significantly inhibited NHL tumor growth in xenograft models[2].
| Animal Model: | anti-IgD Stimulated Mouse Inflammation Model[1] | | Dosage: | 10 mg/kg, 15 mg/kg, 20 mg/kg | | Administration: | po; bid for 5 days | | Result: | Suppressed mouse B-cell activation following stimulation with this anti-IgD. |
| Animal Model: | Ramos Tumor Xenograft Model in NOD/SCID mice[1] | | Dosage: | 15 mg/kg, 30 mg/kg | | Administration: | po; bid; terminated when tumor weights began reaching approximately 1.5 mg, at which time tumors were excised and weighed. | | Result: | Protected mouse from Ramos tumor growth in vivo.
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| [IC 50]
Lck: 249 nM (IC50, [2]); PAK5: 166 nM (IC50, [2]) | [References]
[1] Spurgeon SE, et al. 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. 2013 Feb;344(2):378-87. DOI:10.1124/jpet.112.200832
[2] Coffey G, et al. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis. J Pharmacol Exp Ther. 2012 Feb;340(2):350-9. DOI:10.1124/jpet.111.188441 |
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| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
AstaTech, Inc
|
| Tel: |
(215) 785 3197 |
| Website: |
www.astatechinc.com |
|