ホームページ Angiogenesis Syk inhibitor - Pyk2 inhibitor - FAK inhibitor - PAK inhibitor - Src inhibitor - Mixed Lineage Kinase inhibitor - FLT3 inhibitor PRT062607 (P505-15) HCl For research use only.

PRT062607 (P505-15) HCl

別名：BIIB057, PRT-2607

PRT062607 (P505-15, BIIB057, PRT-2607) 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化学構造

CAS No. 1370261-97-4

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 43500 国内在庫あり
JPY 25500 国内在庫あり
JPY 85500 国内在庫なし(納期7~10日)
JPY 598500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

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PRT062607 (P505-15) HCl関連製品

シグナル伝達経路

Syk Signaling Pathways

Sykシグナル伝達経路

Syk阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
Ramos B Function assay 30 mins Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis, IC50 = 0.178 μM. 26320624
Ramos B Function assay 30 mins Inhibition of Syk in anti-igM stimulated human Ramos B cells assessed as phospho-BLNK level preincubated for 30 mins followed by anti-IgM stimulation measured after 15 mins by flow cytometric analysis, IC50 = 0.178 μM. 25633741
Jurkat T Function assay 30 mins Inhibition of ZAP70 in anti-CD3 stimulated human Jurkat T cells assessed as SLP76 phosphorylation at Y128 preincubated for 30 mins followed by anti-CD3 stimulation measured after 2 mins by FACS analysis, IC50 = 1.805 μM. 25633741
bone marrow cells Cytotoxicity assay 4 days Cytotoxicity against C57BL/6 mouse bone marrow cells assessed as growth inhibition preincubated for 4 days followed by [3H]-thymidine addition measured after 5 hrs by betaplate counting analysis, IC50 = 5.853 μM. 25633741
Ramos Function assay Inhibition of Syk in anti IgM-stimulated human Ramos cells assessed as BLNK phosphorylation by cellular assay, IC50 = 0.178 μM. 24726806
Ramos Cytotoxicity assay Cytotoxicity against human Ramos cells, IC50 = 0.223 μM. 23151054
Ramos Function assay Inhibition of SYK in human Ramos cells, IC50 = 0.223 μM. 23350847
bone marrow cells Function assay Inhibition of IL3 dependent proliferation in C57/B16 mouse bone marrow cells using [3H]thymidine by liquid scintillation counting, IC50 = 5.853 μM. 24726806
CHO Function assay Inhibition of human ERG expressed in CHO cells by automated Qpatch clamp assay, IC50 = 8.6 μM. 25633741
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生物活性

製品説明 PRT062607 (P505-15, BIIB057, PRT-2607) 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)		 もっとクリックする
1 nM 81 nM 88 nM 108 nM 123 nM
In Vitro
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]
Kinase Assay 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.
細胞実験 細胞株 Syk-dependent BaF3 cell
濃度 ~6 μM
反応時間 3 days
実験の流れ

CellTiter Glo
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-Syk / Syk / p-FLT3 / FLT3 / p-STAT5 / STAT5 Bcl6 24525236
Growth inhibition assay Cell viability 28064214
In Vivo
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]
動物実験 動物モデル Mouse Collagen Antibody-Induced Arthritis Model
投与量 5, 15, 30 mg/kg, b.i.d.
投与経路 Oral
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01652937 Withdrawn
Rheumatoid Arthritis
Biogen
 August 2012 Phase 2

化学情報

分子量 429.91 化学式

C19H23N9O.HCl
CAS No. 1370261-97-4 SDF Download PRT062607 (P505-15) HCl SDFをダウンロードする
Smiles C1CCC(C(C1)N)NC2=NC=C(C(=N2)NC3=CC(=CC=C3)N4N=CC=N4)C(=O)N.Cl
保管

In vitro
Batch:

DMSO : 86 mg/mL ( (200.04 mM)； 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 30 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

mg/kg g μL 匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH2O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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