vatalanib succinate : A succinate salt obtained by combining vatalanib with one molar equivalent of succinic acid. It is a multi-targeted tyrosine kinase inhibitor for all isoforms of VEGFR, PDGFR and c-Kit. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 151193 |
| CHEMBL ID | 75232 |
| CHEBI ID | 90623 |
| SCHEMBL ID | 675786 |
| MeSH ID | M0358254 |
| Synonym |
|---|
| chebi:90623 , |
| chembl75232 , |
| ptk-787 , |
| ptk787/zk222584 |
| cgp-79787d |
| zk-222584 |
| ptk/zk |
| 1-(4-chloroanilino)-4-(4-pyridylmethyl)phthalazine succinate |
| nsc719335 |
| vatalanib succinate |
| nsc-719335 |
| 1-phthalazinamine, butanedioate (1:1) |
| 212142-18-2 |
| 1-[4-chloroanilino]-4-[4-pyridylmethyl]phthalazine succinate |
| zk222584 |
| ptk 787 |
| zk 222584 |
| 1-phthalazinamine, n-(4-chlorophenyl)-4-(4-pyridinylmethyl)-, butanedioate (1:1) |
| cgp 79787d |
| ptk 787/zk 222584 |
| v5fub77031 , |
| unii-v5fub77031 |
| AKOS015958655 |
| F9995-0197 |
| n-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine succinate |
| vatalanib succinate [mi] |
| ptk-787/zk-222584 |
| vatalanib succinate [who-dd] |
| LLDWLPRYLVPDTG-UHFFFAOYSA-N |
| MLS006011673 |
| smr004703417 |
| SCHEMBL675786 |
| c24h21cln4o4 |
| vatalanib monosuccinate |
| DTXSID60175445 |
| n-(4-chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine succinate |
| n-(4-chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine butanedioate |
| A912179 |
| BCP24024 |
| Q27162634 |
| SB16583 |
| butanedioic acid;n-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine |
| butanedioate;(4-chlorophenyl)-[4-(pyridin-4-ylmethyl)phthalazin-1-yl]azanium;hydron |
| Role | Description |
|---|---|
| angiogenesis inhibitor | An agent and endogenous substances that antagonize or inhibit the development of new blood vessels. |
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor | An EC 2.7.10.* (protein-tyrosine kinase) inhibitor that interferes with the action of receptor protein-tyrosine kinase (EC 2.7.10.1). |
| vascular endothelial growth factor receptor antagonist | An antagonist at the vascular endothelial growth factor receptor. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| succinate salt | A salt of succinic acid. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Tyrosine-protein kinase ABL1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0001 | 0.7128 | 10.0000 | AID219188 |
| Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0000 | 0.5369 | 10.0000 | AID69880 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 1.3452 | 10.0000 | AID53175 |
| Macrophage colony-stimulating factor 1 receptor | Homo sapiens (human) | IC50 (µMol) | 1.2400 | 0.0006 | 0.5676 | 5.5450 | AID50766 |
| Insulin-like growth factor 1 receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0003 | 0.4308 | 8.0000 | AID93094 |
| Platelet-derived growth factor receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.5450 | 0.0006 | 0.8007 | 8.5000 | AID157463; AID161407 |
| Mast/stem cell growth factor receptor Kit | Homo sapiens (human) | IC50 (µMol) | 0.6600 | 0.0007 | 0.4708 | 10.0000 | AID108256; AID163725 |
| Fibroblast growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0002 | 0.9420 | 10.0000 | AID73451 |
| Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0002 | 0.5335 | 10.0000 | AID219509 |
| Vascular endothelial growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.0935 | 0.0001 | 0.2914 | 7.0000 | AID216631; AID73630 |
| Vascular endothelial growth factor receptor 3 | Homo sapiens (human) | IC50 (µMol) | 0.1950 | 0.0001 | 0.2264 | 4.9000 | AID216922 |
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.0330 | 0.0000 | 0.4830 | 8.8000 | AID216649; AID216652; AID331717; AID94665 |
| Angiopoietin-1 receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0004 | 0.5553 | 9.0700 | AID213567 |
| Macrophage-stimulating protein receptor | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0012 | 0.2698 | 3.3700 | AID108335 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Vascular endothelial growth factor receptor 2 | Homo sapiens (human) | ED50 | 0.0340 | 0.0340 | 0.4820 | 0.9300 | AID217170 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID94665 | Inhibitory activity against kinase domain containing receptor (KDR/VEGFR2) | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12 | New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. |
| AID331719 | Antiproliferative activity against VEGF-induced HUVEC cells | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity. |
| AID86730 | Mean % inhibition of induced angiogenesis by Heparin-binding growth factor 2 at a peroral dose of 50 mg/kg in mice | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID216922 | In vitro inhibition of Vascular endothelial growth factor receptor 3 [VEGFR-3(Flt-4)] expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID40734 | Mean % inhibition of primary tumor growth in B16 mouse administration | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID331717 | Inhibition of KDR by ELISA | 2008 | Bioorganic & medicinal chemistry letters, May-01, Volume: 18, Issue:9 | Conformation-activity relationship on novel 4-pyridylmethylthio derivatives with antiangiogenic activity. |
| AID1055733 | Inhibition of VEGFR2 (unknown origin) using poly (Glu, Tyr)4:1 as substrate preincubated at 10 uM for 5 mins measured after 30 mins by immunoassay | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Synthesis and biological evaluation of substituted 1,2,3-benzotriazines and pyrido[3,2-d]-1,2,3-triazines as inhibitors of vascular endothelial growth factor receptor-2. |
| AID73630 | Inhibitory activity against Flt-kinase | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12 | New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. |
| AID426966 | Antiangiogenic activity in zebrafish embryo assessed as inhibition of intersegmental vessel growth at 0.1 ug/mL after 24 hours by alkaline phosphatase staining relative to control | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6 | Ingol and ingenol diterpenes from the aerial parts of Euphorbia royleana and their antiangiogenic activities. |
| AID108335 | In vitro inhibition of Met proto-oncogene tyrosine kinase (c-Met) expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID216652 | Inhibition of VEGFR induced autophosphorylation of human Vascular endothelial growth factor receptor 2 (VEGFR2) transfected in CHO cells | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID426964 | Antiangiogenic activity in zebrafish embryo assessed as inhibition of intersegmental vessel growth at 10 ug/mL after 24 hours by alkaline phosphatase staining relative to control | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6 | Ingol and ingenol diterpenes from the aerial parts of Euphorbia royleana and their antiangiogenic activities. |
| AID157463 | Inhibition of PDGF- beta receptor kinase | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12 | New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. |
| AID213567 | In vitro inhibition of Tyrosine protein kinase receptor TIE-2 (Tek) expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID1055732 | Growth inhibition of HMVEC after 4 days by MTT assay | 2013 | Bioorganic & medicinal chemistry, Dec-15, Volume: 21, Issue:24 | Synthesis and biological evaluation of substituted 1,2,3-benzotriazines and pyrido[3,2-d]-1,2,3-triazines as inhibitors of vascular endothelial growth factor receptor-2. |
| AID53175 | In vitro inhibition of Cyclin-dependent kinase 1 (CDK-1) expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID161407 | In vitro inhibition of Platelet-derived growth factor receptor beta expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID40733 | Mean % inhibition of lymph node metastasis in B16 mouse administration | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID14484 | The maximum concentration observed (Cmax) in the blood sample at indicated time point (tmax) at a dose 50 mg/Kg administered orally in mice. | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12 | New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. |
| AID24749 | The maximum time reported (tmax) at an oral dose of 50 mg/Kg in mice | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12 | New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. |
| AID219509 | In vitro inhibition of c-SRC kinase expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID426961 | Antiangiogenic activity in zebrafish embryo assessed as inhibition of intersegmental vessels growth after 24 hours by alkaline phosphatase staining | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6 | Ingol and ingenol diterpenes from the aerial parts of Euphorbia royleana and their antiangiogenic activities. |
| AID426962 | Antiangiogenic activity in zebrafish embryo assessed as inhibition of intersegmental vessel growth at 1 ug/mL after 24 hours by alkaline phosphatase staining relative to control | 2009 | Journal of natural products, Jun, Volume: 72, Issue:6 | Ingol and ingenol diterpenes from the aerial parts of Euphorbia royleana and their antiangiogenic activities. |
| AID219188 | In vitro inhibition of c-Abl tyrosine kinase expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID93094 | In vitro inhibition of Insulin-like growth factor I receptor expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID217170 | Inhibition of VEGF-stimulated autophosphorylation of VEGF-receptor 2 (KDR) expressed in CHO cells | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12 | New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. |
| AID69880 | In vitro inhibition of Epidermal growth factor receptor (HER-1,ErbB) expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID108256 | In vitro inhibition of Mast/stem cell growth factor receptor (c-Kit kinase) expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID73451 | In vitro inhibition of Fibroblast growth factor receptor expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID163725 | Inhibition of Proto-oncogene tyrosine-kinase c-Kit | 2000 | Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12 | New anilinophthalazines as potent and orally well absorbed inhibitors of the VEGF receptor tyrosine kinases useful as antagonists of tumor-driven angiogenesis. |
| AID50766 | In vitro inhibition of Colony stimulating factor 1 receptor (CSF-1R) expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID216631 | In vitro inhibition of Vascular endothelial growth factor receptor 1 (VEGFR-1) expressed in baculovirus | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID216649 | In vitro inhibition of Vascular endothelial growth factor receptor 2 (VEGFR-2) | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| AID216620 | Mean % inhibition of induced angiogenesis by Vascular endothelial growth factor (VEGF) at a peroral dose of 50 mg/kg in mice | 2002 | Journal of medicinal chemistry, Dec-19, Volume: 45, Issue:26 | Anthranilic acid amides: a novel class of antiangiogenic VEGF receptor kinase inhibitors. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 4 (80.00) | 29.6817 |
| 2010's | 1 (20.00) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (22.17) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||