ホームページ Protein Tyrosine Kinase VEGFR inhibitor - PDGFR inhibitor - c-Kit inhibitor - c-RET inhibitor - Raf inhibitor Regorafenib (BAY-734506) Monohydrate For research use only.

Regorafenib (BAY-734506) Monohydrate

別名：Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate

Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.

Regorafenib (BAY-734506) Monohydrate化学構造

CAS No. 1019206-88-2

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり

代表番号: 045-509-1970|電子メール：sales@selleck.co.jp
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製品安全説明書

現在のバッチを見る： 純度： 99.99%
99.99

Regorafenib (BAY-734506) Monohydrate関連製品

シグナル伝達経路

VEGFR Signaling Pathways

VEGFRシグナル伝達経路

VEGFR阻害剤の選択性比較

阻害剤 Citation VEGFR1 VEGFR2 VEGFR3 VEGFR VEGF その他
Foretinib 93 Met,Tie-2,RON
Cediranib (AZD2171) 67 c-Kit,PDGFRβ,FGFR1
PD173074 123 FGFR1
Dovitinib (TKI-258) 51 FLT3,c-Kit,FGFR1
Linifanib (ABT-869) 33 CSF-1R,FLT3,Kit
Vatalanib (PTK787) 2HCl 52 PDGFRβ,c-Kit,c-Fms
RAF265 (CHIR-265) 23 B-Raf
Motesanib Diphosphate (AMG-706) 12 Kit,RET,PDGFR
Brivanib (BMS-540215) 10 FGFR1
MGCD-265 analog 12 Met,RON,Tie-2
AEE788 (NVP-AEE788) 13 EGFR,HER2/ErbB2,c-Abl
ENMD-2076 9 FLT3,RET,Aurora A
OSI-930 7 CSF-1R,LCK,C-Raf
CYC116 10 Aurora A,Aurora B,FLT3
Ki8751 20 c-Kit,PDGFRα
Telatinib 5 c-Kit,PDGFRα
PP121 5 PDGFR,Hck,mTOR
KRN 633 6 PDGFRα,c-Kit,BTK
SAR131675 31
Apatinib (YN968D1) mesylate 24 RET
BMS-794833 1 Met
Brivanib Alaninate (BMS-582664) 2 FGFR1
Golvatinib (E7050) 8 c-Met
Semaxanib (SU5416) 20
ZM 323881 HCl 18
ZM 306416 13 Src,Abl
R1530 0 FGFR1
Chiauranib 0 c-Kit,CSF-1R,Aurora B
Emvododstat (PTC299) 0 Dihydroorotate dehydrogenase
XL092 0 AXL,MER,MET
Lucitanib (E3810) hydrochloride 1 FGFR1,FGFR2
Ningetinib 0 Axl,c-Met
Ki20227 1 c-Fms,PDGFRβ,c-Kit
Tyrphostin AG1433 0 PDGFRβ
SU14813 2 PDGFRβ,KIT
Sulfatinib 1 CSF1R,FGFR1
CS-2660 (JNJ-38158471) 0 RET,Kit
SU5204 1 HER2
SU5214 0 EGFR
SU5205 0
SU5408 2
Pamufetinib (TAS-115) 0 recombinant MET
ODM-203 0 FGFR3,FGFR1,FGFR2
WHI-P180 0 RET
Altiratinib 2 MET Y1230C,TrkA,TrkC
Motesanib (AMG-706) 11 c-Kit,c-Ret,PDGFR
Fruquintinib 4
Apatinib 26 RET
Cediranib Maleate 14 c-Kit,PDGFRβ,FGFR1
Toceranib phosphate 1 PDGFR
Anlotinib (AL3818) dihydrochloride 41 c-Kit
Sitravatinib (MGCD516) 4 DDR2,EPHA3,Axl
BFH772 0
BAW2881 (NVP-BAW2881) 2 C-Raf-1,B-RAFV599E,c-Abl
SU5402 19 FGFR1,PDGFRβ
Dovitinib (TKI258) Lactate monohydrate 31 FLT3,c-Kit,FGFR1
LY2874455 14 FGFR2,FGFR1,FGFR4
SKLB1002 4
AZD2932 3 PDGFRβ,Flt3,c-Kit
hVEGF-IN-1 0
4SC-203 0
Chebulinic acid 0
Nastorazepide 0
Vorolanib 0 PDGFR
MAZ51 1 RhoA,GSK3β,Akt
SU5208 0
SU5614 3 FLT3,c-Kit,RET
AG-13958 0
SKLB 610 2 FGFR2,PDGFR
SU1498 2
ZD-4190 0 Flt-1
PDGFR inhibitor 1 2 PDGFR,Kit,c-Fms
Taxifolin (Dihydroquercetin) 4
もっと見る
1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
GISTT1 Cytotoxicity assay 72 hrs Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay, GI50=0.13μM 28991465
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=0.38μM 28991465
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=1.35μM 28991465
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生物活性

製品説明 Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively.
Targets
PDGFRβ [1]
(Cell-free)		 RET [1]
(Cell-free)		 Raf-1 [1]
(Cell-free)		 murine VEGFR2 [1]
(Cell-free)		 KIT [1]
(Cell-free)		 もっとクリックする
1.5 nM 2.5 nM 4.2 nM 7 nM
In Vitro
In vitro Regorafenib strongly prevents VEGFR2 autophosphorylation in NIH-3T3/VEGFR2 cells with IC50 of 3 nM. In HAoSMCs, regorafenib suppress 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 h
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℃. 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.
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
NCT03386825 Completed
Colorectal Neoplasms
Bayer
 January 31 2018 --
NCT01959269 Completed
Colorectal Neoplasm
Bayer
 October 31 2013 --

化学情報

分子量 500.83 化学式

C21H15ClF4N4O3.H2O
CAS No. 1019206-88-2 SDF --
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.O
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (199.66 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

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。

技術サポート

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