VEGFR2 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S1119 Cabozantinib (BMS-907351)

Cabozantinib (XL184, BMS-907351)是一种有效的VEGFR2抑制剂,在无细胞试验中IC50为0.035 nM,也能有效抑制c-Met、 Ret、 Kit、Flt-1/3/4、Tie2和AXL,IC50分别为1.3 nM,4 nM,4.6 nM,12 nM/11.3 nM/6 nM,14.3 nM 和 7 nM。

Selective VEGFR2/KDR, IC50: 0.035 nM
S4001 Cabozantinib malate (XL184)

Cabozantinib malate (XL184)是Cabozantinib的苹果酸盐,是有效的VEGFR2抑制剂,IC50为0.035 nM,也抑制c-Met, Ret, Kit, Flt-1/3/4, Tie2和AXL,无细胞试验中IC50分别为1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM和7 nM。

Selective VEGFR2/KDR, IC50: 0.035 nM
S1363 Ki8751

Ki8751是一种有效的,选择性的VEGFR2抑制剂,IC50为0.9 nM,作用于VEGFR2比作用于c-Kit, PDGFRα和FGFR-2选择性高40倍以上,对EGFR, HGFR和InsR没有抑制活性。

Selective VEGFR2, IC50: 0.9 nM
S1490 Ponatinib (AP24534)

Ponatinib (AP24534)是一种新型有效的多靶点抑制剂,在无细胞试验中作用于Abl,PDGFRα,VEGFR2,FGFR1和Src,IC50分别为0.37 nM,1.1 nM,1.5 nM,2.2 nM和5.4 nM。

Selective VEGFR2, IC50: 1.5 nM
S6870 Ningetinib

Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity.

Selective VEGFR2, IC50: 1.9 nM
S2896 ZM 323881 HCl

ZM 323881 HCl是一种有效的,选择性的VEGFR2抑制剂,IC50为<2 nM,对VEGFR1, PDGFRβ, FGFR1, EGFR和ErbB2几乎没有活性。

Selective VEGFR2, IC50: <2 nM
S8188 BFH772

BFH772是一种新型的、有效的、可口服的VEGFR2抑制剂,IC50为3 nM。

Selective VEGFR2, IC50: 3 nM
S5272 Toceranib phosphate

Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively.

Selective Flk-1/DFR, Ki: 6 nM
S7057 LY2874455

LY2874455是一个泛FGFR的抑制剂,对FGFR1,FGFR2, FGFR3, 和FGFR4的IC50值分别为2.8 nM, 2.6 nM, 6.4 nM,以及6 nM。并且也能抑制VEGFR2的活性,IC50为7 nM。Phase 1。

Selective VEGFR2, IC50: 7 nM
S7003 AZD2932

AZD2932 是一种有效的多靶点蛋白酪氨酸激酶抑制剂,对VEGFR-2PDGFRβFlt-3,和 c-KitIC50 分别为 8 nM,4 nM,7 nM,和 9 nM。

Selective VEGFR-2, IC50: 8 nM
S6412 Altiratinib

Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.

Selective VEGFR2, IC50: 9.2 nM
S7688 Ki20227

Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively.

Selective VEGFR2, IC50: 12 nM
S2622 PP121

PP121是一种作用于PDGFR, Hck, mTORVEGFR2SrcAbl的多靶点抑制剂,IC50分别为2 nM, 8 nM, 10 nM, 12 nM, 14 nM和18 nM,也抑制DNA-PKIC50为60 nM。

Selective VEGFR2, IC50: 12 nM
S1040 Sorafenib (BAY 43-9006) tosylate

Sorafenib Tosylate是一种酪氨酸激酶(VEGFR和PDGFR)RAF/MEK/ERK级联抑制剂,同时作用于Raf-1,wtBRAF和V599EBRAF,IC50分别为6 nM, 22 nM和38 nM。

Selective VEGFR2/Flk1, IC50: 15 nM; VEGFR2, IC50: 90 nM
S2201 BMS-794833

BMS-794833是一种有效的,ATP竞争性Met/VEGFR2抑制剂,IC50为1.7 nM/15 nM,也抑制Ron, Axl和Flt3,IC50低于3 nM;是BMS-817378的前体药物。 Phase 1。

Selective VEGFR2, IC50: 15 nM
S2859 Golvatinib (E7050)

Golvatinib (E7050)是c-MetVEGFR-2双重抑制剂,IC50分别为14 nM和16 nM,不抑制bFGF刺激的HUVEC生长(浓度高达1000 nM)。Phase 1/2。

Selective VEGFR2, IC50: 16 nM
S8696 2-D08

2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. It is also inhibits Axl, IRAK4, ROS1, MLK4, GSK3β, RET (c-RET), KDR and PI3Kα with IC50 values of 0.49, 3.9, 5.3, 9.8, 11, 11, 17 and 35 nM respectively in biochemical assays.

Selective KDR, IC50: 17 nM
S7667 SU5402

SU5402是一种有效的多靶点受体激酶抑制剂,对VEGFR2,FGFR1,和PDGF-Rβ的IC50分别为20 nM,30 nM,和510 nM。

Selective VEGFR2, IC50: 20 nM
S2161 RAF265 (CHIR-265)

RAF265 (CHIR-265)是一种有效的选择性C-Raf/B-Raf/B-Raf V600E抑制剂,IC50为3-60 nM,对VEGFR2磷酸化表现出有效的抑制作用,无细胞试验中EC50为30 nM。Phase 2。

Selective VEGFR2, EC50: 30 nM
S7258 SKLB1002

SKLB1002 是一种与ATP竞争的强效VEGFR2抑制剂,其IC50为32 nM.

Selective VEGFR2, IC50: 32 nM
S0377 CS-2660 (JNJ-38158471)

CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM.

Selective VEGFR2, IC50: 40 nM
S1171 CYC116

CYC116是一种有效的Aurora A/B抑制剂,Ki为8.0 nM/9.2 nM,对VEGFR2(Ki为44 nM)作用稍弱,比作用于CDKs效果强50倍,对PKA, Akt/PKB, PKC没有活性,对GSK-3α/β, CK2, Plk1和SAPK2A.没有抑制效果。Phase 1。

Selective VEGFR2, Ki: 44 nM
S6520 WHI-P180

WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively.

Selective KDR, IC50: 66 nM
S6514 SU5408

SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM.

Selective VEGFR2, IC50: 70 nM
S7781 Sunitinib (SU11248)

Sunitinib 是一种多靶点 RTK 抑制剂,以VEGFR2(Flk-1)和PDGFRβ为靶点,IC50为80 nM 和 2 nM,对c-Kit也有抑制作用。

Selective VEGFR2 , IC50: 80 nM
S1042 Sunitinib (SU11248) malate

Sunitinib Malate是一种多靶点RTK抑制剂,作用于VEGFR2 (Flk-1)PDGFRβ,在无细胞试验中IC50分别为80 nM 和2 nM,也会抑制c-Kit的活性。

Selective VEGFR2, IC50: 80 nM
S1264 PD173074

PD173074是一种有效的FGFR1抑制剂,在无细胞试验中IC50约为25 nM,也能抑制VEGFR2,IC50为100-200 nM,作用于FGFR1比作用于PDGFR和c-Src选择性高1000倍左右。

Selective VEGFR2, IC50: 100 nM-200 nM
S2845 Semaxanib (SU5416)

Semaxanib (SU5416)是一种有效的,选择性的VEGFR(Flk-1/KDR)抑制剂,IC50为1.23 μM,作用于VEGFR比作用于PDGFRβ选择性高20倍,对EGFR, InsR和FGFR没有作用活性。Phase 3。

Selective VEGFR2/Flk1, IC50: 1.23 μM
S0290 SU5204

SU5204 is a bioactive compound.

Selective VEGFR-2, IC50: 4 μM
S6808 SU5205

SU5205 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 9.6 µM.

Selective VEGFR2, IC50: 9.6 μM
S6809 SU5214

SU5214 is a inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively.

Selective VEGFR2, IC50: 14.8 μM
S8721 PDGFR inhibitor 1

PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth.

Selective
S0278 SU5614

SU5614 is a potent and selective inhibitor of FLT3 that induces growth arrest, apoptosis, and cell cycle arrest in Ba/F3 and AML cell lines expressing a constitutively activated FLT3.

Selective
S2366 Taxifolin (Dihydroquercetin)

Taxifolin(Dihydroquercetin)是一种二氢黄酮醇类,是一种黄酮类化合物。是I型VEGFR2 kinase的抑制剂。

Selective
S6535 SU1498

SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells.

Selective
S6543 ZD-4190

ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively.

Selective
S8401 Erdafitinib (JNJ-42756493)

Erdafitinib (JNJ-42756493)是有效的、具有选择性和口服生物活性的泛成纤维细胞生长因子受体FGFR抑制剂,具有潜在的抗肿瘤活性。

Selective
S6526 SKLB 610

SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR.

Selective
S1005 Axitinib (AG 013736)

Axitinib是一种多靶点抑制剂,作用于 VEGFR1VEGFR2VEGFR3,PDGFRβ和c-Kit,在猪主动脉内皮细胞中IC50分别为0.1 nM,0.2 nM,0.1-0.3 nM,1.6 nM和1.7 nM。

Pan VEGFR2/Flk1, IC50: 0.18 nM; VEGFR2/KDR, IC50: 0.2 nM
S8726 Anlotinib (AL3818) dihydrochloride

Anlotinib (AL3818) is a highly potent and selective VEGFR2 inhibitor with IC50 less than 1 nM. It has broad-spectrum antitumor potential in clinical trials. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation.

Pan VEGFR2, IC50: 0.2 nM
S1017 Cediranib (AZD2171)

Cediranib (AZD2171)是一种高效的VEGFR(KDR)抑制剂,IC50为<1 nM,同时也抑制Flt1/4,IC50为5 nM/≤3 nM,此外对c-Kit和PDGFRβ也具有相似的抑制活性,对VEGFR的选择性比PDGFR-α, CSF-1R和Flt3分别高36倍, 110倍 和1000倍以上。Phase 3。

Pan VEGFR2/KDR, IC50: 0.5 nM
S5242 Cediranib Maleate

Cediranib Maleate (AZD-2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.

Pan VEGFR2/KDR, IC50: 0.5 nM
S1111 Foretinib (GSK1363089)

Foretinib (GSK1363089)是一种ATP竞争性的HGFR和VEGFR抑制剂,对MetKDR作用最强,在无细胞试验中IC50分别为0.4 nM和0.9 nM。对Ron, Flt-1/3/4, Kit, PDGFRα/β和Tie-2作用效果稍弱,对FGFR1和EGFR几乎没有抑制活性。Phase 2。

Pan KDR, IC50: 0.86 nM
S1032 Motesanib Diphosphate (AMG-706)

Motesanib Diphosphate (AMG-706)是一种有效的ATP竞争性的VEGFR1/2/3抑制剂,IC50分别为2 nM/3 nM/6 nM;对Kit具有相似的抑制活性,对VEGFR选择性比PDGFR和Ret高10倍。Phase 3。

Pan VEGFR2/Flk1, IC50: 6 nM; VEGFR2, IC50: 3 nM
S1361 MGCD-265 analog

Glesatinib (MGCD265)是一种有效的,多靶点,及ATP竞争性的c-MetVEGFR1/2/3抑制剂,IC50分别为1 nM, 3 nM/3 nM/4 nM,也抑制Ron和Tie2。Phase 1/2。

Pan VEGFR2, IC50: 3 nM
S5793 Motesanib (AMG-706)

Motesanib (AMG-706) is an orally bioavailable receptor tyrosine kinase inhibitor with IC50 values of 2 nM, 3 nM, 6 nM, 8 nM, 84 nM, 59 nM for VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR and Ret, respectively.

Pan VEGFR2, IC50: 3 nM
S5240 Lenvatinib (E7080) Mesylate

Lenvatinib Mesylate (E7080) is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity.

Pan VEGFR2, IC50: 4.0 nM
S1164 Lenvatinib (E7080)

Lenvatinib (E7080)是一种多靶点抑制剂,无细胞试验中,作用于VEGFR2(KDR)/VEGFR3(Flt-4)最有效,IC50为4 nM/5.2,对VEGFR1/Flt-1作用效果稍弱,作用于VEGFR2/3比作用于FGFR1, PDGFRα/β选择性高10倍左右。Phase 3。

Pan VEGFR2/KDR, IC50: 4.0 nM
S1003 Linifanib (ABT-869)

Linifanib (ABT-869)是一种新型有效的ATP竞争性VEGFR/PDGFR抑制剂,作用于KDRCSF-1RFlt-1/3和PDGFRβ,其IC50分别为4 nM,3 nM,3 nM/4 nM和66 nM,对突变激酶依赖性癌细胞(即FLT3)最有效。Phase 3。

Pan VEGFR2/KDR, IC50: 4 nM
S1178 Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506)是一个多靶点抑制剂,作用于VEGFR1,VEGFR2,VEGFR3,PDGFR-β,Kit,RETRaf-1,在无细胞试验中IC50分别是13 nM,4.2 nM,46 nM,22 nM,7 nM,1.5 nM和2.5 nM。

Pan VEGFR2, IC50: 4.2 nM
S4947 Regorafenib Hydrochloride

Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively.

Pan Murine VEGFR2, IC50: 4.2 nM
S5077 Regorafenib (BAY-734506) 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.

Pan murine VEGFR2, IC50: 4.2 nM
S8573 Sitravatinib (MGCD516)

Sitravatinib (MGCD516)是一种新型的、靶向多种参与调节S180肉瘤细胞生长的RTKs的小分子抑制剂,包括c-Kit, PDGFRβ, PDGFRα, c-Met和Axl。

Pan VEGFR2 (KDR), IC50: 5 nM
S2231 Telatinib

Telatinib是一种有效的VEGFR2/3c-Kit和PDGFRα抑制剂,IC50分别为6 nM/4 nM, 1 nM和15 nM。Phase 2。

Pan VEGFR2, IC50: 6 nM
S1207 Tivozanib (AV-951)

Tivozanib (AV-951)是一种有效的,选择性VEGFR抑制剂,作用于VEGFR1/2/3时,IC50分别为0.21 nM/0.16 nM/0.24 nM,也抑制PDGFR和c-Kit,作用于FGFR-1, Flt3, c-Met EGFR和IGF-1R活性较弱。Phase 3。

Pan VEGFR2, IC50: 6.5 nM
S1220 OSI-930

OSI-930是一种有效的KitKDRCSF-1R抑制剂,IC50分别为80 nM, 9 nM和15 nM,对Flt-1, c-Raf和Lck具有适度的抑制活性,对PDGFRα/β, Flt-3和Abl抑制活性较弱。Phase 1。

Pan KDR, IC50: 9 nM
S8189 BAW2881 (NVP-BAW2881)

BAW2881 (NVP-BAW2881)是一种新型的VEGFR酪氨酸激酶抑制剂。在1.0-4.3 nM浓度下能有效地抑制VEGFR1-3;在45-72 nM的浓度下,抑制PDGFRβ, c-Kit和RET。

Pan mVEGF2, IC50: 165 nM; hVEGFR2, IC50: 9 nM
S8882 ODM-203

ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively.

Pan VEGFR2, IC50: 9 nM
S1018 Dovitinib (TKI-258)

Dovitinib (TKI-258, CHIR-258)是一种多靶点的RTK抑制剂,在无细胞试验中对III型(FLT3/c-Kit)作用最强,IC50为1 nM/2 nM,同时也作用于IV类(FGFR1/3)和V类(VEGFR1-4) RTKs,IC50为8-13 nM,但对InsR,EGFR,c-Met,EphA2,Tie2,IGF-1R和HER2作用较弱。Phase 4。

Pan VEGFR2/Flk1, IC50: 13 nM
S1010 Nintedanib (BIBF 1120)

Nintedanib (BIBF 1120)是一种有效的三重血管激酶抑制剂,作用于VEGFR1/2/3FGFR1/2/3PDGFRα/β,在无细胞试验中IC50分别为34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM和59 nM/65 nM。Phase 3。

Pan VEGFR2, IC50: 13 nM
S5234 Nintedanib Ethanesulfonate Salt

Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively.

Pan VEGFR2, IC50: 13 nM
S7765 Dovitinib (TKI258) Lactate

Dovitinib (TKI258) Lactate是Dovitinib的乳酸盐,Dovitinib是一种多靶点的PTK抑制剂,主要对第III类(FLT3/c-Kit)发挥作用,IC50为1 nM/2 nM,对第IV 类(FGFR1/3)和第V 类(VEGFR1-4) RTKs也有效,IC50为8-13 nM,对InsR,EGFR,c-Met,EphA2,Tie2,IGFR1 和HER2作用较差。Phase 4。

Pan VEGFR2/Flk1, IC50: 13 nM
S9621 Donafenib (Sorafenib D3)

Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively.

Pan mVEGFR-2, IC50: 15 nM
S0487 Sulfatinib

Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1/2/3, FGFR1 and CSF1R with IC50 of ranging between 1 and 24 nM.

Pan VEGFR2, IC50: 24 nM
S1084 Brivanib (BMS-540215)

Brivanib (BMS-540215)是一种ATP竞争性的VEGFR2抑制剂,IC50为25 nM,对VEGFR-1和FGFR-1抑制作用适中,但比作用于PDGFR-β效果强240多倍。Phase 3。

Pan Flk1, IC50: 89 nM; VEGFR2, IC50: 25 nM
S1138 Brivanib Alaninate (BMS-582664)

Brivanib Alaninate (BMS-582664)是BMS-540215的前体药物,是一种ATP竞争性的VEGFR2抑制剂,IC50为25 nM。

Pan Flk1, IC50: 89 nM; VEGFR2, IC50: 25 nM
S1035 Pazopanib HCl (GW786034 HCl)

Pazopanib HCl (GW786034 HCl)是一种新型多靶点抑制剂,作用于VEGFR1VEGFR2VEGFR3,PDGFR,FGFR,c-Kit和c-fms,在无细胞试验中IC50分别是10 nM,30 nM,47 nM,84 nM,74 nM,140 nM和146 nM。

Pan VEGFR2, IC50: 30 nM
S3012 Pazopanib

Pazopanib是一种新型多靶点的VEGFR1VEGFR2VEGFR3,PDGFR,FGFR,c-Kit 和 c-Fms抑制剂,无细胞试验中IC50分别为10 nM,30 nM,47 nM,84 nM,74 nM,140 nM 和 146 nM。

Pan VEGFR2, IC50: 30 nM
S5667 Fruquintinib (HMPL-013)

Fruquintinib (HMPL-013) is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases.

Pan VEGFR2, IC50: 35 nM
S1101 Vatalanib (PTK787) 2HCl

Vatalanib (PTK787) 2HCl是一种VEGFR2/KDR抑制剂,无细胞试验中IC50为37 nM,对VEGFR1/Flt-1作用稍弱,是VEGFR3/Flt-4抑制作用的18倍。Phase 3。

Pan VEGFR2/Flk1, IC50: 270 nM; VEGFR2/KDR, IC50: 37 nM
S1046 Vandetanib (ZD6474)

Vandetanib (ZD6474)是一种有效的VEGFR2抑制剂,在无细胞试验中IC50为40 nM。同时,也抑制VEGFR3EGFR,IC50分别为110 nM 和500 nM。对PDGFRβ, Flt-1, Tie-2 和FGFR1作用效果不大,IC50为 1.1-3.6 μM, 对MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt 和 IGF-1R几乎没有作用效果,IC50>10 μM。

Pan VEGFR2, IC50: 40 nM
S0504 SU14813

SU14813 is a multi-targeted receptor tyrosine kinases inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and KIT.

Pan VEGFR2, IC50: 50 nM
S1181 ENMD-2076

ENMD-2076选择性作用于Aurora AVEGFR(Flt3)IC50分别为14 nM和1.86 nM,作用于Aurora A比作用于Aurora B选择性高25倍,对VEGFR2/KDR和VEGFR3, FGFR1和FGFR2和PDGFRα作用效果稍弱。Phase 2。

Pan VEGFR2/KDR, IC50: 58.2 nM
S2018 ENMD-2076 L-(+)-Tartaric acid

ENMD-2076 L-(+)-Tartaric acid 是ENMD-2076的酒石酸,选择性作用于Aurora AVEGFR(Flt3)IC50分别为14 nM和1.86 nM,作用于Aurora A比作用于Aurora B选择性高25倍,对VEGFR2/KDR和VEGFR3, FGFR1和FGFR2和PDGFRα作用效果稍弱。Phase 2。

Pan VEGFR2/KDR, IC50: 58.2 nM
S1486 AEE788 (NVP-AEE788)

AEE788 (NVP-AEE788)是一种有效的EGFRHER2/ErbB2抑制剂,IC50分别为2 nM和6 nM,对VEGFR2/KDR, c-Abl, c-Src,和Flt-1作用效果稍弱,对Ins-R, IGF-1R, PKCα和CDK1没有抑制作用。Phase 1/2。

Pan KDR, IC50: 77 nM
S7397 Sorafenib (BAY 43-9006)

Sorafenib是Raf-1, B-Raf和VEGFR-2的多重激酶抑制剂,无细胞试验中IC50分别为6 nM, 22 nM和90 nM。

Pan VEGFR2, IC50: 90 nM
S1557 KRN 633

KRN 633是一种ATP竞争性的VEGFR1/2/3抑制剂,IC50为170 nM/160 nM/125 nM,微弱抑制PDGFR-α/β和c-Kit,对细胞中FGFR-1, EGFR和c-Met的磷酸化没有抑制作用。

Pan VEGFR2, IC50: 160 nM