Regorafenib

別名:Fluoro-Sorafenib, BAY 73-4506

Regorafenibは VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) および Raf-1 に対するマルチターゲット阻害剤であり、cell-free assay における IC50 はそれぞれ 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM です。Regorafenib はオートファジーを誘導します。

Regorafenib化学構造

CAS No. 755037-03-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 70500 国内在庫あり
JPY 145500 国内在庫あり
JPY 295500 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

現在のバッチを見る: 純度: 99.91%
99.91

Regorafenib関連製品

シグナル伝達経路

VEGFR阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
Hct-116 Growth Inhibition Assay 1-20 μM 48 h inhibits cell growth in a dose-dependent manner 25071018
HT-29 Growth Inhibition Assay 1-20 μM 48 h inhibits cell growth in a dose-dependent manner 25071018
DLD1 Growth Inhibition Assay 1-20 μM 48 h inhibits cell growth in a dose-dependent manner 25071018
HT15 Growth Inhibition Assay 1-20 μM 48 h inhibits cell growth in a dose-dependent manner 25071018
MDA-MB-231 Function Assay 0.5/5 μM 24 h inhibits the cell migration 25253994
MCF-7 Function Assay 0.5/5 μM 24 h inhibits the cell migration 25253994
RJ348 Function Assay 0.5/5 μM 24 h inhibits the cell migration 25253994
RJ345 Function Assay 0.5/5 μM 24 h inhibits the cell migration 25253994
GEO-CR Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
SW48-CR Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
HCT150 Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
LOVO Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
HCT116 Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
SW620 Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
SW480 Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
HT29 Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
SW48 Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
GEO Growth Inhibition Assay 0.01-20 μM 96 h inhibits cell growth in a dose-dependent manner 25838391
HEK293 Function Assay 0.5 μM 2/4/6 h reduces GRP78 expression 25858032
HepG2  Apoptosis Assay 1–5 μM 48 h inhibits cell growth 26329608
PLC/PRF/5  Apoptosis Assay 1–5 μM 48 h inhibits cell growth 26329608
Hep3B Apoptosis Assay 1–5 μM 48 h inhibits cell growth 26329608
HT15 Apoptosis Assay 1-10 μM 48 h induces cell death in a dose-dependent manner 25071018
DLD1 Apoptosis Assay 1-10 μM 48 h induces cell death in a dose-dependent manner 25071018
HT-29 Apoptosis Assay 1-10 μM 48 h induces cell death in a dose-dependent manner 25071018
Hct-116 Apoptosis Assay 1-10 μM 48 h induces cell death in a dose-dependent manner 25071018
GBM5 Apoptosis Assay 0.5–1.0 μM 24 h interacts with lapatinib to induce cell death 24911215
GBM6 Apoptosis Assay 0.5–1.0 μM 24 h interacts with lapatinib to induce cell death 24911215
GBM12 Apoptosis Assay 0.5–1.0 μM 24 h interacts with lapatinib to induce cell death 24911215
GBM14  Apoptosis Assay 0.5–1.0 μM 24 h interacts with lapatinib to induce cell death 24911215
Hep3B Growth Inhibition Assay 1–2.5 μM 24/48/72 h inhibits cell growth 24885890
PLC/PRF/5  Growth Inhibition Assay 1–2.5 μM 24/48/72 h inhibits cell growth 24885890
HepG2  Growth Inhibition Assay 1–2.5 μM 24/48/72 h inhibits cell growth 24885890
HCT116  Function Assay 10/20/40 μM 24 h induces PUMA protein and mRNA expression in a dose- and time-dependent manner 24763611
Lim2405 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
LoVo Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
Lim1215 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
SW48 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
RKO  Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
SW837 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
SW1463 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
SW480 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
Vaco432 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
Vaco400 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
DLD1 Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
HT29  Function Assay 40 μM 24 h induces PUMA protein and cell apoptosis 24763611
PLC/PRF/5  Growth Inhibition Assay 1–5µM 24/48/72 h inhibits cell growth 23169148
HepG2 Growth Inhibition Assay 1–5µM 24/48/72 h inhibits cell growth 23169148
Hep3B  Growth Inhibition Assay 1–5µM 24/48/72 h inhibits cell growth 23169148
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.021 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of TEL-fused PDGFRbeta (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.029 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant and T670I mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.033 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and A829P mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.047 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and N822K mutant and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.049 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of TEL-fused PDGFRalpha (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.051 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D820A mutant and D820A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.063 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and Y823D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.094 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit V560D mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.108 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of KDR (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.114 μM. 30204441
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.13 μM. 28991465
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.231 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (557 to 558 residues) and D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.29 μM. 30204441
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 0.38 μM. 28991465
BA/F3 Growth inhibition assay 72 hrs Inhibition of PDGFRalpha V561D/D842V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.522 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit V560D/V654A mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.549 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion and D816 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.833 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit V560D/D816H mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.834 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 11 deletion (560 to 578 residues) mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 0.943 μM. 30204441
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit exon 9 AY502 to 503 insertion and V654 mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 1.27 μM. 30204441
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 1.35 μM. 28991465
BA/F3 Growth inhibition assay 72 hrs Inhibition of Kit D816V mutant (unknown origin) transfected in mouse BA/F3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTS assay, GI50 = 2.371 μM. 30204441
GIST430 Cytotoxicity assay 72 hrs Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50 = 3 μM. 28991465
BA/F3 Cytotoxicity assay 72 hrs Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay, GI50 = 9.953 μM. 30204441
HROC46 Growth Inhibition Assay IC50=2.4 μM 25309914
HROC43 Growth Inhibition Assay IC50=5.3 μM 25309914
HROC24 Growth Inhibition Assay IC50=4.6 μM 25309914
HROC18 Growth Inhibition Assay IC50=1.3 μM 25309914
HEK293/OATP1B1 Growth Inhibition Assay IC50=6.2±0.3 nM 25753361
HEK293 Growth Inhibition Assay IC50=11.0±1.2 nM 25753361
LLC-PK1/MRP2 Growth Inhibition Assay IC50=82.4±2.7 nM 25753361
LLC-PK1 Growth Inhibition Assay IC50=42.0±3.2 nM 25753361
KB-G2 Growth Inhibition Assay IC50=9.1±0.1 nM 25753361
KB-31 Growth Inhibition Assay IC50=5.5±0.3 nM 25753361
U-2 OS qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 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
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
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生物活性

製品説明 Regorafenibは VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) および Raf-1 に対するマルチターゲット阻害剤であり、cell-free assay における IC50 はそれぞれ 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM, 2.5 nM です。Regorafenib はオートファジーを誘導します。
Targets
RET [1]
(Cell-free assay)
Raf-1 [1]
(Cell-free assay)
VEGFR2 [1]
(Cell-free assay)
Kit [1]
(Cell-free assay)
VEGFR1 [1]
(Cell-free assay)
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1.5 nM 2.5 nM 4.2 nM 7 nM 13 nM
In Vitro
In vitro

Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppresses PDGFR-β autophosphorylation after stimulation with PDGF-BB, with an IC50 of 90 nM. Regorafenib also inhibits FGFR signaling in MCF-7 breast cancer (BC) cells stimulated with FGF10. Regorafenib very potently inhibited the mutant receptors KITK642E and RETC634W, with IC50 of approximately 20 nM and 10 nM, respectively. Regorafenib inhibits the proliferation of VEGF165-stimulated HUVECs, with an IC50 of approximately 3 nM. Regorafenib prevents the proliferation of FGF2-stimulated HUVECs and of PDGF-BB-stimulated HAoSMCs with IC50 of 127 nM and 146 nM, respectively. [1] Regorafenib targets both tumor cell proliferation and tumor vasculature through inhibition of receptors of tyrosine kinases (VEGFR, KIT, RET, FGFR, and PDGFR) and serine/threonine kinases (Raf and p38MAPK). [2] Regorafenib suppresses growth of human Hep3B, PLC/PRF/5 and HepG2 cells in a concentration- and time-dependent manner. [3]

Kinase Assay Kinase assays
In vitro assays using recombinant VEGFR2 (murine aa785–aa1367), VEGFR3 (murine aa818–aa1363), PDGFRβ (aa561–aa1106), Raf-1 (aa305–aa648) and BRafV600E (aa409–aa765) kinase domains are performed. Initial in vitro kinase inhibition profiling is performed at a fixed 1 μM Regorafenib concentration. Inhibitory concentration of 50% (IC50) values are determined from selected responding kinases, e.g., VEGFR1 and RET. TIE2 kinase inhibition is measured with a homogeneous time-resolved fluorescence (HTRF) assay using a recombinant fusion protein of glutathione-S-transferase, the intracellular domain of TIE2 and the peptide biotin-Ahx-EPKDDAYPLYSDFG as substrate.
細胞実験 細胞株 GIST 882 and TT cells
濃度 5 nM-10 μM
反応時間 96 hours
実験の流れ

For proliferation assays, GIST 882 and TT cells are grown in RPMI medium containing L-glutamine, and MDA-MB-231, HepG2 and A375 cells in DMEM always containing 10% hiFBS. Cells are trypsinized, plated at 5×104 cells/well in 96-well plates in complete media containing 10% FBS and grown overnight at 37 °C. The next day, vehicle or Regorafenib serially diluted in complete growth media to between 10 μM and 5 nM final concentrations, and 0.2% DMSO, is added and incubation is continued for 96 hours. Cell proliferation is quantified.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot PUMA / p53 Bim / Bid / Bak / Bcl-Xl / Mcl-1 p-p65(S536) / p65 p-FGFR2 / p-FRS2α / p-AKT / p-MAPK / p-P90RSK / FGFR2 / AKT / MAPK / p90RSK Cyclin D / Cyclin E / Cyclin A / Cyclin B / p27 / p21 p-STAT3 / STAT3 / PARP / Caspase-9 24763611
Immunofluorescence p65 F-actin / Vimentin / E-cadherin 24763611
Growth inhibition assay GI50 Cell viability 29573334
In Vivo
In Vivo

Regorafenib reveals potent dose-dependent TGI in various preclinical human xenograft models in mice, with tumor shrinkages in breast MDA-MB-231 and renal 786-O carcinoma models. Regorafenib prevents not only the growth of syngeneic primary 4T1 breast tumors growing orthotopically in the fat pad, but also suppresses the formation of tumor metastasis in the lung. [1]

動物実験 動物モデル Female athymic NCr nu/nu mice with Colo-205, MDA-MB-231 or 786-O
投与量 3 mg/kg, 10 mg/kg, 30 mg/kg, 100 mg/kg
投与経路 Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06137170 Not yet recruiting
Metastatic Colorectal Cancer
Bayer
January 22 2024 --
NCT06029010 Completed
Metastatic Colorectal Cancer
Bayer
August 31 2023 --
NCT05370807 Recruiting
Melanoma Stage III|Melanoma Stage IV
Universitair Ziekenhuis Brussel
October 3 2022 Phase 2

化学情報

分子量 482.82 化学式

C21H15ClF4N4O3

CAS No. 755037-03-7 SDF Download Regorafenib SDFをダウンロードする
Smiles CNC(=O)C1=NC=CC(=C1)OC2=CC(=C(C=C2)NC(=O)NC3=CC(=C(C=C3)Cl)C(F)(F)F)F
保管

In vitro
Batch:

DMSO : 97 mg/mL ( (200.9 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。)

Ethanol : 3 mg/mL

Water : 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。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

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よくある質問(FAQ)

質問1:
How to resuspend Regorafenib for in vivo studies?

回答
For in vivo study, we recommend to use 2% DMSO+30% PEG 300+5% Tween 80+ddH2O up to 5mg/ml.

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