Parsatuzumab (Anti-EGFL7; RG 7414) is a humanized monoclonal antibody, acts as an immunomodulator and binds to EGFL7. Parsatuzumab selectively blocks the interaction between EGFL7 and endothelial cells, potentially inhibiting vascular regrowth and reducing vascular endothelial growth factor (VEGF) inhibition[1].
VEGFR-2-IN-6 (example 64) is a VEGFR2 inhibitor (angiogenesis modulator), which is extracted from patent WO 02/059110[1].
(Z)-FeCP-oxindole is a selective human vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with an IC50 value of 200 nM. (Z)-FeCP-oxindole can significantly inhibit VEGFR1 and PDGFRa or b at 10 μM. (Z)-FeCP-oxindole has some anticancer activity, acting on B16 murine melanoma lines with IC50 less than 1 μM[1].
Vanucizumab is a first-in-class, bispecific IgG1-like monoclonal antibody that simultaneously blocks VEGF-A and angiopoietin-2 (Ang-2) from interacting with their receptors. Vanucizumab has antiangiogenic and anticancer effects[1].
Sunitinib Malate (SU 11248 Malate) is a potent tyrosine kinase inhibitor targeting VEGFR2 and PDGFRβ with IC50s of 80 nM and 2 nM, respectively.
Cabozantinib-d6 (XL184-d6) is the deuterium labeled Cabozantinib. Cabozantinib is a potent multiple receptor tyrosine kinases (RTKs) inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively[1][2][3].
Pegdinetanib (BMS-844203; CT-322) is a selective VEGFR-2 (VEGFR) inhibitor with Kds of 11 nM and 250 nM and IC50s of 16 nM and 240 nM for human and murine VEGFR-2, respectively. Pegdinetanib does not bind to VEGFR-1 or VEGFR-3. Pegdinetanib has antitumor activity[1].
VEGFR2-IN-3 (compound 385) is a potent VEGFR2 inhibitor[1].
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ, c-Kit, FGFR1, and c-Fms with IC50s of 10, 30, 47, 84, 74, 140 and 146 nM, respectively.
Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].
VS 8 (Compound VS 8) is a potent, orally active VEGFR-2 inhibitor with significant anti-angiogenic effects. VS 8 induces cancer cell apoptosis and migration. VS 8 is active against CSCs (Cancer stem cells)[1].
AhR modulator-1 (compound 6-MCDF) is a selective and orally active aryl hydrocarbon receptor (AhR) modulator. AhR modulator-1 inhibits metastasis, in part, by inhibiting prostatic VEGF production prior to tumor formation. AhR modulator-1 also possess anti-estrogenic properties in rat uterus[1].
Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
ABP 215 (Bevacizumab-awwb), a Bevacizumab (Bevacizumab (HY-P9906)) biosimilar, is a humanized IgG1 monoclonal antibody targeting VEGFA (VEGFR). ABP 215 has anticancer effects, and can be used metastatic colorectal cancer (mCRC) research[1][2].
GW806742X is a Mixed Lineage Kinase Domain-Like (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and anti-necroptosis activity. GW806742X has activity against VEGFR2[1][2].
Apatinib-d8 (free base) is the deuterium labeled Apatinib free base[1]. Apatinib free base (YN968D1 free base) is an orally bioavailable tyrosine kinase inhibitor, which selectively targets VEGFR-2 (IC50=1 nM). Apatinib free base (YN968D1 free base) is an anti-angiogenic drug for the treatment of advanced or metastatic gastric cancer. Apatinib free base (YN968D1 free base) potently inhibits Ret, c-Kit and c-Src with IC50s of 13, 429 and 530 nM, respectively. It also inhibits cellular phosphorylation of VEGFR-2, c-kit and PDGFRβ[2][3][4].
VEGFR-2-IN-20 (Compound 7) is a potent inhibitor of VEGFR. VEGFR-2-IN-20 has the potential for the research of cancer diseases[1].
Vatalanib (PTK787) succinate is a potent and orally active VEGFR inhibitor with IC50s of 37 nM, 77 nM, 270 nM, 660 nM, 730 nM, 1400 nM, and 580 nM for KDR, Flt-1, Flk, Flt-4, c-Kit, c-Fms, and PDGFR-β, respectively[1].
VEGFR-IN-1 (compound 3) is a potent angiogenesis inhibitor with IC50s of 0.02, 0.18, 0.24 7.3, and 7 µM for KDR, Flt-1, c-Kit, EGF-R, and c-Src, respectively[1].
hVEGF-IN-2 (compound 19) is a selective VEGF (Flk-1) receptor tyrosine kinases (RTK) inhibitor with an IC50 value of 2.5 μM. hVEGF-IN-2 inhibits PDGF RTK activity with an IC50 value of 33.1 μM. hVEGF-IN-2 can be used for the development of RTK-specific drugs[1].
Regorafenib D3 (BAY 73-4506 D3) is a deuterium labeled Regorafenib. Regorafenib is a multi-targeted receptor tyrosine kinase inhibitor[1].
BIBF 1120 is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
Ramucirumab is a human VEGFR-2 antagonist for the treatment of solid tumors[1]. Ramucirumab is a recombinant human immunoglobulin G1 monoclonal antibody that binds to the extracellular binding domain of VEGFR-2 and prevents the binding of VEGFR ligands: VEGF-A, VEGF-C, and VEGF-D[2].
VEGFR-2-IN-24 is a potent VEGFR-2 inhibitor with IC50 value of 0.22 µM. VEGFR-2-IN-24 can be used for tumor research[1].
Ilorasertib hydrochloride (ABT-348 hydrochloride) is a potent and ATP-competitive multitargeted kinase inhibitor, which inhibits Aurora C, Aurora B, and Aurora A with IC50s of 1 nM, 7 nM, 120 nM, respectively. Ilorasertib hydrochloride (ABT-348 hydrochloride) also suppresses RET tyrosine kinase, PDGFRβ and Flt1 with IC50s of 7 nM, 3 nM and 32 nM, respectively[1].
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer[1].
VEGFR-2-IN-29 (Compound 5) is a VEGFR-2 inhibitor with an IC50 of 16.5 nM[1].
(Rac)-SAR131675 is the racemate of SAR131675. SAR131675 is a potent and selective VEGFR3 inhibitor with an IC50 of 23 nM[1][2].
Ponatinib is a potent, orally available multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
Protein LMWP is a cell-penetrating peptide with vascular endothelial growth factor (VEGF) inhibitory activity. Protein LMWP can inhibit tumor growth and is used in cancer research[1].