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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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1g |
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Other Sizes |
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Purity: ≥98%
Vandetanib (formerly also known as ZD6474; trade name Caprelsa) is a highly potent, orally bioavailable, and selective inhibitor of VEGFR2 with potential anticancer activity. In a test without cells, it inhibits VEGFR2 with an IC50 of 40 nM. In April 2011, the FDA approved vandetanib for the treatment of advanced thyroid cancer. Vandetanib reduces tumor vessel permeability by specifically inhibiting the tyrosine kinase activity of vascular endothelial growth factor receptor 2 (VEGF2). This prevents VEGF-stimulated endothelial cell migration and proliferation.
Targets |
VEGFR2 (IC50 = 40 nM); VEGFR3 (IC50 = 110 nM); EGFR/HER1 (IC50 = 500 nM)
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ln Vitro |
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ln Vivo |
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Enzyme Assay |
In 96-well plates coated with a poly(Glu, Ala, Tyr) 6:3:1 random copolymer substrate, vandetanib is incubated with the enzyme, 10 mM MnCl2, and 2 μM ATP. The next step is to identify phosphorylated tyrosine by sequentially incubating 2,2′-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid), a horseradish peroxidase-linked sheep antimouse immunoglobulin antibody, and a mouse IgG anti-phosphotyrosine 4G10 antibody. To investigate selectivity against tyrosine kinases linked to FGFR1, c-kit, erbB2, IGF-1R, FAK, PDGFRβ, Tie-2, and FGFR1, this methodology is modified. Appropriate ATP concentrations at or slightly below the corresponding Km (0.2–14 μM) were used in all enzyme assays (tyrosine or serine–threonine). Selectivity against serine-threonine kinases (CDK2, AKT, and PDK1) is investigated in 96-well plates using a pertinent scintillation proximity-assay (SPA). The conditions for the CDK2 assays were as follows: 10 mM MnCl2, 4.5 μM ATP, 0.15 μCi of [γ-33 P]ATP/reaction, 50 mM HEPES (pH 7.5), 1 mM DTT, 0.1 mM sodium orthovanadate, 0.1 mM sodium fluoride, 10 mM sodium glycerophosphate, 1 mg/mL BSA fraction V, and a retinoblastoma substrate (a portion of the retinoblastoma gene, 792–928, expressed in a glutathione S-transferase expression system; 0.22 μM initial concentration). The reactions are conducted at room temperature for 60 minutes and then quenched for two hours using 150 μL of a solution that contains 0.8 mg/reaction of protein A SPA-polyvinyltoluene beads, 3 μg of rabbit immunoglobulin anti-glutathione S-transferase antibody, and EDTA (62 mM final concentration). After that, the plates are sealed, centrifuged for five minutes at 1200 x g, and counted for thirty seconds using a Microplate scintillation counter.
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Cell Assay |
The MTT assay is modified to measure growth inhibition. In a nutshell, the cells are exposed to either vandetanib or gefitinib for 72 hours after being plated at a density of 2000 cells per well in 96-well plates. Triples of each assay are run. For every medication, the 50% inhibitory concentration (IC50) is calculated using the mean±standard deviation (SD).
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Animal Protocol |
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References |
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Molecular Formula |
C22H24BRFN4O2
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Molecular Weight |
475.35
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Exact Mass |
474.11
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Elemental Analysis |
C, 55.59; H, 5.09; Br, 16.81; F, 4.00; N, 11.79; O, 6.73
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CAS # |
443913-73-3
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Appearance |
Light yellow to yellow solid powder
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SMILES |
CN1CCC(CC1)COC2=C(C=C3C(=C2)N=CN=C3NC4=C(C=C(C=C4)Br)F)OC
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InChi Key |
UHTHHESEBZOYNR-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H24BrFN4O2/c1-28-7-5-14(6-8-28)12-30-21-11-19-16(10-20(21)29-2)22(26-13-25-19)27-18-4-3-15(23)9-17(18)24/h3-4,9-11,13-14H,5-8,12H2,1-2H3,(H,25,26,27)
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Chemical Name |
N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
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Synonyms |
ZD 6474; AZD-6474; ZD6474; AZD6474; CHEBI:38942; Vandetanib; ZD-6474; AZD 6474; Zactim; Caprelsa
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1037 mL | 10.5186 mL | 21.0371 mL | |
5 mM | 0.4207 mL | 2.1037 mL | 4.2074 mL | |
10 mM | 0.2104 mL | 1.0519 mL | 2.1037 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01496313 | Active Recruiting |
Drug: 300mg vandetanib Drug: 150mg vandetanib |
Thyroid Cancer | Genzyme, a Sanofi Company/td> | August 28, 2012 | Phase 4 |
NCT01582191 | Active Recruiting |
Drug: Vandetanib Drug: Everolimus |
Advanced Malignant Neoplasm Metastatic Malignant Neoplasm |
M.D. Anderson Cancer Center | May 14, 2012 | Phase 1 |
NCT00537095 | Active Recruiting |
Drug: Vandetanib Other: Placebo |
Thyroid Neoplasms | Genzyme, a Sanofi Company | September 29, 2007 | Phase 2 |
NCT04211337 | Active Recruiting |
Drug: Selpercatinib Drug: Vandetanib |
Medullary Thyroid Cancer | Loxo Oncology, Inc. | February 11, 2020 | Phase 3 |
NCT00410761 | Active Recruiting |
Drug: ZD6474 (Vandetanib) |
Thyroid Cancer | Genzyme, a Sanofi Company | November 30, 2006 | Phase 3 |
Inhibitory effects of vandetanib on cell proliferation, and phosphorylation of VEGFR-2 and EGFR. Clin Cancer Res . 2012 Jul 15;18(14):3924-33. td> |
Serial changes in tumor growth induced by treatment with vandetanib in mice carrying subcutaneously implanted human hepatoma cell tumors. Clin Cancer Res . 2012 Jul 15;18(14):3924-33. td> |
Vandetanib inhibits tumor growth in the liver in nude mice. Clin Cancer Res . 2012 Jul 15;18(14):3924-33. td> |
Beneficial effects of vandetanib on the survival time and the intrahepatic metastasis in mice implanted with KYN-2 cells. Clin Cancer Res . 2012 Jul 15;18(14):3924-33. td> |