VEGFR1 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
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.

Selective VEGFR1, IC50: 2 nM
S2897 ZM 306416

ZM 306416是一种VEGFR(Flt和KDR)抑制剂,作用于VEGFR1IC50为0.33 μM,也抑制EGFR,IC50为<10 nM。

Selective VEGFR1, IC50: 0.33 μM
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 VEGFR1/FLT1, IC50: 0.1 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 VEGFR1, IC50: 2 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 VEGFR1, IC50: 2 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 VEGFR1, IC50: 2 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 VEGFR1, IC50: 3 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 VEGFR1/FLT1, IC50: 3 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 VEGFR1/FLT1, IC50: 5 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 VEGFR1/FLT1, IC50: 5 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 VEGFR1 (FLT1), IC50: 6 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 VEGFR1/FLT1, IC50: 6.8 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 FLT1, IC50: 8 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 VEGFR1/FLT1, IC50: 10 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 VEGFR1, IC50: 10 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 VEGFR1/FLT1, IC50: 10 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 VEGFR1, IC50: 10 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 VEGFR1, IC50: 13 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 VEGFR1, IC50: 13 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 VEGFR1, IC50: 13 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 VEGFR1/FLT1, IC50: 22 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 VEGFR1, IC50: 22 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 VEGFR1, IC50: 26 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 VEGFR1, 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 VEGFR1, IC50: 33 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 VEGFR1, IC50: 34 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 VEGFR1, IC50: 34 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 FLT1, IC50: 59 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 VEGFR1/FLT1, IC50: 77 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 VEGFR1, IC50: 170 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 VEGFR1, IC50: 380 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 VEGFR1, IC50: 380 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 hVEGFR1, IC50: 820 nM