Vandetanib
- CAS No.
- 443913-73-3
- Chemical Name:
- Vandetanib
- Synonyms
- CS-97;D6474;Zactima;ZD 6474;AZD6474;Vetanib;VANDETANIB;Vandetanib base;ZD6474; ZACTIMA;ZD6474;AZD-6474
- CBNumber:
- CB01011762
- Molecular Formula:
- C22H24BrFN4O2
- Molecular Weight:
- 475.35
- MOL File:
- 443913-73-3.mol
- Modify Date:
- 2024/7/23 13:47:40
| Melting point | 240-2430C |
|---|---|
| Boiling point | 538.2±50.0 °C(Predicted) |
| Density | 1.406 |
| Flash point | 279.3℃ |
| storage temp. | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| solubility | Soluble in DMSO (30 mg/ml); Ethanol (10 mg/ml with warming) |
| pka | 8.92±0.10(Predicted) |
| form | solid |
| color | White to off-white |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 1 month. |
| InChIKey | UHTHHESEBZOYNR-UHFFFAOYSA-N |
| SMILES | N1=C2C(C=C(OC)C(OCC3CCN(C)CC3)=C2)=C(NC2=CC=C(Br)C=C2F)N=C1 |
| CAS DataBase Reference | 443913-73-3 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |    GHS05,GHS07,GHS09 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Danger | |||||||||
| Hazard statements | H302-H312-H315-H318-H332-H335-H227-H410 | |||||||||
| Precautionary statements | P210-P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P310-P330-P332+P313-P362-P370+P378-P403+P233-P403+P235-P405-P501-P273 | |||||||||
| Safety Statements | 24/25 | |||||||||
| HS Code | 29333220 | |||||||||
| NFPA 704 |
|
Vandetanib Chemical Properties,Uses,Production
Description
In April 2011, the U.S. FDA approved vandetanib (ZD6474) for the treatment of symptomatic or progressive medullary thyroid cancer (MTC) in adult patients with inoperable advanced ormetastatic disease. Vandetanib inhibits KDR/VEGFR2, VEGFR3, EGFR, and RET kinases with IC50's of 40, 110, 500, and <100 nM, respectively. In athymic mice bearing MTC tumors, a 14.5-fold reduction of tumor volume was observed after 45 days of treatment with vandetanib at 50 mg/kg/day. The decrease in tumor volume was accompanied by decreases in mitotic index (Ki67) and tumor angiogenesis in treated xenografts. Key steps in the synthesis of vandetanib include the displacement of the chlorine atom from 7-benzyloxy-4-chloro-6-methoxyquinazoline with 4-bromo-2- fluoroaniline under acidic conditions in a protic solvent and a Mitsunobu reaction of a N-protected piperidine alcohol with a phenol.
Chemical Properties
Yellow Solid
Uses
Vandetanib is a once-daily oral inhibitor of vascular endothelial growth factor receptor-2 and epidermal growth factor receptor kinase activity. The activity of Vandetanib plus Docetaxel was assessed in patients with previously treated non-small-cell lung cancer (NSCLC).
General Description
Class: receptor tyrosine kinase; Treatment: RET-altered thyroid cancers; Other name: AZD-6474; Elimination half-life = 19 days; Protein binding = 90%
Clinical Use
Vandetanib, an oral VEGF, EGF, and RET receptor tyrosine kinase inhibitor, was developed by AstraZeneca for the treatment of symptomatic or aggressive medullary thyroid cancer (MTC) in patients with advanced or metastatic disease. This is the first drug approved for the treatment of MTC. Trials for other cancer indications such as small-cell lung cancer (SCLC), breast cancer, head and neck cancer, colorectal cancer, hormone-resistant prostate cancer, and papillary thyroid cancer are currently being explored. While AstraZeneca had previously developed ZD-4190 which displays similar efficacy and pharmacokinetic profile to vandetanib, vandetanib exhibited significantly improved solubility.
target
VEGFR2/RET
IC 50
Vandetanib Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | Inquiry |
|---|---|---|---|---|---|
| Apicore Pharmaceuticals Pvt Ltd | +91-2662267177 +91-2662267166 | Gujarat, India | 181 | 58 | Inquiry |
| Manus Aktteva | +91 (79) 6512-3395 | New Delhi, India | 581 | 34 | Inquiry |
| CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
| A.J Chemicals | 91-9810153283 | New Delhi, India | 6124 | 58 | Inquiry |
| Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
| SynZeal Research Pvt Ltd | +1 226-802-2078 | Gujarat, India | 6522 | 58 | Inquiry |
| Manus Aktteva Biopharma LLP | 08048250218Ext 800 | Ahmedabad, India | 655 | 58 | Inquiry |
| Clearsynth Labs | 91-22-45045900 | Maharashtra, India | 3889 | 58 | Inquiry |
| Archerchem Healthcare Pvt., Ltd. (part of Archerchem Group) | 91-22-42361111 | Maharashtra, India | 147 | 58 | Inquiry |
| CLEANCHEM LABORATORIES LLP | +91 98921 69560 | New Delhi, India | 326 | 58 | Inquiry |
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