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Cediranib

Cediranib structure

CAS No:
288383-20-0
Formula:
C25H27FN4O3
Chemical Name:
Cediranib
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;790713-41-6;557795-03-6
Categories:
Active Pharmaceutical Ingredients > Antineoplastic Agents

Description

Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.

4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]quinazoline is an aromatic ether.|The novel indole-ether quinazoline Cediranib is a highly potent (IC50 < 1 nmol/L) ATP-competitive inhibitor of recombinant KDR tyrosine kinase in vitro. It is being developed clinically as a once-daily oral therapy for the treatment of cancer.

Cediranib Basic Attributes

Molecular Weight：

450.51

Exact Mass：

450.51

EC Number：

1308068-626-2

UNII：

NQU9IPY4K9

DSSTox ID：

DTXSID10183035

ATC Code：

L - Antineoplastic and immunomodulating agents

Characteristics

PSA：

72.5

XLogP3：

4.9

Density：

1.3±0.1 g/cm3

Boiling Point：

626.557°C at 760 mmHg

Flash Point：

332.7±31.5 °C

Refractive Index：

1.642

Safety Information

Precautionary statement(s)：

P201, P202, P260, P264, P270, P273, P280, P281, P301+P310, P302+P352, P308+P313, P312, P314, P321, P322, P330, P332+P313, P362, P363, P391, P405, P501

Hazard Statements：

H301

GHS Classification：

|Danger|H301 (100%): Toxic if swallowed [Danger Acute toxicity, oral]|P201, P202, P260, P264, P270, P273, P280, P281, P301+P310, P302+P352, P308+P313, P312, P314, P321, P322, P330, P332+P313, P362, P363, P391, P405, and P501|Aggregated GHS information provided by 5 companies from 3 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Drug Indication：

For the treatment of liver cancer, advanced non-small cell lung cancer (NSCLC), advanced colorectal cancer (CRC) and other solid tumors.

Pharmacology：

Cediranib is a once-daily, orally available, highly potent and selective VEGF signalling inhibitor that inhibits all three VEGF receptors. The preclinical profile of Cediranib indicates that it has the potential to be the 'best in class' VEGF signalling inhibitor. Phase I data indicate that Cediranib is generally well tolerated, with the most common dose related adverse events being diarrhoea, hoarseness, headache and hypertension.

MeSH：

Substances that inhibit or prevent the proliferation of NEOPLASMS. (See all compounds classified as Antineoplastic Agents.)|Agents that inhibit PROTEIN KINASES. (See all compounds classified as Protein Kinase Inhibitors.)

Absorption：

Available following oral administration.

Biological Half-Life：

12 to 35 hours

Mechanism of Action：

Cediranib inhibits vacular endothelial growth factor (VEGF) receptor tyrosine kinase (RTK). By forming a blockade at the VEGF receptors, Cediranib limits the growth of new blood vessels, which are essential to supporting tumor growth. Thus, lacking sufficient blood supply, tumor cells become starved for nutrients, slowing or halting growth and potentially improving the efficacy of other treatments. Preclinical evidence indicated that the drug had a high affinity at these sites, and was well tolerated and efficacious in animal studies.

MeSH Entry Terms：

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

Cediranib Use and Manufacturing

Uses

Cediranib (AZD2171) inhibited VEGF-stimulated proliferation and KDR phosphorylation with IC50 of 0.4 and 0.5 nM, respectively.

Use Classification：

Human drugs -> Rare disease (orphan)

Computed Properties

Molecular Weight:450.5
XLogP3:4.9
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:7
Rotatable Bond Count:8
Exact Mass:450.20671890
Monoisotopic Mass:450.20671890
Topological Polar Surface Area:72.5
Heavy Atom Count:33
Complexity:625
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes

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