ホームページ Protein Tyrosine Kinase CSF-1R inhibitor GW2580 For research use only.

GW2580

別名：SC-203877

GW2580 (SC-203877) is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.

GW2580化学構造

CAS No. 870483-87-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 40500 国内在庫あり
JPY 220500 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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GW2580関連製品

シグナル伝達経路

CSF-1R Signaling Pathways

CSF-1Rシグナル伝達経路

CSF-1R阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
human PBMC Function assay Inhibition of LPS-induced IL6 production in human PBMC by ELISA, EC50=1.89 μM 23095041
human HN5 cells Growth inhibition assay Growth inhibition of serum-stimulated human HN5 cells after 3 days by spectrophotometry, IC50=29 μM 16249345
human BT474 cells Growth inhibition assay Growth inhibition of serum-stimulated human BT474 cells after 3 days by spectrophotometry, IC50=21 μM 16249345
mouse NSO cells Growth inhibition assay Growth inhibition of serum-stimulated mouse NSO cells after 3 days by spectrophotometry, IC50=13.5 μM 16249345
HUVEC Growth inhibition assay Growth inhibition of VEGF-stimulated HUVEC after 3 days by spectrophotometry 16249345
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生物活性

製品説明 GW2580 (SC-203877) is a selective CSF-1R inhibitor for c-FMS with IC50 of 30 nM, 150- to 500-fold selective compared to b-Raf, CDK4, c-KIT, c-SRC, EGFR, ERBB2/4, ERK2, FLT-3, GSK3, ITK, JAK2 etc.
Targets
c-Fms [1]
30 nM
In Vitro
In vitro GW2580 completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 inhibits the growth of CSF-1 stimulated M-NFS-60 myeloid tumor cells, serum stimulated NSO myeloid tumor cells, CSF-1 stimulated freshly isolated human monocytes, and VEGF stimulated human umbilical vein vascular endothelial cells with IC50 of 0.33, 13.5, 0.47 and 12 μM, respectively. 1 μM GW2580 completely inhibits CSF-1-induced growth of mouse M-NFS-60 myeloid cells and human monocytes and completely inhibits bone degradation in cultures of human osteoclasts, rat calvaria, and rat fetal long bone. [1] GW2580 inhibits CSF1R phosphorylation in RAW264.7 murine macrophages stimulated with 10 ng/mL with IC50 of approximately 10 nM. [2] GW2580 also inhibits TRKA activity with IC50 of 0.88 μM. [3]
Kinase Assay cFMS tyrosine kinase assay
The enzyme is activated by autophosphorylation by incubating 10 μM enzyme, 100 μM ATP, and 5 mM MgCl2 in 50 mM Tris HCL for 90 min at room temperature. Enzyme reactions are performed in a volume of 45 μL, by using round-bottom polystyrene 96-well plates on a Biomek 2000. Compound in 1 μL DMSO or DMSO alone are added to each well containing 30 μL of a 1.5× substrate reaction mix containing 50 mM Mops (3-[N-Morpholino]propanesulfonic acid), pH 7.5, 15 mM MgCl2, 6 μM peptide substrate, biotin-EAIYAPFAKKK-NH2 7.5 mM DTT, 75 mM NaCl, 10 μM ATP, and 0.5 μCi (1 Ci = 37 GBq) [33P-γ] ATP per assay. The reaction is initiated by the addition of 15 μL of diluted enzyme solution, resulting in a final enzyme concentration 20 nM. EDTA is added to control wells for determination of background. The reaction is allowed to proceed for 40 min and stopped by the addition of an equal volume of 0.5% phosphoric acid, and 75 μL is transferred to a 96-well phosphocellulose filter plate that has been prewet with 100 μL of 0.5% phosphoric acid. The plate is filtered on a Millipore filter-plate vacuum manifold and washed three times with the phosphoric acid solution, followed by the addition of 40 μL of scintillation solution. The plates are sealed and counted in a Packard Topcount NXT scintillation counter.
細胞実験 細胞株 MCSF-dependent mouse myeloid M-NFS-60 cell line
濃度 ~20 μM
反応時間 3 days
実験の流れ One day before the start of the cell growth assay the cells are spun down and placed in a depleted media at 2× 106 cells per ml for 24 h. Depleted medium for M-NSF60 cells lacks MCSF. The next day, GW2580 at 10 mM in DMSO is diluted to 20 μM and 0.2% DMSO in medium containing 10% serum and serially diluted to yield a 10-point concentration curve. The M-NFS-60 cells are resuspended in medium at 0.5× 106 cells/mL with 10% serum and 20 ng/mL mouse MCSF. Cells (50 μL) are added to each well containing inhibitor (50 μL), and, 3 days later, 10 μL of WST-1 reagent is added to each well. After a 4-h incubation, the absorbance is measured at 440 nm and growth calculated as the difference between wells with full medium and wells with depleted medium.
In Vivo
In Vivo GW2580 (dosed orally at 40 mg/kg 0.5 h before the CSF-1-priming dose) blocks the ability of exogenous CSF-1 to increase LPS-induced TNF-α production in mice by 63%. When given to mice before CSF-1 priming, GW2580 completely blocks the ability of CSF-1 to prime the mouse for increased IL-6 production. GW2580 (80 mg/kg p.o.) completely inhibits the growth of CSF-1-dependent M-NFS-60 tumor cells in the peritoneal cavity. GW2580 (80 mg/kg) dosed orally twice a day the week before thioglycolate injection and for the 4-day period after thioglycolate injection, diminishes the accumulation of macrophages in the peritoneal cavity after thioglycolate injection (by 45%). [1] In a 21-day adjuvant arthritis model, GW2580 (50 mg/kg) dosed twice a day from days 0 to 21, 7 to 21, or 14 to 21 inhibits joint connective tissue and bone destruction. [3] Gw2580 (160 mg/kg) induces a more than 2-fold reduction of total CD45+ CD11b+ myeloid cells, CD11b+ F4/80+ TAMs, and CD11b+ Gr-1+ MDSCs in implanted 3LL lung tumor, through inhibiting tumor recruitment of myeloid cells from peripheral blood. GW2580 (80 mg/kg) treatment is able to suppress Vegf-a (by 35%) and Mmp9 (by 70%) expression, as well as tumor vascular density (CD31 staining). Combination therapy with GW2580 and an anti-VEGFR-2 antibody results in synergistic tumor growth reduction. DC101 alone reduces tumor growth by 35%, the combination of DC101 and GW2580 results in an apparent synergistic tumor growth reduction of approximately 70%. [2]
動物実験 動物モデル Mouse myeloid carcinoma xenografts M-NFS-60
投与量 80 mg/kg
投与経路 Orally twice a day

化学情報

分子量 366.41 化学式

C20H22N4O3
CAS No. 870483-87-7 SDF Download GW2580 SDFをダウンロードする
Smiles COC1=CC=C(C=C1)COC2=C(C=C(C=C2)CC3=CN=C(N=C3N)N)OC
保管

In vitro
Batch:

DMSO : 25 mg/mL ( (68.22 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 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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Handling Instructions

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よくある質問（FAQ）

質問1:
How to reconstitute the inhibitor for i.p. injection in mice?

回答
It can be dissolved in 5% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly. When prepare this kind of vehicle, please dissolve the drug in DMSO clearly first, then add PEG and Tween. After they mixed homogeneously, then dilute with water.

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