PRT062607 (P505-15) HCl

For research use only.

Catalog No.S8032 Synonyms: BIIB057

31 publications

PRT062607 (P505-15) HCl Chemical Structure

CAS No. 1370261-97-4

PRT062607 (P505-15, BIIB057) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.

Size Price Stock Quantity  
10mM (1mL in DMSO) EUR 285 In stock
EUR 167 In stock
EUR 560 In stock
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Selleck's PRT062607 (P505-15) HCl has been cited by 31 publications

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Biological Activity

Description PRT062607 (P505-15, BIIB057) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
Syk [1]
(Cell-free assay)
FGR [1]
(Cell-free assay)
MLK1 [1]
(Cell-free assay)
PYK2 [1]
(Cell-free assay)
YES [1]
(Cell-free assay)
1 nM 81 nM 88 nM 108 nM 123 nM
In vitro

PRT062607(P505-15) anti-SYK activity is at least 80-fold greater than its affinity for other kinases. at least 80-fold greater than its affinity for other kinases. PRT062607 potently inhibits 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). [1] PRT062607 inhibits BCR-dependent secretion of the chemokines CCL3 and CCL4 by CLL cells, and leukemia cell migration toward the tissue homing chemokines CXCL12, CXCL13, and beneath stromal cells. PRT062607 furthermore inhibits Syk and extracellular signal-regulated kinase phosphorylation after BCR triggering. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Ramos cells NEnrXWdHfW6ldHnvckBie3OjeR?= MmPPTY5pcWKrdHnvckBw\iCVWVugbY4hcHWvYX6gVoFud3NiY3XscJMtKEmFNUC9NE4zOjNizszN Mm\ZNlM{PTB6NEe=
human Ramos cells Mm\PR5l1d3SxeHnjxsBie3OjeR?= NH\YflJEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBT[W2xczDj[YxteyxiSVO1NF0xNjJ{MzFOwG0> NHm5UHMzOzF3MUC1OC=>
human whole blood NF7VeIhHfW6ldHnvckBie3OjeR?= NV7iRW5[UW6qaXLpeIlwdiCxZjDTfYshcW5iaIXtZY4hf2ixbHWgZoxwd2RiYYPz[ZN{\WRiYYOgbY5pcWKrdHnvckBw\iCSLWPMVFc3KGmwIFPENVQsKG2xbn;jfZRmeyCkeTDmcI94KGO7dH;t[ZRzgSxiSVO1NF0xNjl3MjFOwG0> MlfKNlQ4OjZ6ME[=
C57BL/6 mouse bone marrow cells NHHJXIVEgXSxdH;4bYPDqGG|c3H5 M3PiV|UhcA>? MVnDfZRwfG:6aXPpeJkh[WejaX7zeEBEPTeETD:2JI1wfXOnIHLvcoUhdWG{cn;3JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJJBz\WmwY4XiZZRm\CCob4KgOEBl[Xm|IH\vcIxwf2WmIHL5JHs{UF1vdHj5cYllcW6nIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDViaILzJIJ6KGKndHHwcIF1\SClb4XueIlv\yCjbnHsfZNqeyxiSVO1NF02Njh3MzFOwG0> M2rzUlI2PjN|N{Sx
CHO cells MVjGeY5kfGmxbjDhd5NigQ>? MW\Jcohq[mm2aX;uJI9nKGi3bXHuJGVTTyCneIDy[ZN{\WRiaX6gR2hQKGOnbHzzJIJ6KGG3dH;tZZRm\CCTcHH0Z4gh[2yjbYCgZZN{[XluIFnDOVA:QC54IN88US=> NY\ieIU1OjV4M{O3OFE>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-Syk / Syk / p-FLT3 / FLT3 / p-STAT5 / STAT5 ; 

PubMed: 24525236     

Western blot for indicated proteins from MOLM-14 and MV4–11 cells treated with 3 µM PRT062607 or 5 µM Merck SYKi. The phosphosite Y768 was detected on FLT3 total immunoprecipitate


PubMed: 25759025     

BCL6 protein expression by Western blotting in presence or absence of SYK inhibitor (PRT062607, 10 μmol/l for 24 hr in a TCF3-PBX1 ALL cell line (RCH-ACV) and a primary sample (ICN12) cells.

24525236 25759025
Growth inhibition assay
Cell viability ; 

PubMed: 28064214     

Cell viability normalized to DMSO controls in 5 BL cell lines treated with the indicated concentrations of PRT062607.

In vivo The pharmacokinetic/pharmacodynamic relationship predicted that 70% Syk suppression is maintained in mice over a 24h period after 30 mg/kg dosing. At 15 mg/kg, Syk inhibition ranges from 7.5% (Cmin) to 78.4% (Cmax) with an average inhibition of 67% over 24 h. Oral administration of PRT062607 produced dose-dependent anti-inflammatory activity in two rodent models of rheumatoid arthritis. Statistically significant efficacy is observed at concentrations that specifically suppressed Syk activity by 67%.[1]


Kinase Assay:


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fluorescence resonance energy transfer (FRET) assay:

The extent of substrate phosphorylation by Syk is measured in the presence of various PRT062607 concentrations. Syk activity is determined by a fluorescent antibody specific for phosphorylated tyrosine by using the increase of FRET. Twelve concentrations are tested for dose response. Specificity and potency of kinase inhibition is determined by evaluation of PRT062607 in the Millipore KinaseProfiler panel of 270 independent purified kinase assays. For profiling, PRT062607 is tested in duplicate at two concentrations at a fixed concentration of ATP. Subsequently, IC50 determinations using the radioactive assays are carried out at an ATP concentration optimized for each individual kinase. All radioactive ATP incorporationenzyme assays are performed at Millipore.
Cell Research:


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  • Cell lines: Syk-dependent BaF3 cell
  • Concentrations: ~6 μM
  • Incubation Time: 3 days
  • Method:

    CellTiter Glo

    (Only for Reference)
Animal Research:


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  • Animal Models: Mouse Collagen Antibody-Induced Arthritis Model
  • Dosages: 5, 15, 30 mg/kg, b.i.d.
  • Administration: Oral
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (200.04 mM)
Water 86 mg/mL (200.04 mM)
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 429.91


CAS No. 1370261-97-4
Storage powder
in solvent
Synonyms BIIB057
Smiles C1CCC(C(C1)N)NC2=NC=C(C(=N2)NC3=CC(=CC=C3)N4N=CC=N4)C(=O)N.Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01652937 Withdrawn Drug: BIIB057|Drug: Placebo Rheumatoid Arthritis Biogen August 2012 Phase 2

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Syk Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID