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VEGFR

VEGFR

Three protein-tyrosine kinases (VEGFR1, VEGFR2, and VEGFR3) and two non-protein kinase co-receptors (neuropilin-1 and neuropilin-2) make up the vascular endothelial growth factor (VEGF) family of receptors. The extracellular component of VEGFRs, which has seven immunoglobulin-like domains, one transmembrane domain, and a split tyrosine kinase domain, make up typical tyrosine kinase receptors (TKRs). VEGFR-1 binds to VEGF-A, -B, and PlGF; VEGFR-2 is activated by VEGF-A, -C, -D, and -E; and VEGFR-3 is particular to VEGF-C and -D. The consensus model for ligand-induced activation of RTKs states that VEGF binds to a cognate VEGFR to cause receptor dimerization, which then triggers the activation of protein kinases, autophosphorylation of tyrosine residues in the intracellular domains of the receptor, and the initiation of signaling pathways like PI3K/AKT and MAPK/ERK1/2.VEGFR signaling is tightly controlled at many different levels, including receptor expression levels, the availability and affinities of its various ligands for binding, the presence of VEGF-binding co-receptors, non-VEGF-binding auxiliary proteins, and inactivating tyrosine phosphatases, as well as the rate of receptor cellular uptake, extent of receptor degradation, and speed of recycling.

VEGFR related products

Structure Cat No. Product Name CAS No. Product Description
(Z)-Guggulsterone V5032 (Z)-Guggulsterone 39025-23-5 Z)-Guggulsterone, the cis-isomer ofGuggulsterone, is a naturally occuring phytosteroid isolated from the resin of the guggul plant, Commiphora mukul.
AAL-993 V2092 AAL-993 269390-77-4 AAL-993 is a novel, orally bioavailable and highly potent VEGFR inhibitor that inhibits VEGFR1, 2, and 3 with IC50 values of 130, 23, and 18 nM, respectively.
ACC-789 V3414 ACC-789 300842-64-2 ACC-789, also known as ZK-202650 and NVP-ACC789 is a novel, potent, selective and orally bioavailable inhibitor of human VEGFR-1, VEGFR-2 (mouse VEGFR-2), VEGFR-3 and PDGFR-β with IC50s of 0.38, 0.02 (0.23), 0.18, 1.4 μM, respectively.
Altiratinib V2885 Altiratinib 1345847-93-9 Altiratinib (also known as DCC-2701 and DP-5164) is an orally active, highly potent and selective multi-kinase inhibitor with IC50 values of 2.7, 8, 9.2, 9.3, 0.85, 4.6, 0.83 nM for MET, TIE2, VEGFR2, FLT3, Trk1, Trk2, and Trk3.
AMG-Tie2-1 V2156 AMG-Tie2-1 870223-96-4 AMG-Tie2-1 is an inhibitor (blocker/antagonist) of intimal endothelial cell kinase 2 (Tie2) with IC50 of 1 nM.
Anti-Mouse VEGFR-2 Antibody (DC101) V85007 Anti-Mouse VEGFR-2 Antibody (DC101)
Apatinib (Rivoceranib, YN968D1) V0503 Apatinib (Rivoceranib, YN968D1) 811803-05-1 Apatinib (formerly known as Rivoceranib,YN-968D1) is a potent, orally bioavailable, and selective inhibitor of the VEGF (vascular endothelial growth factor receptor) signaling pathway withpotential antiangiogenic and antineoplastic activities.
Apatinib mesylate V3283 Apatinib mesylate 1218779-75-9 Apatinibmesylate, themesylate salt of apatinib, is a potent, orally bioavailable, and selective inhibitor of the VEGF (vascular endothelial growth factor receptor) signaling pathway with IC50 of 1 nM for VEGFR2.
Axitinib (AG-013736; Inlyta) V0492 Axitinib (AG-013736; Inlyta) 319460-85-0 Axitinib (formerly AG013736; brand name Inlyta), is a potent, orally bioavailable, small molecule and multi-targeted kinase inhibitor with potential antitumor activity.
AZD2932 V0496 AZD2932 883986-34-3 AZD2932 (AZD-2932), a new quinazoline ether, is a novel, potent, high affinity and mutil-targeted tyrosine kinase inhibitor with potential anticancer activity.
BFH772 V2674 BFH772 890128-81-1 BFH772 (also known as BFH-772)is a novel andpotent orallybioavailableVEGFR2 inhibitor thattargets VEGFR2 kinase with IC50 of 3 nM.
BHEP V85453 BHEP
BIBF-1202 V12626 BIBF-1202 894783-71-2 BIBF-1202 (BIBF1202; BIBF 1202) is the carboxylate metabolite of Nintedanib (formerly BIBF-1120; Vargatef), which is an approved anticancer medication acting as an orally bioavailable triple angiokinase (VEGFR, PDGFR, FGFR) inhibitor.
BMS-794833 V0501 BMS-794833 1174046-72-0 BMS-794833 (BMS794833; BMS 794833) is an ATP competitive multi-kinase (Met/VEGFR2) inhibitor with potential anticancer activity.
Brivanib (BMS-540215) V0506 Brivanib (BMS-540215) 649735-46-6 Brivanib (formerlyBMS-540215; BMS540215) is a novel,investigational, oral andATP-competitive inhibitor of VEGFR2 with potential anticancer activity.
Brivanib Alaninate (BMS-582664) V0512 Brivanib Alaninate (BMS-582664) 649735-63-7 Brivanib alaninate (formerly BMS-582664) is the alaninate ester form and prodrug of Brivanib, which is an investigational and ATP-competitive inhibitor of VEGFR2 with potential anticancer activity.
Cabozantinib (XL184; BMS907351; Cometriq) V0490 Cabozantinib (XL184; BMS907351; Cometriq) 849217-68-1 Cabozantinib (formerly known as XL-184 or BMS-907351; trade name Cometriq) is a novel, orally bioavailable and potent VEGFR2 inhibitor with anticancer activity.
Cabozantinib malate (XL184) V0526 Cabozantinib malate (XL184) 1140909-48-3 Cabozantinib malate (formerly known as XL-184 or BMS-907351; trade name Cometriq) is the malate salt form of Cabozantinib, a novel, potent and orally bioavailable VEGFR2 inhibitor with potential anticancer activity.
Cediranib (NSC-732208; AZD-2171) V0517 Cediranib (NSC-732208; AZD-2171) 288383-20-0 Cediranib (also called NSC732208; AZD2171,tentative trade name Recenti),an indole ether quinazoline derivative, is a potent and oral VEGFR (vascular endothelial growth factor receptors) inhibitor with potential antitumor activity.
Cediranib maleate V3282 Cediranib maleate 857036-77-2 Cediranib maleate(AZD-2171;Recenti, an indole ether quinazoline derivative), the maleate salt of Cediranib, is a novle and highly potent VEGFR (KDR) inhibitor with anticancer activity.
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