ホームページ MAPK Raf inhibitor - PDGFR inhibitor - VEGFR inhibitor - FLT3 inhibitor - c-Kit inhibitor - FGFR inhibitor - Ferroptosis activator - Autophagy activator - Apoptosis related activator Sorafenib tosylate For research use only.

Sorafenib tosylate

別名：BAY 43-9006 tosylate,NSC-724772 tosylate

Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.

Sorafenib tosylate化学構造

CAS No. 475207-59-1

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 52800 国内在庫あり
JPY 22000 国内在庫あり
JPY 100500 国内在庫あり
JPY 239500 国内在庫あり
JPY 598500 国内在庫あり

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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Sorafenib tosylate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
HT-29 Growth Inhibition Assay 48 h GI50=2.5 μM 22560627
EKVX Growth Inhibition Assay 48 h GI50=2.5 μM 22560627
MCF7 Growth Inhibition Assay 48 h GI50=2.5 μM 22560627
UACC257 Growth Inhibition Assay 48 h GI50=2 μM 22560627
MDA-MB-435 Growth Inhibition Assay 48 h GI50=2 μM 22560627
SNB19 Growth Inhibition Assay 48 h GI50=3.2 μM 22560627
OVCAR3 Growth Inhibition Assay 48 h GI50=3.2 μM 22560627
CAKI-1 Growth Inhibition Assay 48 h GI50=3.2 μM 22560627
SW620 Growth Inhibition Assay 48 h GI50=3.2 μM 22560627
TK10 Growth Inhibition Assay 48 h GI50=5 μM 22560627
endothelial precursor cells Function assay Inhibition of endothelial cord area formation in endothelial precursor cells by CD31 cord area detection based phenotypic drug discovery based assay, IC50 = 0.00421 μM. 22409666
Sf9 Function assay Inhibition of GST-tagged recombinant human VEGFR2 expressed in Sf9 cells by radiometric assay, IC50 = 0.0125 μM. 24368209
endothelial precursor cells/ADSC cells Toxicity assay Toxicity in endothelial precursor cells co-cultured with stromal precursor ADSC cells by total nuclei count detection based phenotypic drug discovery based assay, EC50 = 5.46 μM. 22409666
endothelial precursor cells Function assay Inhibition of cell migration in endothelial precursor cells by Oris cell migration kit based phenotypic drug discovery based assay, IC50 = 16.7 μM. 22409666
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
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生物活性

製品説明 Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.
Targets
Raf-1 [1]
(Cell-free assay)		 VEGFR2/Flk1 [1]
(Cell-free assay)		 B-Raf [1]
(Cell-free assay)		 B-Raf (V599E) [1]
(Cell-free assay)		 PDGFRβ [1]
(Cell-free assay)		 もっとクリックする
6 nM 15 nM 22 nM 38 nM 57 nM
In Vitro
In vitro

Sorafenib tosylate inhibits both wild-type and V599E mutant B-Raf activity with IC50 of 22 nM and 38 nM, respectively. Sorafenib tosylate also potently inhibits mVEGFR2 (Flk-1), mVEGFR3, mPDGFRβ, Flt3, and c-Kit with IC50 of 15 nM, 20 nM, 57 nM, 58 nM, and 68 nM, respectively. Sorafenib tosylate weakly inhibits FGFR-1 with IC50 of 580 nM. Sorafenib tosylate is not active against ERK-1, MEK-1, EGFR, HER-2, IGFR-1, c-Met, PKB, PKA, cdk1/cyclinB, PKCα, PKCγ, and pim-1. Sorafenib tosylate markedly inhibits VEGFR2 phosphorylation in NIH 3T3 cells with IC50 of 30 nM, and Flt-3 phosphorylation in HEK-293 cells with IC50 of 20 nM. Sorafenib tosylate potently blocks MEK 1/2 and ERK 1/2 phosphorylation in most cell lines but not in A549 or H460 cells, while having no effect on inhibition of the PKB pathway. Sorafenib tosylate inhibits the proliferation of HAoSMC and MDA-MB-231 cells with IC50 of 0.28 μM and 2.6 μM, respectively. [1] In addition to inhibition of the RAF/MEK/ERK signaling pathway, Sorafenib tosylate significantly inhibits the phosphorylation of eIF4E and down-regulates Mcl-1 levels in hepatocellular carcinoma (HCC) cells in a MEK/ERK-independent manner. Sorafenib tosylate inhibits the proliferation of PLC/PRF/5 and HepG2 cells with IC50 of 6.3 μM and 4.5 μM, respectively, and leads to the significant induction of apoptosis. [2]
Kinase Assay Biochemical assays
Recombinant baculoviruses expressing Raf-1 (residues 305–648) and B-Raf (residues 409–765) are purified as fusion proteins. Full-length human MEK-1 is generated by PCR and purified as a fusion protein from Escherichia coli lysates. Sorafenib tosylate is added to a mixture of Raf-1 (80 ng), or B-Raf (80 ng) with MEK-1 (1 μg) in assay buffer [20 mM Tris (pH 8.2), 100 mM NaCl, 5 mM MgCl2, and 0.15% β-mercaptoethanol] at a final concentration of 1% DMSO. The Raf kinase assay (final volume of 50 μL) is initiated by adding 25 μL of 10 μM γ[33P]ATP (400 Ci/mol) and incubated at 32 °C for 25 minutes. Phosphorylated MEK-1 is harvested by filtration onto a phosphocellulose mat, and 1% phosphoric acid is used to wash away unbound radioactivity. After drying by microwave heating, a β-plate counter is used to quantify filter-bound radioactivity. Human VEGFR2 (KDR) kinase domain is expressed and purified from Sf9 lysates. Time-resolved fluorescence energy transfer assays for VEGFR2 are performed in 96-well opaque plates in the time-resolved fluorescence energy transfer format. Final reaction conditions are as follows: 1 to 10 μM ATP, 25 nM poly GT-biotin, 2 nM Europium-labeled phospho (p)-Tyr antibody (PY20), 10 nM APC, 1 to 7 nM cytoplasmic kinase domain in final concentrations of 1% DMSO, 50 mM HEPES (pH 7.5), 10 mM MgCl2, 0.1 mM EDTA, 0.015% Brij-35, 0.1 mg/mL BSA, and 0.1% β-mercaptoethanol. Reaction volumes are 100 μL and are initiated by addition of enzyme. Plates are read at both 615 and 665 nM on a Perkin-Elmer VictorV Multilabel counter at ~1.5 to 2.0 hours after reaction initiation. Signal is calculated as a ratio: (665 nm/615 nM) × 10,000 for each well. For IC50 generation, Sorafenib tosylate is added before the enzyme initiation. A 50-fold stock plate is made with Sorafenib tosylate serially diluted 1:3 in a 50% DMSO/50% distilled water solution. Final Sorafenib tosylate concentrations range from 10 μM to 4.56 nM in 1% DMSO.
細胞実験 細胞株 MDA-MB-231, and HAoSMC
濃度 Dissolved in DMSO, final concentrations ~10 μM
反応時間 72 hours
実験の流れ

Cells are exposed to increasing concentrations of Sorafenib tosylate for 72 hours. Cell number is quantitated using the Cell TiterGlo ATP Luminescent assay kit. This assay measures the number of viable cells per well by measurement of luminescent signal based on amount of cellular ATP.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot LC3-I / LC-3II / ATG5 p-STAT3 / STAT3/ Mcl-1 β-catenin / Survivin / Mcl-1 / PTMA pERK / ERK p-PKM2(Y105) / PMK2 / Caspase-9 RET(pY1016) / VEGFR2(pY1214) / MEK1(pT292) / ERK(pY204) Cyclin D1 23392173
Immunofluorescence p65 cytochrome c 22286758
Growth inhibition assay Cell viability 26039995
ELISA TGF-beta / CD206 Caspase-9 / Caspase-3 26158762
In Vivo
In Vivo

Oral administration of Sorafenib tosylate (~60 mg/kg) demonstrates broad spectrum, dose-dependent anti-tumor activity against a variety of human tumor xenograft models including MDA-MB-231, Colo-205, HT-29, DLD-1, NCI-H460, and A549, with no evidence of toxicity. In association with the anti-tumor efficacy, Sorafenib tosylatetreatment potently inhibits MEK 1/2 phosphorylation and pERK 1/2 levels in HT-29 and MDA-MB-231 xenografts but not in Colo-205 xenografts, and significantly suppresses tumor microvessel area (MVA) and microvessel density (MVD) in MDA MB-231, HT-29 and Colo-205 tumor xenografts. [1] Sorafenib tosylate treatment produces dose-dependent growth inhibition of PLC/PRF/5 tumor xenografts in SCID mice with TGIs of 49% and 78% at 10 mg/kg and 30 mg/kg, respectively, consistent with the inhibition of ERK and eIF4E phosphorylation, reduction of the microvessel area, and induction of tumor cell apoptosis. [2]
動物実験 動物モデル Female NCr-nu/nu mice implanted s.c. with MDA-MB-231, Colo-205, HT-29, H460, or A549 cells
投与量 ~60 mg/kg
投与経路 Orally once daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05068752 Recruiting
Pancreas Cancer
HonorHealth Research Institute|Bayer|Genentech Inc.
 October 28 2021 Phase 2
NCT04763408 Active not recruiting
Carcinoma Hepatocellular
Eisai Inc.
 April 9 2021 --

化学情報

分子量 637.03 化学式

C21H16ClF3N4O3.C7H8O3S
CAS No. 475207-59-1 SDF Download Sorafenib tosylate SDFをダウンロードする
Smiles CC1=CC=C(C=C1)S(=O)(=O)O.CNC(=O)C1=NC=CC(=C1)OC2=CC=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F
保管

In vitro
Batch:

DMSO : 127 mg/mL ( (199.36 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 : 0.01 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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