ホームページ MAPK Raf inhibitor SB590885 For research use only.

SB590885

SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.

SB590885化学構造

CAS No. 405554-55-4

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 33000 国内在庫あり
JPY 25500 国内在庫あり
JPY 100500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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SB590885関連製品

シグナル伝達経路

Raf Signaling Pathways

Rafシグナル伝達経路

Raf阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
white blood cells Antifibrotic assay 25 to 150 mg/kg 13 days Antifibrotic activity in bleomycin-induced C57B1/6 mouse model assessed as inhibition of white blood cells in bronchoalveolar lavage at 25 to 150 mg/kg, po bid administered 2 hrs prior bleomycin induction for 13 days 22222036
insect cells Function assay 30 mins Inhibition of full length human 6His-tagged BRAF V600E mutant expressed in baculovirus infected insect cells co-expressing human CDC37 (1 to 378 residues) using MEK1 as substrate after 30 mins, IC50=0.00016μM 29461827
A549 Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human A549 cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
Colo205 Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human Colo205 cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
HT-29 Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human HT-29 cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
MALME3M Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human MALME3M cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
SKMEL28 Function assay 60 mins Inhibition of B-Raf V600E mutant-mediated Erk phosphorylation in human SKMEL28 cells after 60 mins by Western blot analysis, EC50=0.028μM 22222036
A375 Cytotoxicity assay 48 hrs Cytotoxicity against human A375 cells harboring BRAF V600E mutant after 48 hrs by CellTiter-Glo assay, IC50=0.37μM 29461827
HFF Function assay 60 mins Inhibition of B-Raf-mediated Erk phosphorylation in human HFF cells after 60 mins by Western blot analysis, EC50=1.1μM 22222036
HMEC Function assay 60 mins Inhibition of B-Raf-mediated Erk phosphorylation in human HMEC cells after 60 mins by Western blot analysis, EC50=1.1μM 22222036
PREC Function assay 60 mins Inhibition of B-Raf-mediated Erk phosphorylation in human PREC cells after 60 mins by Western blot analysis, EC50=1.1μM 22222036
HCT116 Growth inhibition assay 72 hrs Growth inhibition of human HCT116 cells expressing wild-type B-Raf and K-Ras2 G13D mutant after 72 hrs by WST-1 assay, EC50=1.1μM 22222036
SK-MEL-2 Growth inhibition assay 72 hrs Growth inhibition of human SK-MEL-2 cells expressing wild-type B-Raf and N-Ras2 Q61R mutant after 72 hrs by WST-1 assay, EC50=1.1μM 22222036
Sf9 Function assay Binding affinity to human N-His6-tagged B-Raf expressed in Sf9 cells, Kd=0.00016μM 22024030
A375 Function assay Inhibition of b-Raf in human A375 cells assessed phosphorylation of ERK, IC50=0.29μM 22808911
A375 Function assay Inhibition of BRAF V600E mutant in human A375 cells assessed as reduction in ERK phosphorylation by immunoblot analysis, IC50=0.29μM 29461827
A375 Antiproliferative assay Antiproliferative activity against human A375 cells expressing B-Raf V600E mutant and wild type Ras, IC50=0.37μM 22808911
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells expressing wild type b-Raf and KRAS mutant, IC50=4.6μM 22808911
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生物活性

製品説明 SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM in a cell-free assay, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
特性 Displays significant selectivity for B-Raf over c-Raf.
Targets
B-Raf [1]
(Cell-free assay)
0.16 nM(Ki)
In Vitro
In vitro SB590885 displays significant selectivity for B-Raf over c-Raf with Ki of 0.16 nM over 1.72 nM. SB-590885 is a more potent inhibitor than the previously described Raf/VEGFR kinase inhibitor BAY 439006 (Ki = 38 nM for mutant B-Raf, 6 nM for c-Raf). SB590885 displays potent selectivity over 46 other kinases. Unlike the multi-kinase inhibitor BAY43-9006, SB590885 stabilizes the oncogenic B-Raf kinase domain in an active configuration. In Colo205, HT29, A375P, SKMEL28, and MALME-3M cells expressing oncogenic B-RafV600E, SB590885 treatment potently inhibits ERK phosphorylation with EC50 of 28 nM, 58 nM, 290 nM, 58 nM, and 190 nM, respectively, and consistently, inhibits the proliferation with EC50 of 0.1 μM, 0.87 μM, 0.37 μM, 0.12 μM, and 0.15 μM, respectively. SB590885 decreases anchorage-independent growth of melanoma cell lines in a BRAF mutant-selective manner. [1] SB590885 displays high affinity for B-Raf with Kd of 0.3 nM. [2] Most of the melanoma cell lines that harbor the BRAF V600E mutation and lack CDK4 mutations (451Lu, WM35, and WM983) are highly sensitive to SB590885 with IC50 of <1 μM. Increased levels of cyclin D1 resulting from genomic amplification mediate SB590885 resistance in B-Raf V600E-mutated melanomas. [3]
細胞実験 細胞株 Colo205, HT29, A375P, SKMEL28, and MALME-3M
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 72 hours
実験の流れ Cells are treated with increasing concentrations of SB590885 and incubated for 72 hours. Viable cells are quantified using CellTiter-Glo reagent and luminescence detection on a Victor 2V plate reader. Cells are prepared for cell cycle analysis on a Becton Dickinson FACScan. Data is acquired and analyzed using CellQuest v3.3 software.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-MEK / MEK / p-ERK / ERK 25879420
In Vivo
In Vivo Administration of SB590885 potently decreases tumorigenesis in murine xenografts established from mutant B-Raf-expressing A375P melanoma cells, and modestly inhibits tumor growth. [1]
動物実験 動物モデル Female nude mice injected s.c. with of A375P cells
投与量 50 mg/kg/day
投与経路 Injection i.p.

化学情報

分子量 453.54 化学式

C27H27N5O2
CAS No. 405554-55-4 SDF Download SB590885 SDFをダウンロードする
Smiles CN(C)CCOC1=CC=C(C=C1)C2=NC(=C(N2)C3=CC=NC=C3)C4=CC5=C(C=C4)C(=NO)CC5
保管

In vitro
Batch:

DMSO : 46 mg/mL ( (101.42 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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