Vandetanib
| Code | Size | Price |
|---|
| CDX-V0043-M005 | 5 mg | £41.00 |
Quantity:
| CDX-V0043-M025 | 25 mg | £102.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
AMBIENT
Storage:
+4°C
Documents
Further Information
Alternate Names/Synonyms:
N-(4-Bromo-2-fluorophenyl)-6-methoxy-7-[(1-methyl-4-piperidinyl)methoxy]-4-quinazolinamine; ZD6474; Zactima; CH 331
Appearance:
White to beige powder.
CAS:
443913-73-3
EClass:
32160000
Form (Short):
liquid
GHS Symbol:
GHS07
Handling Advice:
Protect from light and moisture.
Hazards:
H315, H319, H335
InChi:
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)
InChiKey:
UHTHHESEBZOYNR-UHFFFAOYSA-N
Long Description:
Chemical. CAS: 443913-73-3. Formula: C22H24BrFN4O2. MW: 475.4. Vandetanib is an orally available, ATP mimetic small molecule tyrosine kinases inhibitor that targets vascular endothelial growth factor receptor-2 (VEGFR-2), VEGFR-3 and epidermal growth factor receptor (EGFR), REarranged during Transfection (RET) and slightly VEGFR-1. Inhibition of these tyrosine kinases blocks multiple intracellular signaling pathways involved in tumor growth, proliferation, progression and angiogenesis. It inhibits RET, VEGFR2, VEGFR3, VEGFR1, EGFR, PDGFRbeta, Tie-2, and FGFR1 in cell-free assays (IC50s = 34, 40, 110, 1,600, 500, 1,100, 2,500, and 3,600 nM, respectively). It also binds to 142 additional kinases in a panel of 442 kinases (Kds = 4.6-7,900 nM). Vandetanib (1 and 2.5 µM) induces apoptosis, autophagy, ROS and cell cycle arrest at the G0/G1 phase and has anti-proliferative properties in several cancer cell lines and in in vivo cancer models. Formulations containing vandetanib have been used in the treatment of medullary thyroid cancer.
MDL:
MFCD07772346
Molecular Formula:
C22H24BrFN4O2
Molecular Weight:
475.4
Package Type:
Vial
Precautions:
P261, P264, P271, P280, P302+P352, P304+P340+P312, P305+P351+P338, P332+P313, P337+P313, P362, P403+P233, P405, P501
Product Description:
Vandetanib is an orally available, ATP mimetic small molecule tyrosine kinases inhibitor that targets vascular endothelial growth factor receptor-2 (VEGFR-2), VEGFR-3 and epidermal growth factor receptor (EGFR), REarranged during Transfection (RET) and slightly VEGFR-1. Inhibition of these tyrosine kinases blocks multiple intracellular signaling pathways involved in tumor growth, proliferation, progression and angiogenesis. It inhibits RET, VEGFR2, VEGFR3, VEGFR1, EGFR, PDGFRbeta, Tie-2, and FGFR1 in cell-free assays (IC50s = 34, 40, 110, 1,600, 500, 1,100, 2,500, and 3,600 nM, respectively). It also binds to 142 additional kinases in a panel of 442 kinases (Kds = 4.6-7,900 nM). Vandetanib (1 and 2.5 µM) induces apoptosis, autophagy, ROS and cell cycle arrest at the G0/G1 phase and has anti-proliferative properties in several cancer cell lines and in in vivo cancer models. Formulations containing vandetanib have been used in the treatment of medullary thyroid cancer.
Purity:
>98% (NMR)
Signal word:
Warning
SMILES:
BrC(C=C1F)=CC=C1NC2=NC=NC3=CC(OCC4CCN(C)CC4)=C(OC)C=C32
Solubility Chemicals:
Soluble in DMSO or DMF (5mg/ml).
Source / Host:
Synthetic.
Transportation:
Non-hazardous
UNSPSC Category:
Biochemical Reagents
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at +4°C.
References
(1) L.F. Hennequin, et al.; J. Med. Chem. 45, 1300 (2002) | (2) F. Carlomagno, et al.; Cancer Res. 62, 7284 (2002) | (3) S.R. Wedge, et al.; Cancer Res. 62, 4645 (2002) | (4) F. Ciardiello, et al.; Clin. Cancer Res. 9, 1546 (2003) | (5) J.N. Rich, et al.; Clin. Cancer Res. 11, 8145 (2005) | (6) S. Sathornsumetee & J.N. Rich; Drugs Today 42, 657 (2006) (Review) | (7) R.S. Herbst, et al.; Expert Opin. Investig. Drugs 16, 239 (2007) (Review) | (8) A. Morabito, et al.; Oncologist 14, 378 (2009) (Review) | (9) M.I. Davis, et al.; Nat. Biotechnol. 29, 1046 (2011) | (10) K. Inoue, et al.; Clin. Cancer Res. 18, 3924 (2012) | (11) G.M. Keating, et al.; BioDrugs 26, 431 (2012) (Review) | (12) S. Jasim, et al.; Biologics 8, 281 (2014) | (13) M.W. Sim & M.S. Cohen; Expert Opin. Drug Discov. 9, 105 (2014) (Review)