PRT062607 (P505-15, BIIB057) HCl

Catalog No.S8032

PRT062607 (P505-15, BIIB057) HCl Chemical Structure

Molecular Weight(MW): 429.91

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, Lyn, FAK, Pyk2 and Zap70.

Size Price Stock Quantity  
In DMSO USD 290 In stock
USD 170 In stock
USD 570 In stock
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5 Customer Reviews

  • Ptpn6fl/fl and Inpp5dfl/fl ALL cells carrying 4-OHT-inducible Cre (Cre) or an empty vector were pre-treated with PRT062607 (2.5 µmol/L) for 2 days. Deletion of Ptpn6 (i) or Inpp5d (j) was induced by addition of 4-OHT and relative changes of GFP1 cells were monitored by flow cytometry.

    Nature, 2015, 521(7552): 357-61. PRT062607 (P505-15, BIIB057) HCl purchased from Selleck.

    ALL cells were treated with vehicle, PRT (2.5 µmol/L), 3AC (7.5 µmol/L) alone, or pre-treated with PRT for 2 days, after which 3AC was added. Viability was monitored by flow cytometry.

    Nature, 2015, 521(7552): 357-61. PRT062607 (P505-15, BIIB057) HCl purchased from Selleck.

  • B cells were stimulated by irradiated CD40L+ L cells. Left: Forward scatter vs. BrdU incorporation analysis (day 5) in the gated CD19+ CLL cells. The distribution of cells with high FSC (blasts, right quadrants) and proliferation (BrdU+, upper quadrants) are shown. Right panel: gated CD19+ CLL cells, stimulated by CD40L in the presence of DMSO or R406 (5 or 50μM). Blastogenesis (%) was calculated by subtracting unstimulated background: stimulated CLL cells [upper right (UR) + lower right (LR) quadrants] – unstimulated CLL cells [UR+LR]. Proliferation (%): stimulated CLL cells [upper left (UL) + upper right (UR)] quadrants)-unstimulated CLL cells [UL+UR]. Wilcoxon signed-rank test, n=10, P<0.006 for all comparisons in (D); no significant differences in (E) (n=10).

    Haematologica, 2016, 101(2):e59-62.. PRT062607 (P505-15, BIIB057) HCl purchased from Selleck.

    Dectin-1 is involved in activation of NLRP3-inflammasome by Malassezia spp. IL-1b secretion from mature human mono-DCs incubated with Syk-inhibitors (piceatannol, R406 or P505), 1 h prior to exposure to medium, MSU, b-glucan, nigericin or live M. furfur (MOI = 10) was determined after 6 h by ELISA.

    Exp Dermatol 2014 23(12), 884-9. PRT062607 (P505-15, BIIB057) HCl purchased from Selleck.

  • Change of protein and mRNA with or without the pretreatment of Syk inhibitors. After pretreated with PRT062607 and Piceatannol for 30 min before A. fumigatus hyphae stimulation, activation of Syk was inhibited by 1 μM PRT062607 (p < 0.05), 2 μM PRT062607 (p < 0.01), 5 μM Piceatannol (p < 0.05), 10 μM Piceatannol (p < 0.01) a compared with untreated cells. **means p < 0.01, *p < 0.05.

    BMC Ophthalmol, 2015, 15:55.. PRT062607 (P505-15, BIIB057) HCl purchased from Selleck.

Purity & Quality Control

Choose Selective Syk Inhibitors

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, Lyn, FAK, Pyk2 and Zap70.
Targets
Syk [1]
(Cell-free assay)
FGR [1]
(Cell-free assay)
MLK1 [1]
(Cell-free assay)
1 nM 81 nM 88 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 NHvMWnRHfW6ldHnvckBie3OjeR?= NF3yV49KdmirYnn0bY9vKG:oIGPZT{BqdiCqdX3hckBT[W2xczDj[YxteyxiSVO1NF0xNjJ{MzFOwG0> MojLNlM{PTB6NEe=
human Ramos cells NXXWcXVDS3m2b4TvfIlkyqCjc4PhfS=> MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDSZY1weyClZXzsd{whUUN3ME2wMlIzOyEQvF2= MW[yN|E2OTB3NB?=
human whole blood MlnxSpVv[3Srb36gZZN{[Xl? MXnJcohq[mm2aX;uJI9nKFO7azDpckBpfW2jbjD3bI9t\SCkbH;v[EBie3Onc4Pl[EBieyCrbnjpZol1cW:wIH;mJHAuW0ySN{[gbY4hS0RzNDugcY9vd2O7dHXzJIJ6KG[ub4egZ5l1d22ndIL5MEBKSzVyPUCuPVUzKM7:TR?= MYCyOFczPjhyNh?=
C57BL/6 mouse bone marrow cells M2W0e2N6fG:2b4jpZ:Kh[XO|YYm= M1XQXVUhcA>? NWPneWlPS3m2b4TvfIlkcXS7IHHnZYlve3RiQ{W3RmwwPiCvb4Xz[UBjd26nIH3hdpJwfyClZXzsd{Bie3Onc4Pl[EBieyCpcn;3eIghcW6qaXLpeIlwdiCycnXpcoN2[mG2ZXSg[o9zKDRiZHH5d{Bnd2yub4fl[EBjgSCdM1jdMZRpgW2rZHnu[UBi\GSrdHnvckBu\WG|dYLl[EBi\nSncjC1JIhzeyCkeTDi[ZRieGyjdHWgZ492dnSrbnegZY5idHm|aYOsJGlEPTB;NT64OVMh|ryP Mkf4NlU3OzN5NEG=
CHO cells MXPGeY5kfGmxbjDhd5NigQ>? MlHLTY5pcWKrdHnvckBw\iCqdX3hckBGWkdiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{BjgSCjdYTvcYF1\WRiUYDheINpKGOuYX3wJIF{e2G7LDDJR|UxRThwNjFOwG0> NIjOcVMzPTZ|M{e0NS=>

... Click to View More Cell Line Experimental Data

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]

Protocol

Kinase Assay:

[1]

+ Expand

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:

[1]

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

    CellTiter Glo


    (Only for Reference)
Animal Research:

[1]

+ Expand
  • Animal Models: Mouse Collagen Antibody-Induced Arthritis Model
  • Formulation: --
  • 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:
Saline
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
Formula

C19H23N9O.HCl

CAS No. 1370261-97-4
Storage powder
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01652937 Withdrawn 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

Tel: +1-832-582-8158 Ext:3

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Syk Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID