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.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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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. |
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V0501 | BMS-794833 | 1174046-72-0 | BMS-794833 (BMS794833; BMS 794833) is an ATP competitive multi-kinase (Met/VEGFR2) inhibitor with potential anticancer activity. |
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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. |
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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. |
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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. |
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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. |
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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. |
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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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V5272 | CP-547632 (PAN-90806) | 252003-65-9 | CP-547632 (PAN-90806), a novel isothiazole, is a novel, orally bioavailable and ATP-competitive inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. |
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V31207 | CP-547632 hydrochloride (PAN-90806) | 252003-71-7 | CP-547632 HCl (PAN90806), a novel isothiazole, is a orally-bioavailable and ATP-competitive inhibitor of the VEGFR-2 and basic fibroblast growth factor (FGF) kinases with IC50s of 11 nM and 9 nM, respectively. |
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