vegfr 1

VEGFR-3-IN-1 is a novel potent and selective VEGFR3 inhibitor with an IC50 of 110.4 nM.VEGFR-3-IN-1 possesses antitumor activity, inactivates the VEGFR3 signaling pathway, and inhibits the proliferation and migration of VEGF-C-induced human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231 and MDA-MB-436 cells. MB-436 cells and inhibited the proliferation and migration of human dermal lymphatic endothelial cells (HDLEC), MDA-MB-231 and MDA-MB-436 cells.

VEGFR-2/c-Met-IN-1 is a dual inhibitor targeting VEGFR-2 and c-Met with respective IC50 values of 138 nM and 74 nM, demonstrating antitumor activity [1].

VEGFR-2/BRAF-IN-1, a dual inhibitor of VEGFR-2 and BRAF kinases, demonstrates potent inhibitory activity with IC50 values of 0.049 µM for VEGFR-2, 0.063 µM for BRAF V600E, and 0.005 µM for BRAF WT. It effectively induces apoptosis and arrests the cell cycle primarily at the G1/S phase.

VEGFR inhibitor

VEGFR-2/DHFR-IN-1 (compound 8b) is a chemical inhibitor targeting VEGFR-2 and DHFR, exhibiting IC50 values of 0.384 μM and 7.881 μM, respectively. It demonstrates effective antibacterial properties against a range of pathogens including Escherichia coli, Streptococcus faecalis, Salmonella enterica, MSSA, and MRSA, with MIC values ranging from 8 to 16 μg/mL. Additionally, this compound shows potent cytotoxic effects against various cancer cell lines such as C26, HepG2, and MCF7, with IC50 values between 2.97 and 7.12 μM, rendering it a valuable tool for cancer research [1].

TIE-2/VEGFR-2 kinase-IN-1 is used for the synthesis of TIE-2 and/or VEGFR-2 inhibitors that can be used for the study of diseases associated with inappropriate angiogenesis [1].

PROTAC VEGFR-2 Degrader-1 (PROTAC-1), a specific degrader of PROTAC VEGFR-2, demonstrates minimal inhibition of VEGFR-2 (IC50 > 1 μM) and exhibits low anti-proliferative effects on EA.hy926 cells (IC50 > 100 μM) [1].

VEGFR/PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively. It impairs DNA damage repair pathways, promotes apoptosis, and halts cells in the G2/M phase. This compound demonstrates considerable antiproliferative activity against BRCA wild-type breast cancer cells, with IC50 values of 4.1 μM for MDA-MB-231 cells and 3.5 μM for MCF-7 cells, indicating its potential as an antitumor and anti-metastasis agent [1].

hCA/VEGFR-2-IN-1 (compound 13a) is a potent dual inhibitor targeting both Carbonic Anhydrase (CA) IX/XII and Vascular Endothelial Growth Factor Receptor 2 (VEGFR-2). It exhibits Ki values of 4.7 nM for hCA XII and 8.3 nM for hCA IX, alongside an IC50 of 26.3 nM for VEGFR-2. This compound demonstrates anticancer activity [1].

VEGFR2-IN-1 is a selective and potent VEGFR2 inhibitor with antitumor activity that inhibits cell proliferation and migration and can be used in the study of breast cancer.

VEGFR2/HDAC1-IN-1 (compound 13) is a potent dual inhibitor of VEGFR-2 and HDAC, with IC50 values of 57.83 nM for VEGFR-2 and 9.82 nM for HDAC. It arrests the cell cycle at the S and G2 phases and induces apoptosis in HeLa cells, demonstrating an anti-angiogenic effect [1].

FGFR1/VEGFR2-IN-1 (compound 2b) is an inhibitor of both FGFR1 and VEGFR2, applicable in cancer research [1].

PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting both PI3K and VEGFR2 with IC50 values of 2.21 μM for PI3K and 68 μM for VEGFR2, respectively. This compound also induces apoptosis and is utilized in cancer research [1].

Tesevatinib (XL-647) is an orally available, multi-target tyrosine kinase inhibitor (IC50s: 0.3, 16, 1.5, 8.7, and 1.4 nM for EGFR, ErbB2, KDR, Flt4, and EphB4).

Pazopanib (GW786034), a small molecule inhibitor, inhibits multiple protein tyrosine kinases with potential antineoplastic activity. Pazopanib selectively inhibits VEGFR-1, -2 and -3, c-kit and PDGF-R, which may result in inhibition of angiogenesis in tumors in which these receptors are upregulated.

Cabozantinib hydrochloride (XL184) is a potent pan-tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl, and Flt4 (IC50s: 0.035, 1.3, 4.6, 7 and 6 nM).

(Z)-Semaxinib (SU5416) is a potent and selective VEGFR(Flk-1/KDR) inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR over PDGFRβ, no inhibition for FGFR, InsR, and EGFR. (Z)-Semaxinib is a quinolone derivative with potential antineoplastic activity.

Famitinib (SHR1020) is a potent orally active multi-targeted kinase inhibitor that effectively inhibits the activity of c-kit, VEGFR-2, and PDGFRβ with IC50 values of 2.3 nM, 4.7 nM, and 6.6 nM, respectively [1]. It demonstrates remarkable antitumor properties in human gastric cancer cells and xenografts, inducing apoptosis [2].

Sorafenib tosylate (Bay 43-9006) is a potent multikinase inhibitor (IC50s: 6/20/22 nM for Raf-1/VEGFR-3/B-Raf).

OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.

Cediranib (AZD2171) (AZD2171) is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro, also inhibits Flt1/4 (IC50: 5 nM/≤3 nM), similar activity against PDGFRβ and c-Kit, selective more for VEGFR than PDGFR-α (36-fold), CSF-1R (110-fold), and Flt3 (1000-fold) in HUVEC cells.

Semaxinib (SU5416) is a potent and selective VEGFR2 inhibitor (IC50: 1.23 μM), 20-fold more selective for VEGFR than PDGFRβ, lack of activity against InsR, EGFR, and FGFR. Semaxanib reversibly inhibits ATP binding to the tyrosine kinase domain of vascular endothelial growth factor receptor 2 (VEGFR2), which may inhibit VEGF-stimulated endothelial cell migration and proliferation and reduce the tumor microvasculature.

Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase (RTK) inhibitor that inhibits VEGFR2 and PDGFRβ (IC50=80/2 nM). Sunitinib has antitumor activity and can be used for the treatment of kidney cancer and gastrointestinal tumors.

Sitravatinib (MGCD516) is an inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Met, c-Kit, PDGFRα/β, PDGFR, and Axl.

Chloramphenicol (Chloromycetin), a broad-spectrum antibiotic, blocks bacterial protein synthesis.

ACC-789 (NVP-ACC789 (ZK202650); ZK-202650) is an effective, specific and orally active inhibitor of the VEGF receptor tyrosine kinases.

Multi-kinase-IN-5 (compound 15c) is a multi-kinase inhibitory agent that shows significant inhibition against a range of protein kinases including RET, KIT, cMet, VEGFR1, VEGFR2, FGFR1, PDGFR, and BRAF, with corresponding inhibition percentages of 74%, 31%, 62%, 40%, 73%, 74%, 59%, and 69%. Its IC50 values are 1.287 μM for FGFR1, 0.117 μM for VEGFR, and 1.185 μM for RET kinases, indicating its potency [1].

SU5214 is a modulator of tyrosine kinase signal transduction.

SU5204 (3-[(2-Ethoxyphenyl)methylidene]-1H-indol-2-one), an analogue of SU5025, pharmacologically inhibits VEGFR2(IC50s of 4 and 51.5 μM for FLK-1 (VEGFR-2) and HER2)

VEGFR-2-IN-37 (compound 12), a VEGFR-2 inhibitor, exhibits an inhibition rate of approximately 56.9 μM at a concentration of 200 μM. It is also identified as a potential inhibitor of human umbilical vein endothelial cell (HUVEC) proliferation [1].

ZD-4190 is a compound that inhibits both the vascular endothelial growth factor receptor 2 (VEGFR2) and the epidermal growth factor receptor (EGFR) signaling pathways, utilized in cancer treatment.

T-1-MCPAB, a VEGFR-2 inhibitor with an IC50 of 0.135 µM, effectively suppresses MCF7 cell migration and has applications in cancer research [1].

Sotiburafusp alfa is a humanized bispecific fusion protein comprising a VEGFR-1 extracellular domain fragment (129-228, 1-100 in the current sequence) connected through a 101 GGSGGSGGSGGSGGS 115 peptide linker to the N-terminus (116-564) of a humanized IgG1-kappa anti-human PD-L1 heavy chain with L352>A and L353>A mutations. Additionally, sotiburafusp alfa functions as an angiogenesis inhibitor [1].

LXW7 TFA, a cyclic peptide encompassing Arg-Gly-Asp (RGD), serves as an inhibitor of integrin αvβ3. It demonstrates high binding affinity towards αvβ3 integrin, evidenced by an IC50 value of 0.68 μM. Additionally, LXW7 TFA promotes the phosphorylation of VEGFR-2 and the activation of ERK1/2, contributing to its anti-inflammatory effects [1] [2] [3].

JK-P3 is a pyrazole-based inhibitor of VEGFR-2 (IC50: 7.8 μM). JK-P3 inhibits FGFR 1/3 kinase activity in vitro, but has no effect on FGFR signaling in cell-based assays. The compound blocks wound healing and tube formation in HUVEC without effecting endo

SU5205 is a VEGFR2 inhibitor.

TIE-2/VEGFR-2 kinase-IN-4, a benzimidazole derivative, serves as a potent inhibitor of the tyrosine kinase receptors TIE-2 and VEGFR-2, exhibiting inhibitory concentration (IC50) values of 5.2 nM and 5.1 nM, respectively. This compound is utilized in angiogenesis research [1].

Azurin p28 peptide, a tumor-penetrating antitumor agent, stabilizes p53 by reducing its proteasomal degradation via the formation of a p28:p53 complex. It elicits apoptosis or cell cycle arrest and suppresses the growth of p53-positive tumors. Additionally, the peptide exhibits antiangiogenic properties by inhibiting the phosphorylation of VEGFR-2, FAK, and Akt [1] [2] [3].

VEGFR-2/DHFR-IN-2 (compound 5b) is a dual inhibitor targeting VEGFR-2 and DHFR, with respective IC50 values of 0.623 μM and 9.085 μM. It demonstrates potent cytotoxicity against C26, HepG2, and MCF7 cancer cell lines, with IC50 values ranging from 3.59 μM to 8.38 μM. VEGFR-2/DHFR-IN-2 holds promise for cancer research [1].

VEGFR-2-IN-18 (Compound 15d) is a high-potency inhibitor of VEGFR-2, with an IC 50 value of 60 nM. This compound effectively initiates cell apoptosis and demonstrates significant antitumor properties [1].

WHI-P180 (Janex 3) is a potent EGFR and Cdk2 inhibitors with IC50 of 4.0 and 1.0 uM, respectively.

Sunitinib Malate (Sunitinib) is an indolinone-based tyrosine kinase inhibitor. It blocks the tyrosine kinase activities of VEGFR2, PDGFRβ (IC50: 80/2 nM), and c-kit.

VEGFR-2-IN-19 (Compound 15b) is a highly efficacious inhibitor of VEGFR2, a receptor involved in angiogenesis. Its mechanism of action involves the induction of cellular apoptosis and elevation of intracellular reactive oxygen species. Due to these properties, VEGFR-2-IN-19 holds promise as an effective anticancer agent [1].

Tyrphostin AG1433 (AG1433) is an inhibitor of tyrosine kinases and also a dual inhibitor of PDGFRβ(IC50s = 5.0 μM) and VEGFR-2 (Flk-1/KDR)(IC50s = 9.3 μM).

Linifanib (AL-39324) (ABT-869) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR (IC50: 4 nM), CSF-1R (IC50: 3 nM), Flt-1/3 (IC50: 3/4 nM) and PDGFRβ (IC50: 66 nM). Linifanib may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3).

Ki-20227 is a specific c-Fms tyrosine kinase(CSF1R) inhibitor (IC50: 2 nM). It also has certain inhibitory against VEGFR2(IC50: 12 nM) and c-Kit/PDGFRβ(IC50: 451/217 nM), respectively.

Tivozanib (KRN951) is an orally bioavailable inhibitor of vascular endothelial growth factor receptors (VEGFRs) 1, 2 and 3 with potential antiangiogenic and antineoplastic activities.

Fruquintinib-d3 is a deuterated compound of Fruquintinib. Fruquintinib has a CAS number of 1194506-26-7. Fruquintinib is an orally available, small molecule inhibitor of vascular endothelial growth factor receptors (VEGFRs), with potential anti-angiogenic and antineoplastic activities.

VEGFR-2-IN-33 (Compound 4d), a potent VEGFR inhibitor with an IC50 value of 61.04 nM, demonstrates significant inhibition of HepG2 cell proliferation, achieving an IC50 of 4.31 nM. This compound is utilized for hepatocellular carcinoma (HCC) research [1].

VEGFR-2-IN-35 (compound 7) is a potent inhibitor of VEGFR-2, exhibiting an IC50 of 37 nM. Additionally, it demonstrates inhibitory activity against MCF-7 and HCT 116 cancer cell lines with IC50 values of 10.56 μM and 7.07 μM, respectively [1].