Vatalanib base
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CAS No.:
212141-54-3
Content:
99%
Price valid (until):
2026-10-03
Company Type:
Manufactory
Location:
United States
Qualification:
Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Product Description
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Seller Information
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Description
ProductName Vatalanib base Cat No CEI-0054 Description Vatalanib base can inhibit VEGFR-2 (KDR), VEGF-R1(FLT-1), Flk and c-Kit with IC50 of 37 nM, 77 nM, 270 nM and 730 nM. Alias ZK222584 CAS No 212141-54-3 Molecular Weight 346.81 Purity >99% Storage 2 years at -20centigrade Powder Synonyms ZK222584 Targets VEGFR-2 (KDR) Molecular Formula C20H15ClN4 Chemical Name N-(4-chlorophenyl)-4-(pyridin-4-ylmethyl)phthalazin-1-amine dihydrochloride Solubility DMSO 85 mg/mL Water 10 mg/mL Ethanol 6 mg/mL In vitro Vatalanib base can inhibit VEGFR-2 (KDR), VEGF-R1(FLT-1), Flk and c-Kit with IC50 of 37 nM, 77 nM, 270 nM and 730 nM. Vatalanib base inhibits VEGF-induced autophosphorylation of kinase insert domain-containing receptor (KDR), endothelial cell proliferation, migration, and survival. Vatalanib base induces dose-dependent inhibition of VEGF and PDGF-induced angiogenesis in a growth factor implant model, as well as a tumor cell-driven angiogenesis. In vivo (1) Renal cell carcinoma (RCC):As a specific inhibitor of both VEGF-receptor tyrosine kinases, Vatalanib base potently inhibits tumor growth, metastases formation, and tumor vascularization in murine renal cell carcinoma. (2) MM cell lines: Vatalanib base acts both directly on MM cells and in the bone marrow microenvironment. Specifically, Vatalanib base (1-5 micro M) inhibits proliferation of MM cells by 50%. This effect of vatalanib base is dose dependent in both MM cell lines. Vatalanib base enhances the inhibitory effect of dexamethasone on growth of MM cells and can overcome the protective effect of interleukin 6 (IL-6) against dexamethasone-induced apoptosis. Vatalanib base (1 micro M) also blocks VEGF-induced migration of MM cells across an extracellular matrix. Importantly, Vatalanib base also inhibits the increased MM cell proliferation and increased IL-6 and VEGF secretion in cultures of MM cells adherent to bone marrow stem cells. (3) Malignant glioma cell lines:Early and delayed application of Vatalanib base in V(+) glioma-bearing animals resulted in a significant reduction of tumor size (71% and 36%, P (4) Models of rheumatoid arthritis:Vatalanib base treatment caused dose dependent reduction in the vascularity of the granulomatous air pouch model. Vatalanib base inhibited knee swelling by 40% in antigen-induced arthritis. category Specialty Chemicals(c26) cas_num 212141-54-3 ECHEMI Editorial ReferenceVatalanib is a member of the class of phthalazines that is phthalazine in which the hydrogens at positions 1 and 4have been replaced by a p-chlorophenylamino group and a pyridin-4-ylmethyl group, respectively. It is a multi-targeted tyrosine kinase inhibitor for all isoforms of VEGFR, PDGFR and c-Kit. It has a role as an antineoplastic agent, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an angiogenesis inhibitor and a vascular endothelial growth factor receptor antagonist. It is a member of phthalazines, a member of pyridines, a member of monochlorobenzenes and a secondary amino compound.|Vatalanib (PTK787/ZK-222584) is a new oral antiangiogenic molecule that inhibits all known vascular endothelial growth factor receptors. Vatalanib is under investigation for the treatment of solid tumors.|Vatalanib is an orally bioavailable anilinophthalazine with potential antineoplastic activity. Vatalanib binds to and inhibits the protein kinase domain of vascular endothelial growth factor receptors 1 and 2; both receptor tyrosine kinases are involved in angiogenesis. This agent also binds to and inhibits related receptor tyrosine kinases, including platelet-derived growth factor (PDGF) receptor, c-Kit, and c-Fms.Basic Info-
Product Name:
Vatalanib
Other Name:1-Phthalazinamine,N-(4-chlorophenyl)-4-(4-pyridinylmethyl)-;N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine;CGP 79787;Vatalanib;Pynasunate;Vatalinib
CAS No.:212141-54-3
Molecular Formula:C20H15ClN4
InChIKeys:InChIKey=YCOYDOIWSSHVCK-UHFFFAOYSA-N
Molecular Weight:346.81
Exact Mass:346.81
UNII:5DX9U76296
DSSTox ID:DTXSID2046919
NCI Thesaurus Code:C1868
Categories:
Characteristics-
PSA:
50.7 Ų
Density:1.330±0.06 g/cm3
Melting Point:209-212 °C
Boiling Point:587.8±50.0 °C(Predicted)
PKA:5.46±0.10
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Seller Information
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Business Type:
Manufactory
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Main Products:
Coenzymes,Inhibito,Enzymes,Zymogens,Substrates,Native Microorganism Creatine Amidinohydrolase
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Location:
Shirley, New York 11967, USA
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Payment Terms:
TT against copy of documents,D/P
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Average lead Time:
15
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Total Annual Revenue:
$1 million-$2.5 million
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Year of Establishment:
2004
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