VEGFR

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Isoform-specific Inhibitors

VEGFR Products

Catalog No. Information Product Use Citations Product Validations
A2003New

Ramucirumab (anti-VEGFR2)

Ramucirumab is a monoclonal antibody of the IgG1 class that binds to VEGF-R2 and prevents its activation. The IC50 value for blocking KDR binding to VEGF is 0.8 nM for ramucirumab, MW: 143.6 KD.

A2006

Bevacizumab (anti-VEGF)

Bevacizumab (anti-VEGF, Avastin) is a humanized anti-VEGF monoclonal antibody which binds to and neutralizes all human VEGF-A isoforms and bioactive proteolytic fragments, MW:149 KD.

S1040

Sorafenib Tosylate

Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.

S1042

Sunitinib Malate

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

S1029

Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.

S1119

Cabozantinib (BMS-907351)

Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.

S1490

Ponatinib (AP24534)

Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.

S6870New

Ningetinib

Ningetinib 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.

S9621New

Donafenib (Sorafenib D3)

Sorafenib D3 (Bay 43-9006 D3) 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.

S7688New

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.

S6843New

X-82 (Vorolanib)

Vorolanib is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities.

S0487New

Sulfatinib

Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.

S0377New

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) also inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.

S0278New

SU5614

SU5416 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5416 also inhibits RET with IC50 of 170 nM. SU5416 reduces cell proliferation and induces apoptosis.

S6808New

SU5205

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

S6809New

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.

S6514New

SU5408

SU5408 is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM.

S6763New

Acrizanib (LHA510)

Acrizanib is an inhibitor of VEGFR-2 with IC50 of 17.4 nM in BaF3-Tel-KDR cells.

S6764New

TAS-115

TAS-115 is a unique VEGFR/MET-targeted inhibitor with IC50 of 30nM and 32nM for rVEGFR2 and rMET, respectively.

S2211New

AG-13958

AG–013958, a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD).

S8882New

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.

S1005

Axitinib

Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

S1111

Foretinib (GSK1363089)

Foretinib (GSK1363089, EXEL-2880, XL-880) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.

S1046

Vandetanib (ZD6474)

Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).

S1010

Nintedanib (BIBF 1120)

Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

S1178

Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506, Fluoro-Sorafenib) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, 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 in cell-free assays, respectively. Regorafenib induces autophagy.

S1035

Pazopanib HCl (GW786034 HCl)

Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.

S1017

Cediranib (AZD2171)

Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.

S1264

PD173074

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.

S1018

Dovitinib (TKI-258)

Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.

S1003

Linifanib (ABT-869)

Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.

S1101

Vatalanib (PTK787) 2HCl

Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.

S2161

RAF265 (CHIR-265)

RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.

S1207

Tivozanib (AV-951)

Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3.

S1032

Motesanib Diphosphate (AMG-706)

Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.

S1164

Lenvatinib (E7080)

Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, KIT, RET, and shows potent antitumor activities. Phase 3.

S1084

Brivanib (BMS-540215)

Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.

S1361

MGCD-265 analog

MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.

S1486

AEE788 (NVP-AEE788)

AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.

S1181

ENMD-2076

ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.

S1220

OSI-930

OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.

S1171

CYC116

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.

S1363

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.

S2231

Telatinib

Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.

S2622

PP121

PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.

S3012

Pazopanib

Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.

S1557

KRN 633

KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.

S2842

SAR131675

SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.

S2201

BMS-794833

BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.

S7397

Sorafenib

Sorafenib (BAY 43-9006) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.

S4001

Cabozantinib malate (XL184)

Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.

S1138

Brivanib Alaninate (BMS-582664)

Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.

S2859

Golvatinib (E7050)

Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.

S2845

Semaxanib (SU5416)

Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3.

S2897

ZM 306416

ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.

S2896

ZM 323881 HCl

ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.

S2018

ENMD-2076 L-(+)-Tartaric acid

ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.

S7057

LY2874455

LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.

S8189

BAW2881 (NVP-BAW2881)

BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET at 45-72 nM concentrations.

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 and kinase insert domain receptor (KDR), respectively.

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.

S6535

SU1498

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

S7667

SU5402

SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.

S8721

PDGFR inhibitor 1

PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of 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.

S7765

Dovitinib (TKI258) Lactate

Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

S5272

Toceranib phosphate

Toceranib phosphate, 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.

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.

S8188

BFH772

BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.

S5240

lenvatinib Mesylate

Lenvatinib Mesylate 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), and rearranged during transfection (RET). Lenvatinib Mesylate has potential antineoplastic activity.

S5667

Fruquintinib (HMPL-013)

Fruquintinib 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.

S8401

Erdafitinib (JNJ-42756493)

Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET, CSF-1R, PDGFR-α/PDGFR-β, FLT4, KIT and VEGFR-2 and induces cellular apoptosis.

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.

S7781

Sunitinib

Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.

S8573

Sitravatinib (MGCD516)

Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.

S7258

SKLB1002

SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 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.

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, 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.

S6412

Altiratinib

Altiratinib is a potent single-digit nanomolar inhibitor of TRK, 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 and MET mutant with IC50 values in the range of 0.3-6 nM.

S4686

Vitamin E

Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.

S7847

SGI-7079

SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.

S7003

AZD2932

AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.

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.

S5234

Nintedanib Ethanesulfonate Salt

Nintedanib 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.

S5077

Regorafenib Monohydrate

Regorafenib 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, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

S2366

Taxifolin (Dihydroquercetin)

Taxifolin, type I inhibitor for VEGFR-2 kinase, is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.

S2431New

TMTD (Tetramethylthiuram disulfide)

TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.

S9190

Oroxin B

Oroxin B, one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment.

Catalog No. Information Product Use Citations Product Validations
A2003New

Ramucirumab (anti-VEGFR2)

Ramucirumab is a monoclonal antibody of the IgG1 class that binds to VEGF-R2 and prevents its activation. The IC50 value for blocking KDR binding to VEGF is 0.8 nM for ramucirumab, MW: 143.6 KD.

A2006

Bevacizumab (anti-VEGF)

Bevacizumab (anti-VEGF, Avastin) is a humanized anti-VEGF monoclonal antibody which binds to and neutralizes all human VEGF-A isoforms and bioactive proteolytic fragments, MW:149 KD.

S1040

Sorafenib Tosylate

Sorafenib Tosylate (Bay 43-9006) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.

S1042

Sunitinib Malate

Sunitinib Malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis.

S1029

Lenalidomide (CC-5013)

Lenalidomide (CC-5013) is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis.

S1119

Cabozantinib (BMS-907351)

Cabozantinib (XL184, BMS-907351) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.

S1490

Ponatinib (AP24534)

Ponatinib (AP24534) is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy.

S6870New

Ningetinib

Ningetinib 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.

S9621New

Donafenib (Sorafenib D3)

Sorafenib D3 (Bay 43-9006 D3) 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.

S7688New

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.

S6843New

X-82 (Vorolanib)

Vorolanib is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities.

S0487New

Sulfatinib

Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs.

S0377New

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) also inhibits closely related tyrosine kinases such as Ret and Kit with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3.

S0278New

SU5614

SU5416 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5416 also inhibits RET with IC50 of 170 nM. SU5416 reduces cell proliferation and induces apoptosis.

S6808New

SU5205

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

S6809New

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.

S6514New

SU5408

SU5408 is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM.

S6763New

Acrizanib (LHA510)

Acrizanib is an inhibitor of VEGFR-2 with IC50 of 17.4 nM in BaF3-Tel-KDR cells.

S6764New

TAS-115

TAS-115 is a unique VEGFR/MET-targeted inhibitor with IC50 of 30nM and 32nM for rVEGFR2 and rMET, respectively.

S2211New

AG-13958

AG–013958, a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD).

S8882New

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.

S1005

Axitinib

Axitinib (AG 013736) is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively.

S1111

Foretinib (GSK1363089)

Foretinib (GSK1363089, EXEL-2880, XL-880) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2.

S1046

Vandetanib (ZD6474)

Vandetanib (ZD6474) is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS).

S1010

Nintedanib (BIBF 1120)

Nintedanib (BIBF 1120, Intedanib, Vargatef, Ofev) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3.

S1178

Regorafenib (BAY 73-4506)

Regorafenib (BAY 73-4506, Fluoro-Sorafenib) is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit, 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 in cell-free assays, respectively. Regorafenib induces autophagy.

S1035

Pazopanib HCl (GW786034 HCl)

Pazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death.

S1017

Cediranib (AZD2171)

Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.

S1264

PD173074

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.

S1018

Dovitinib (TKI-258)

Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4.

S1003

Linifanib (ABT-869)

Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3.

S1101

Vatalanib (PTK787) 2HCl

Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3.

S2161

RAF265 (CHIR-265)

RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2.

S1207

Tivozanib (AV-951)

Tivozanib (AV-951, KRN-951) is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3.

S1032

Motesanib Diphosphate (AMG-706)

Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit, ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3.

S1164

Lenvatinib (E7080)

Lenvatinib (E7080) is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, KIT, RET, and shows potent antitumor activities. Phase 3.

S1084

Brivanib (BMS-540215)

Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3.

S1361

MGCD-265 analog

MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2.

S1486

AEE788 (NVP-AEE788)

AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.

S1181

ENMD-2076

ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2.

S1220

OSI-930

OSI-930 is a potent inhibitor of Kit, KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1.

S1171

CYC116

CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1.

S1363

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.

S2231

Telatinib

Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2.

S2622

PP121

PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM.

S3012

Pazopanib

Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy.

S1557

KRN 633

KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell.

S2842

SAR131675

SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc.

S2201

BMS-794833

BMS-794833 is a potent ATP competitive inhibitor of Met/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1.

S7397

Sorafenib

Sorafenib (BAY 43-9006) is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity.

S4001

Cabozantinib malate (XL184)

Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis.

S1138

Brivanib Alaninate (BMS-582664)

Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM.

S2859

Golvatinib (E7050)

Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.

S2845

Semaxanib (SU5416)

Semaxanib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3.

S2897

ZM 306416

ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM.

S2896

ZM 323881 HCl

ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2.

S2018

ENMD-2076 L-(+)-Tartaric acid

ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2.

S7057

LY2874455

LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.

S8189

BAW2881 (NVP-BAW2881)

BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET at 45-72 nM concentrations.

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 and kinase insert domain receptor (KDR), respectively.

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.

S6535

SU1498

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

S7667

SU5402

SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.

S8721

PDGFR inhibitor 1

PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of 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.

S7765

Dovitinib (TKI258) Lactate

Dovitinib (TKI258) Lactate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.

S5272

Toceranib phosphate

Toceranib phosphate, 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.

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.

S8188

BFH772

BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.

S5240

lenvatinib Mesylate

Lenvatinib Mesylate 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), and rearranged during transfection (RET). Lenvatinib Mesylate has potential antineoplastic activity.

S5667

Fruquintinib (HMPL-013)

Fruquintinib 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.

S8401

Erdafitinib (JNJ-42756493)

Erdafitinib (JNJ-42756493) is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET, CSF-1R, PDGFR-α/PDGFR-β, FLT4, KIT and VEGFR-2 and induces cellular apoptosis.

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.

S7781

Sunitinib

Sunitinib (SU11248) is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis.

S8573

Sitravatinib (MGCD516)

Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl.

S7258

SKLB1002

SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 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.

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, 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.

S6412

Altiratinib

Altiratinib is a potent single-digit nanomolar inhibitor of TRK, 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 and MET mutant with IC50 values in the range of 0.3-6 nM.

S4686

Vitamin E

Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription.

S7847

SGI-7079

SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.

S7003

AZD2932

AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.

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.

S5234

Nintedanib Ethanesulfonate Salt

Nintedanib 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.

S5077

Regorafenib Monohydrate

Regorafenib 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, RET, RAF-1, B-RAF and B-RAF(V600E) respectively.

S2366

Taxifolin (Dihydroquercetin)

Taxifolin, type I inhibitor for VEGFR-2 kinase, is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on.

Catalog No. Information Product Use Citations Product Validations
S2431New

TMTD (Tetramethylthiuram disulfide)

TMTD (Tetramethylthiuram disulfide) can reduce the growth performance of chickens through decreasing liver index, whereas increasing kidney, cardiac, and spleen index, and induces tibial dyschondrolplasia (TD) by changing the expressions of VEGF, HIF-1α and WNT4. TMTD (Tetramethylthiuram disulfide) is widely used in rubber processing as an ultra accelerator for low-temperature cures and in agriculture as an important pesticide.

Catalog No. Information Product Use Citations Product Validations
S9190

Oroxin B

Oroxin B, one of flavonoids isolated from traditional Chinese herbal medicine Oroxylum indicum (L.) Vent, selectively induces tumor-suppressive ER stress in malignant lymphoma cells and has antioxidant activity. Oroxin B significantly inhibits proliferation and induce apoptosis, which may be strongly associated with the inhibiting COX-2/VEGF and PTEN/PI3K/AKT signaling pathway in SMMC-7721 cells, Oroxin B potentially be used as a novel therapeutic agent for liver cancer.COX-2, VEGF, PI3K, and p-AKT expression levels is found to be downregulated, while PTEN was upregulated after Oroxin B treatment.

Tags: VEGFR inhibition | VEGFR cancer | VEGFR2 cancer | VEGFR pathway | VEGFR phosphorylation | VEGFR2 phosphorylation | VEGFR signaling pathway | VEGFR assay | VEGFR inhibitor drug | VEGFR inhibitor review