PRT062607 (P505-15) HCl

Catalog No.S8032 Synonyms: BIIB057, PRT-2607

For research use only.

PRT062607 (P505-15, BIIB057, PRT-2607) 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.

PRT062607 (P505-15) HCl Chemical Structure

CAS No. 1370261-97-4

Selleck's PRT062607 (P505-15) HCl has been cited by 41 publications

Purity & Quality Control

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Biological Activity

Description PRT062607 (P505-15, BIIB057, PRT-2607) 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.
Targets
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)
Click to View More Targets
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
Ramos MVPGeY5kfGmxbjDhd5NigQ>? NITMfo9KdmirYnn0bY9vKG:oIGP5b{BqdiCjboTpJGloVS2|dHnteYxifGWmIHj1cYFvKFKjbX;zJINmdGy|IHHzd4V{e2WmIHHzJGJNVkticHjvd5Bpd3K7bHH0bY9vKGK7IHPlcIx2dGG{IHHzd4F6NCCLQ{WwJF0hOC5zN{ig{txONg>? NIjqcms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEeyOlgxPid-MkS3NlY5ODZ:L3G+
Ramos B MYPGeY5kfGmxbjDhd5NigQ>? NUK5PIl[OzBibXnudy=> NHjoNIpKdmirYnn0bY9vKG:oIGP5b{BqdiCjboTpMYloVSC|dHnteYxifGWmIHj1cYFvKFKjbX;zJGIh[2WubIOgZZN{\XO|ZXSgZZMheGixc4Doc{1DVE6NIHzleoVtKHC{ZXnuZ5Vj[XSnZDDmc5IhOzBibXnud{Bnd2yub4fl[EBjgSCjboTpMWloVSC|dHnteYxifGmxbjDt[YF{fXKnZDDh[pRmeiBzNTDtbY5{KGK7IH\sc5ch[3m2b33leJJq[yCjbnHsfZNqeyxiSVO1NEA:KDBwMUe4JO69VS5? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|M{e0NUc,OjV4M{O3OFE9N2F-
Ramos B MUfGeY5kfGmxbjDhd5NigQ>? NHzKZYU{OCCvaX7z Mmm2TY5pcWKrdHnvckBw\iCVeXugbY4h[W62aT3p[20he3SrbYXsZZRm\CCqdX3hckBT[W2xczDCJINmdGy|IHHzd4V{e2WmIHHzJJBpd3OyaH:tRmxPUyCuZY\lcEBxemWrbnP1ZoF1\WRiZn;yJFMxKG2rboOg[o9tdG:5ZXSgZpkh[W62aT3J[20he3SrbYXsZZRqd25ibXXhd5Vz\WRiYX\0[ZIhOTVibXnud{BjgSCobH;3JIN6fG:vZYTybYMh[W6jbInzbZMtKEmFNUCgQUAxNjF5ODFOwG0v M3W0VFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ4M{KwOlI1Lz5{NkOyNFYzPDxxYU6=
Ramos MX3DfZRwfG:6aXPpeJkh[XO|YYm= NXm2VG9XS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hWmGvb4OgZ4VtdHNuIFnDOVAhRSByLkKyN{DPxE1w NYiweZRlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOxOVExPTRpPkKzNVUyODV2PD;hQi=>
Ramos NV\Y[W9HTnWwY4Tpc44h[XO|YYm= NHrvWYFKdmirYnn0bY9vKG:oIGPZT{BqdiCqdX3hckBT[W2xczDj[YxteyxiSVO1NEA:KDBwMkKzJO69VS5? M2HucFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|M{WwPFQ4Lz5{M{O1NFg1PzxxYU6=
Jurkat T NFnPWWxHfW6ldHnvckBie3OjeR?= NX74b2gzOzBibXnudy=> NHzESWZKdmirYnn0bY9vKG:oIGrBVFcxKGmwIHHueIkuS0R|IIP0bY12dGG2ZXSgbJVu[W5iSoXyb4F1KFRiY3XscJMh[XO|ZYPz[YQh[XNiU1zQO|YheGixc4Doc5J6dGG2aX;uJIF1KFlzMkigdJJmcW6ldXLheIVlKG[xcjCzNEBucW6|IH\vcIxwf2WmIHL5JIFvfGlvQ1SzJJN1cW23bHH0bY9vKG2nYYP1doVlKGGodHXyJFIhdWmwczDifUBHSUOVIHHuZYx6e2m|LDDJR|UxKD1iMT64NFUh|ryPLh?= MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPTZ|M{e0NUc,OjV4M{O3OFE9N2F-
bone marrow cells MlP1R5l1d3SxeHnjbZR6KGG|c3H5 M4q2RlQh\GG7cx?= MXnDfZRwfG:6aXPpeJkh[WejaX7zeEBEPTeETD:2JI1wfXOnIHLvcoUhdWG{cn;3JINmdGy|IHHzd4V{e2WmIHHzJIdzd3e2aDDpcohq[mm2aX;uJJBz\WmwY4XiZZRm\CCob4KgOEBl[Xm|IH\vcIxwf2WmIHL5JHs{UF1vdHj5cYllcW6nIHHk[Il1cW:wIH3lZZN2emWmIHHmeIVzKDViaILzJIJ6KGKndHHwcIF1\SClb4XueIlv\yCjbnHsfZNqeyxiSVO1NEA:KDVwOEWzJO69VS5? NFq3cnU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zN|c1OSd-MkW2N|M4PDF:L3G+
bone marrow cells MmXxSpVv[3Srb36gZZN{[Xl? M4raXWlvcGmkaYTpc44hd2ZiSVyzJIRmeGWwZHXueEBxem:uaX\ldoF1cW:wIHnuJGM2Py:EMU[gcY92e2ViYn;u[UBu[XK{b4egZ4VtdHNidYPpcochYzOKXYTofY1q\GmwZTDifUBtcXG3aXSgd4NqdnSrbHzheIlwdiClb4XueIlv\yxiSVO1NEA:KDVwOEWzJO69VS5? M2joU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{K2PFA3Lz5{NEeyOlgxPjxxYU6=
CHO NGrhdINHfW6ldHnvckBie3OjeR?= MojPTY5pcWKrdHnvckBw\iCqdX3hckBGWkdiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{BjgSCjdYTvcYF1\WRiUYDheINpKGOuYX3wJIF{e2G7LDDJR|UxKD1iOD62JO69VS5? NH3mVIc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NU[zN|c1OSd-MkW2N|M4PDF:L3G+
Assay
Methods Test Index PMID
Western blot p-Syk / Syk / p-FLT3 / FLT3 / p-STAT5 / STAT5 ; Bcl6 24525236 25759025
Growth inhibition assay Cell viability 28064214
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 (from reference)

Kinase Assay:

[1]

  • 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]

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

    CellTiter Glo

Animal Research:

[1]

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

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 429.91
Formula

C19H23N9O.HCl

CAS No. 1370261-97-4
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CCC(C(C1)N)NC2=NC=C(C(=N2)NC3=CC(=CC=C3)N4N=CC=N4)C(=O)N.Cl

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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