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Ki8751

Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.

Ki8751化学構造

CAS No. 228559-41-9

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Ki8751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.

生物活性

製品説明 Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR.
Targets
VEGFR2 [1] c-Kit [1] PDGFRα [1]
0.9 nM 40 nM 67 nM
In Vitro
In vitro Ki8751 potently and selectively inhibits VEGFR2 with IC50 of 0.9 nM. Ki8751 also inhibits PDGFRα, c-Kit, and FGFR-2, with much higher IC50 values (40 nM–170 nM). Except for these several kinases, Ki8751 doesn't disturb other kinases, including HGFR, EGFR, and InsulinR, even at 10 μM. [1] In human umbilical vein endothelial cells (HUVECs), Ki8751 (1 nM–100 nM) effectively decreases VEGF-stimulated cell proliferation and vasculature permeability. [2] In metastatic colorectal cancer (CRC) cells MIP, RKO, SW620, and SW480, but not in HCT116, Ki8751 (10 nM) increases cellular senescence. [3]
Kinase Assay Cellular Kinase Assays
NIH3T3 cells prepared by transfection of human KDR. The cells are cultured in a collagen type I coated 96-well plate in an amount of 1.5 × 104 per well. The medium is then replaced by a DMEM medium containing 0.1% FCS. Ki8751 diluted in DMSO is added to each well and cultured. rhVEGF is added to a final concentration of 100 ng/mL, and the stimulation of cells is carried out at 37 °C. The cells are washed with PBS (pH 7.4), 50 μL of a solubilization buffer (20 mM HEPES (pH 7.4), 150 mM NaCl, 0.2% Triton X-100, 10% glycerol, 5 mM Na3VO4, 5 mM disodium ethylenediamine tetraacetate, and 2 mM Na4P2O7) is then added and a cell extract is prepared. Separately, PBS (50 μL, pH 7.4) containing 5 μg/mL of antiphosphotyrosine antibody (PY20) is added to a microplate for ELISA. After washing of the plate, 300 μL of a blocking solution is added. The cell extract is transferred to the plate. An anti-VEGFR2 antibody and a peroxidase-labeled anti-rabbit Ig antibody are added. Next, a chromophoric substrate for peroxidase is added, and the absorbance at 450 nm is measured with microplate reader. The VEGFR2 phosphorylation activity for each well is determined by presuming the absorbance with the addition of VEGF and without the addition of the test sample to be 100% VEGFR2 phosphorylation activity and VEGF to be 0% VEGFR2 phosphorylation activity. The concentration of the inhibition (%) of VEGFR2 Phosphorylation is determined for each case, and IC50 value is calculated.
細胞実験 細胞株 HUVECs
濃度 1 nM–100 nM
反応時間 1 hour
実験の流れ

To evaluate the inhibition of VEGF-Stimulated HUVEC proliferation by Ki8751, HUVECs are plated at a density of 4000 cells/200 μL/well in a type I collagen pre-coated 96-well plates. After 24 hours, the cells are incubated for 1 hour with Ki8751 and then stimulated with 20 ng/mL rhVEGF. The cultures are incubated at 37 °C for 72 hours, then pulsed with 1 μCi/well [3H]thymidine and re-incubated for 14 hours. Cells are assayed for the incorporation of tritium using a beta counter.
In Vivo
In Vivo In nude mice bearing human tumor xenografts of GL07, St-4, LC6, DLD-1, and A375 cells, Ki8751 (20 mg/kg) inhibits tumor growth. In nude rat xenograft models of LC-6 cells, Ki8751 (5 mg/kg) completely inhibits tumor growth without affecting body weight. [1]

化学情報

分子量 469.41 化学式

C24H18F3N3O4
CAS No. 228559-41-9 SDF Download Ki8751 SDFをダウンロードする
Smiles COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC(=C(C=C3)NC(=O)NC4=C(C=C(C=C4)F)F)F
保管

In vitro
Batch:

DMSO : 53 mg/mL ( (112.9 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。)

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
Clear solution
4%DMSO Corn oil
2.5mg/ml (5.33mM) Taking the 1 mL working solution as an example, add 40 μL of 62.5 mg/ml clear DMSO stock solution to 960 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 

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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