[CAS NO. 288383-20-0] Cediranib (AZD2171)

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PRODUCTS SPECIFICATIONS [288383-20-0]

Catalog

SLK-S1017

Brand

Selleck

CAS

288383-20-0

DESCRIPTION [288383-20-0]

Overview

MDL	-
Molecular Weight	450.51
Molecular Formula	C25H27FN4O3
SMILES	O(C=1C2=C(C=C(OCCCN3CCCC3)C(OC)=C2)N=CN1)C=4C(F)=C5C(=CC4)NC(C)=C5

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.2197 mL	11.0985 mL	22.1971 mL
5 mM	0.4439 mL	2.2197 mL	4.4394 mL
10 mM	0.2220 mL	1.1099 mL	2.2197 mL
50 mM	0.0444 mL	0.2220 mL	0.4439 mL

Description

Cediranib (AZD2171, NSC-732208) is a highly potent inhibitor with of <1 nM, also inhibits Flt1/4 with of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3.

Targets

In vitro

Cediranib inhibits VEGF-stimulated proliferation with IC50 of 0.4 nM. Cediranib suppresses PDGF-AA with IC50 of 0.04 μM in MG63 cell lines. Cediranib has been shown to block Flt1-associated kinase with IC50 of 5 nM and VEGF-C and VEGF-D receptor Flt-4 with IC50 less than 3 nM. In addition, the IC50 values for inhibition of c-Kit and PDGFRβ tyrosine kinase are 2 nM and 5 nM respectively. Furthermore, no inhibition of enzyme activity is observed when 10 μM Cediranib is assayed with 100 μM ATP against AMPK, Chk1 Akt/PKB and others. Micromolar concentrations of Cediranib are needed to prevent tumor cell proliferation in vitro.

In vivo

Cediranib even suppresses tubule sprouting at subnanomolar concentrations and inhibits VEGF-induced angiogenesis. Cediranib causes hypertrophy in bone growth plate and prevents luteal development in ovary. These are physiological processes that are dependent upon angiogenesis. Cediranib shows broad spectrum activity in human tumor models at doses that are well tolerated. Besides, Cediranib causes regression of vascular tissues in human lung tumor xenografts.

References

[1] Wedge SR, et al. Cancer Res, 2005, 65(10), 4389-4400.
[2] Morton CL, et al. Pediatr Blood Cancer, 2012, 58(4), 566-571.

Synonyms

Quinazoline, 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]-

4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]quinazoline

4-(4-Fluoro-2-methylindol-5-yloxy)-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline

AZD 2171

Cediranib

ZD 2171

4-[(4-Fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(pyrrolidin-1-yl)propoxy]quinazoline

AZD2171

AZD-2171