Vandetanib

Description

Vandetanib · CAS 443913-73-3 · C22H24BrFN4O2. UNII YO460OQ37K. Solubility: 0.008; LogP: log Kow = 5.0.

Identification

CAS Registry Number	443913-73-3
PubChem CID	3081361
Molecular formula	C22H24BrFN4O2
IUPAC name	N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine
UNII (FDA)	YO460OQ37K

Computed Descriptors

Molecular Weight	475.4
XLogP3	4.9
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	6
Exact Mass	474.10667
Monoisotopic Mass	474.10667
Topological Polar Surface Area	59.5
Heavy Atom Count	30
Formal Charge	0

Physical & Chemical Properties

Solubility	0.008
LogP	log Kow = 5.0

Physical description & handling notes

• In water, 330 uM (pH 7.4); approx 650 uM (pH approx 6.5)
• Vandetanib solid is found to be stable to both thermal and hydrolytic degradation but a small degree of degradation is observed under stressed photolytic conditions. In solution, vandetanib is degraded under acidic, oxidative and light stress conditions but it is stable under basic conditions.
• Stable if stored as directed; avoid strong oxidizing agents
• Thermal decomposition may produce toxic gases such as carbon monoxide, carbon dioxide, and nitrogen oxides.
• Mean IC50 of approximately 2.1 μg/mL.
• Table: Vandetanib Preparations [Table#8178]

GHS Hazard Classification

Reported hazard statements	H302 (97.2%), H360 (11.1%), H373 (97.2%), H410 (97.2%)

Documented Uses

• Preparation: L. F. A. Hennequin et al., World Intellectual Property Organization patent 01032651; eidem, United States of America patent 7173038 (2001, 2007 both to AstraZeneca).
• Vandetanib is currently approved as an alternative to local therapies for both unresectable and disseminated disease. Because Vandetanib can prolong the Q-T interval, it is contraindicated for use in patients with serious cardiac complications such as congenital long QT syndrome and uncompensated heart failure.
• Vandetanib is a multi-kinase inhibitor that is used in the therapy of advanced or metastatic medullary thyroid cancer. Vandetanib therapy is commonly associated with transient elevations in serum aminotransferase during therapy, but has not been linked to cases of clinically apparent acute liver injury with jaundice.
• Breast Feeding; Lactation; Antineoplastic Agents; Enzyme Inhibitors; Protein Kinase Inhibitors; Signal Transduction Inhibitors; Tyrosine Kinase Inhibitors;
• Vandetanib is approved to treat:
• • Medullary thyroid cancer that cannot be removed by surgery and is locally advanced or has metastasized (spread to other parts of the body).

Synonyms

Vandetanib; 443913-73-3; Zactima; ZD6474; Caprelsa; N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine; N-(4-bromo-2-fluorophenyl)-6-methoxy-7-[(1-methylpiperidin-4-yl)methoxy]quinazolin-4-amine; ZD-6474; ZD 6474; GNF-PF-2188; ZD-64; NSC-744325; NSC-760766; DTXSID1046681; YO460OQ37K; N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-4-quinazolinamine

Frequently Asked Questions

What are the CAS number and molecular formula of Vandetanib?

CAS 443913-73-3; molecular formula C22H24BrFN4O2; molecular weight — g/mol.

What other names is Vandetanib known by?

Vandetanib, 443913-73-3, Zactima, ZD6474, Caprelsa, N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-((1-methylpiperidin-4-yl)methoxy)quinazolin-4-amine.

Is Vandetanib classified as hazardous?

Hazard statements reported: H302, H360, H373, H410.

What are the key physical properties of Vandetanib?

Solubility: 0.008; LogP: log Kow = 5.0.

Facts on this page are taken from PubChem (US National Library of Medicine) and Wikidata. Grade-specific data — assay, moisture, particle size, packaging, shelf life — is issued per batch on the COA and is not published here.