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P505-15 hydrochloride

Cat. No. M2063
P505-15 hydrochloride Structure
Synonym:

PRT062607 hydrochloride; PRT-2607 hydrochloride; BIIB-057 hydrochloride

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 180  USD180 In stock
50mg USD 570  USD570 In stock
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Quality Control & Documentation
Biological Activity

P505-15 (also known as PRT062607) is a highly specific and potent, orally bioavailable small molecule spleen tyrosine kinase (Syk) inhibitor (IC50 = 1 nM) with anti-Syk activity that is at least 80-fold greater than its affinity for other kinases. P505-15 potently inhibited B cell antigen receptor-mediated B cell signaling and activation (IC50 0.27 and 0.28 μM, respectively) and Fcε receptor 1-mediated basophil degranulation (IC50 0.15 μM) in human whole blood. Similar levels of ex vivo inhibition were measured after dosing in mice (Syk signaling IC50 0.32 μM). P505-15 (PRT062607) decreased cell viability in NHL and CLL. Oral administration of P505-15 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. In addition, combination treatment of primary CLL cells with P505-15 plus fludarabine produced synergistic enhancement of activity at nanomolar concentrations.

Customer Product Validations & Biological Datas
Source J Pharmacol Exp Ther (2013). Figure 1. P505-15
Method flow cytometry
Cell Lines Ramos cells
Concentrations 2 μM
Incubation Time 72 h
Results These data are consistent with previous observations that P505-15 is a selective and potent inhibitor of Syk, with no appreciable activity against other BCR-related kinases
Chemical Information
Molecular Weight 429.91
Formula C19H23N9O.HCl
CAS Number 1370261-97-4
Solubility (25°C) DMSO 80 mg/mL
Water 80 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Spurgeon SE, et al. J Pharmacol Exp Ther. 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.

[2] Coffey G, et al. J Pharmacol Exp Ther. Specific inhibition of spleen tyrosine kinase suppresses leukocyte immune function and inflammation in animal models of rheumatoid arthritis.

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Keywords: P505-15 hydrochloride, PRT062607 hydrochloride; PRT-2607 hydrochloride; BIIB-057 hydrochloride supplier, Syk, inhibitors, activators


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