Fostamatinib disodium hexahydrate

別名:Tavalisse, R788 disodium hexahydrate, Tamatinib Fosdium hexahydrate

Fostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay.

Fostamatinib disodium hexahydrate化学構造

CAS No. 914295-16-2

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
JPY 58000 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(3)

製品安全説明書

現在のバッチを見る: S494401 DMSO] 100 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false 純度: 99.8%
99.8

Fostamatinib disodium hexahydrate関連製品

シグナル伝達経路

Syk阻害剤の選択性比較

生物活性

製品説明 Fostamatinib (R788) disodium (Tamatinib Fosdium) hexahydrate, a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay.
Targets
Syk [1]
(Cell-free assay)
41 nM
In Vitro
In vitro

R788 is a prodrug of the spleen tyrosine kinase (Syk) inhibitor R406. R788 is a competitive inhibitor for ATP binding with a Ki of 30 nM. R788 dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM. R788 also inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. Inhibition of Syk by R788 results in inhibition of all phosphorylation events downstream of Syk signaling. Next to FcϵRI signaling in CHMC, R788 most potently inhibits the signaling of IL-4 and IL-2 receptors. R788 specifically inhibits FcγR signaling in human mast cells, macrophages, and neutrophils. R788 can inhibit local inflammatory injury mediated by immune complexes.[1] R788 induces apoptosis of the majority of examined DLBCL cell lines. In R788-sensitive DLBCL cell lines, R788 specifically inhibits both tonic- and ligand-induced BCR signaling (autophosphorylation of SYK525/526 and SYK-dependent phosphorylation of the B-cell linker protein [BLNK]).[2]

Kinase Assay Fluorescence polarization kinase assay and Ki determination
The fluorescence polarization reactions are performed. For Ki determination, duplicate 200-μL reactions are set up at eight different ATP concentrations from 200 μM (2-fold serial dilutions) in the presence of either DMSO or R788 at 125, 62.5, 31.25, 15.5, or 7.8 nM. At different time points, 20 μL of each reaction is removed and quenched to stop the reaction. For each concentration of R788, the rate of reaction at each concentration of ATP is determined and plotted against the ATP concentration to determine the apparent Km and Vmax. Finally the apparent Km (or apparent Ki/Vmax) is plotted against the inhibitor concentration to determine the Ki.
細胞実験 細胞株 Cultured human mast cells (CHMC)
濃度 0-100 μM
反応時間 0.5 h
実験の流れ

Cultured human mast cells (CHMC) are derived from cord blood CD34+ progenitor cells and grown, primed, and stimulated and shown in supplemental data. Before stimulation, cells are incubated with R788 or DMSO for 30 minutes. Cells are then stimulated with either 0.25 to 2 mg/mL anti-IgE or anti-IgG or 2 μM ionomycin. For tryptase measurement, ~1500 cells per well are stimulated for 30 min in modified Tyrode's buffer. For LTC4 and cytokine production, 100,000 cells per well are stimulated for 1 or 7 hours, respectively. Tryptase activity is measured by luminescence readout of a peptide substrate, and LTC4 and cytokines are measured using Luminex multiplex technology.

In Vivo
In Vivo

Oral administration of R788 to mice reduces immune complex-mediated inflammation in a reverse-passive Arthus reaction and two antibody-induced arthritis models.[1] In another study, R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolongs survival of the treated animals.[3] R788 demonstrates a significant reduction in major inflammatory mediators such as TNFalpha, IL-1, IL-6 and IL-18, leading to reduced inflammation and bone degradation in models of rheumatoid arthritis.[4]

動物実験 動物モデル Balb/c mice with arthritis
投与量 1 mg/kg or 5 mg/kg
投与経路 o.g.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05904093 Not yet recruiting
Sickle Cell Disease|Hb-SS Disease|Hemoglobin S|Disease Sickle Cell Anemia|Sickle Cell Disorders|Hemoglobin Beta Thalassemia Disease
National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)
May 15 2024 Phase 1
NCT05509582 Enrolling by invitation
Immune Mediated Anemia|Immune Mediated Thrombocytopenia|Chronic GVHD
National Heart Lung and Blood Institute (NHLBI)|National Institutes of Health Clinical Center (CC)
May 15 2024 Phase 2
NCT06071520 Completed
Primary Immune Thrombocytopenia
Fundación Pública Andaluza para la gestión de la Investigación en Sevilla
March 1 2023 --
NCT05613296 Not yet recruiting
ITP - Immune Thrombocytopenia|Chronic ITP|Refractory ITP
Gruppo Italiano Malattie EMatologiche dell''Adulto
February 2023 --
NCT04543279 Terminated
Myelofibrosis|Thrombocytopenia
Washington University School of Medicine|Rigel Pharmaceuticals
May 3 2021 Phase 2
NCT04904276 Terminated
ITP|Immune Thrombocytopenia
Rigel Pharmaceuticals
May 18 2021 --

化学情報

分子量 732.51 化学式

C23H36FN6Na2O15P

CAS No. 914295-16-2 SDF --
Smiles O.O.O.O.O.O.[Na+].[Na+].COC1=CC(=CC(=C1OC)OC)NC2=NC=C(F)C(=N2)NC3=NC4=C(OC(C)(C)C(=O)N4CO[P]([O-])([O-])=O)C=C3
保管 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (136.51 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 : Insoluble

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

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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