CP-673451

Details

Stereochemistry	ACHIRAL
Molecular Formula	C24H27N5O2
Molecular Weight	417.5035
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COCCOC1=CC=C2N(C=NC2=C1)C3=NC4=C(C=CC=C4C=C3)N5CCC(N)CC5

InChI

InChIKey=DEEOXSOLTLIWMG-UHFFFAOYSA-N

InChI=1S/C24H27N5O2/c1-30-13-14-31-19-6-7-21-20(15-19)26-16-29(21)23-8-5-17-3-2-4-22(24(17)27-23)28-11-9-18(25)10-12-28/h2-8,15-16,18H,9-14,25H2,1H3

HIDE SMILES / InChI

Molecular Formula	C24H27N5O2
Molecular Weight	417.5035
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/15705896

CP-673,451 is a potent inhibitor of platelet-derived growth factor beta-receptor (PDGFR-beta) kinase- and PDGF-BB-stimulated autophosphorylation of PDGFR-beta in cells. CP 673451 in a sponge implant model where a surgical sponge was soaked with PDGFBB to initiate angiogenesis, CP 673451 inhibited 75% of PDGF-BB-stimulated angiogenesis at a dose of 3 mg/kg for 5 days. CP 673451 did not inhibit angiogenesis induced by either VEGF or bFGF in the sponge. CP 673451 also inhibited tumour growth in H460 human lung carcinoma, Colo205 and LS174T human colon carcinomas and U87MG human glioblastoma multiforme xenograft models. CP-673,451 has not been studied in clinical trials due to issues with toxicity in preclinical studies.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Platelet-derived growth factor receptor beta 56 Target ID: CHEMBL1913 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15705896	Inhibitor 8297		1.0 nM [IC50]
Platelet-derived growth factor receptor alpha 30 Target ID: CHEMBL2007 Sources: https://www.ncbi.nlm.nih.gov/pubmed/15705896	Inhibitor 8297		10.0 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Unknown 2578

PubMed

Title	Date	PubMed
Antiangiogenic and antitumor activity of a selective PDGFR tyrosine kinase inhibitor, CP-673,451.	2005 Feb 1	15705896

Patents

Sample Use Guides

In Vivo Use Guide

Athymic female mice (CD-1 nu/nu, ~20 grams) were used for In vivo evaluation of antiangiogenesis. Animals received CP-673451 doses of 3, 10, or 33 mg/kg q.d. p.o. for 5 days. PDGF-BB-induced angiogenesis was inhibited by 70-90% following 5 daily oral doses of 3-30 mg/kg CP-673,451.

Route of Administration: Oral

In Vitro Use Guide

Porcine aortic endothelial (PAE) cells stably expressing full-length PDGFR was used for Cell-Based Phospho-PDGFR Inhibition Assay. CP-673451 was diluted in 100% DMSO, added to the cells at a final DMSO concentration of 0.25% v/v, and incubated at 370C for 10 minutes. CP-673451 (1-100nM) shows potent inhibition of PDGFR-beta phosphorylation.

Substance Class	Chemical Created by `admin` on `Sat Dec 16 08:18:38 GMT 2023` Edited by `admin` on `Sat Dec 16 08:18:38 GMT 2023`
Record UNII	0AM0WWD90A
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CP-673451

Common Name

English

4-PIPERIDINAMINE, 1-(2-(5-(2-METHOXYETHOXY)-1H-BENZIMIDAZOL-1-YL)-8-QUINOLINYL)-

Systematic Name

English

1-(2-(5-(2-METHOXYETHOXY)BENZIMIDAZOL-1-YL)QUINOLIN-8-YL)PIPERIDIN-4-YLAMINE

Systematic Name

English

Code System Code Type Description

CAS

343787-29-1