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Cediranib Maleate

Cediranib Maleate structure

CAS No:
857036-77-2
Formula:
C29H31FN4O7
Chemical Name:
Cediranib Maleate
Synonyms:
Cediranib Maleate;AZD 2171 Maleate;West to Ni BuMa Maleate;Cediranib Maleate(AZD-2171)
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

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

Cediranib Maleate is the maleate salt of an indole ether quinazoline derivative with antineoplastic activities. Competing with adenosine triphosphate, cediranib binds to and inhibits all three vascular endothelial growth factor receptor (VEGFR-1,-2,-3) tyrosine kinases, thereby blocking VEGF-signaling, angiogenesis, and tumor cell growth.

Cediranib Maleate Basic Attributes

Molecular Weight：

566.586

Exact Mass：

566.21800

UNII：

68AYS9A614

NSC Number：

732208

NCI Thesaurus Code：

C48379

Characteristics

PSA：

147

XLogP3：

4.87390

Melting Point：

198.3-200.08 °C (polymorph)

Safety Information

Precautionary statement(s)：

P201, P202, P260, P264, P270, P273, P281, P301+P310, P308+P313, P314, P321, P330, P391, P405, P501

Hazard Statements：

H301

Drug Information

Drug Indication：

Treatment of high-grade glioma

Cediranib Maleate 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 -> EU pediatric investigation plans

Computed Properties

Molecular Weight:566.6
Hydrogen Bond Donor Count:3
Hydrogen Bond Acceptor Count:11
Rotatable Bond Count:10
Exact Mass:566.21767750
Monoisotopic Mass:566.21767750
Topological Polar Surface Area:147
Heavy Atom Count:41
Complexity:743
Defined Bond Stereocenter Count:1
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes