Cediranib | VEGFR inhibitor

CAS:
 288383-20-0
Catalog Number:
 10-4142
Cediranib chemical structure

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Cediranib (288383-20-0) is a highly potent (IC50 =  <1 nM) inhibitor of VEGFR-2.1 It also inhibits VEGFR-1, VEGFR-3, c-Kit, and PDGFRß (IC50s respectively: 5 nM, 3 nM, 2nM, and 5 nm). It displays broad-spectrum activity in various human tumor models. Cediranib normalized tumor vasculature decreasing permeability, increasing blood perfusion, and allowing better drug delivery in glioblastoma patients.2,3 It enhanced transcription of MHC-I leading to enhanced CD8+ T cell infiltration and improved efficacy of anti-PD-L1 therapy.4

References/Citations:

  1. Wedge et al. (2005), AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer; Cancer Res. 65 4389
  2. Sorensen et al. (2011), Increased Survival in Glioblastoma Patients to Anti-angiogenic Therapy with Elevated Blood Perfusion; Cancer Res. 72 402
  3. Batchelor et al. (2013), Increased tumor oxygenation and survival in glioblastoma patients who shoe increased blood perfusion after cediranib and chemoradiation; Proc. Natl. Acad. Sci. USA 110 19059
  4. Zhang et al. (2024), Cediranib enhances the transcription of MHC-I by upregulating IRF-1; Biochem. Pharmacol. 221 116036
288383-20-0, AZD-2171, AZD2171, AZD2171 supplier, cediranib, Cediranib supplier
CAS:
288383-20-0
Catalog Number:
10-4142
Activity:
VEGFR inhibitor
Chemical Names:
4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline
Alternate Name:
AZD2171
Molecular Weight:
450.51
Molecular Formula:

C25H27FN4O3

Solubility:
Soluble in DMSO (20 mg/ml)
Physical Properties:
Beige solid
Purity:

>98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

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Product Data Sheet:

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Cediranib (288383-20-0) is a highly potent (IC50 =  <1 nM) inhibitor of VEGFR-2.1 It also inhibits VEGFR-1, VEGFR-3, c-Kit, and PDGFRß (IC50s respectively: 5 nM, 3 nM, 2nM, and 5 nm). It displays broad-spectrum activity in various human tumor models. Cediranib normalized tumor vasculature decreasing permeability, increasing blood perfusion, and allowing better drug delivery in glioblastoma patients.2,3 It enhanced transcription of MHC-I leading to enhanced CD8+ T cell infiltration and improved efficacy of anti-PD-L1 therapy.4

References/Citations:

  1. Wedge et al. (2005), AZD2171: a highly potent, orally bioavailable, vascular endothelial growth factor receptor-2 tyrosine kinase inhibitor for the treatment of cancer; Cancer Res. 65 4389
  2. Sorensen et al. (2011), Increased Survival in Glioblastoma Patients to Anti-angiogenic Therapy with Elevated Blood Perfusion; Cancer Res. 72 402
  3. Batchelor et al. (2013), Increased tumor oxygenation and survival in glioblastoma patients who shoe increased blood perfusion after cediranib and chemoradiation; Proc. Natl. Acad. Sci. USA 110 19059
  4. Zhang et al. (2024), Cediranib enhances the transcription of MHC-I by upregulating IRF-1; Biochem. Pharmacol. 221 116036

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