Cediranib, Free Base (AZD2171, NSC-732208, Recentin, CAS 288383-20-0), >99%

LC Laboratories' Product Number C-4300 - Cediranib, Free Base (AZD2171, NSC-732208, Recentin, CAS 288383-20-0), >99% - for research use only. Cediranib is a highly potent inhibitor of recombinant KDR tyrosine kinase activity in vitro (IC50 < 1 nM). Inhibitory activity was also observed against the kinase associated with Flt-1 (IC50 = 5 nM), the VEGF-C and VEGF-D receptor Flt-4 (IC50 ≤ 3 nM), recombinant PDGFR-related kinase c-Kit (IC50 = 2 nM), and PDGFRβ tyrosine kinase (IC50 = 5 nM). In HUVEC, it inhibited VEGF-stimulated phosphorylation of KDR, c-Kit, PDGFR-α, PDGFR-β in a dose-dependent manner with IC50 values of 0.5, 1, 5, and 8 nM, respectively. It inhibited VEGF-stimulated HUVEC proliferation potently with an IC50 value of 0.4 nM. Consistent with potent activity against VEGF signaling, cediranib inhibited vessel branching, length, and area in vitro with IC50 values of 0.1, 0.1, and 0.2 nM, respectively. It also completely abolished VEGF-induced angiogenesis in vivo. However, it inhibited tumor cell proliferation in vitro only at comparatively high concentrations, showing IC50 values of 3.0 µM for SKOV-3 cells, 3.8 µM for MDA-MB-231 cells, 5.8 µM for PC-3 cells, 6.4 µM for Calu-6 cells, and 7.4 µM for SW620 cells. It also inhibited the growth of these five tumor models in nude mice. Furthermore, cediranib induced vascular regression in human lung tumor xenografts. Cediranib significantly increased survival of mice wth glioblastoma by decreasing tumor vessel permeability, normalizing perivascular cell coverage, and thinning of the basement membrane, thus controlling edema. Hypertension induced by cediranib is reported to be manageable. Cediranib demonstrated potent antitumor and antiangiogenic efficacy in the murine renal cell carcinoma model. Combined treatments of cediranib with radiation in Calu-6 lung xenografts induced a significantly enhanced growth delay when compared with either modality alone. Cediranib reverses ABCB1 (P-glycoprotein)- and ABCC1 (MRP1)-mediated multidrug resistance by directly inhibiting their drug efflux function. Cediranib is the active ingredient in the drug formulation designated by the trade name Recentin®. This drug has been in human clinical trials for use in patients with non-small cell lung cancer, small cell lung cancer, kidney cancer, colorectal cancer, breast cancer, liver and ovarian cancer, melanoma, mesothelioma, and glioblastoma. NOTE: The Cediranib, Free Base research compound sold by LC Laboratories is NOT Recentin®, and is NOT for human use. Related CAS numbers: 857036-77-2 for the cediranib maleate. Other CAS numbers previously assigned to cediranib, namely 557795-03-6 and 790713-41-6, have been deleted by CAS and are no longer in use.

• Supplier: LC Laboratories
• Product #: C-4300
• Sku #: C-4300_300mg