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SML3368

Sigma-Aldrich

CP-673451

≥95% (HPLC)

Synonym(s):

1-[2-[5-(2-Methoxyethoxy)-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine, 1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine, CP 673,451, CP 673451, CP-673,451, CP673,451, CP673451

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About This Item

Empirical Formula (Hill Notation):
C24H27N5O2
CAS Number:
343787-29-1
Molecular Weight:
417.50
MDL number:
MFCD11100329
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

−20°C

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

InChI key

DEEOXSOLTLIWMG-UHFFFAOYSA-N

Biochem/physiol Actions

CP-673451 is an ATP-competitive, potent and selective platelet-derived growth factor receptor inhibitor (PDGFR1 (β)/PDGFR2 (α) IC50 = 1/10 nM with 10 μM ATP; IC50 = 252 nM/c-kit, 450 nM/VEGFR-1/2; >450-fold reduced potency toward other angiogenic receptors and non-receptor kinases). CP-673451 potently inhibits PDGF-BB-induced receptor phosphorylation (IC50 = 6.4 nM; PDGFR1 transfectant) and effectively suppress human cancer xenografts-derived tumor in mice in vivo (ED50 ≤33 mg/kg via b.i.d. or q.d. p.o.) by inhibiting PDGFR phosphorylation and angiogenesis in tumor tissues.

wgk_germany

WGK 3

Certificates of Analysis (COA)

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W Gregory Roberts et al.
Cancer research, 65(3), 957-966 (2005-02-12)
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 (IC(50) = 1 nmol/L) being more than 450-fold selective for PDGFR-beta versus other angiogenic receptors (e.g., vascular endothelial growth factor receptor
Shuguang Pan et al.
American journal of translational research, 12(7), 3577-3595 (2020-08-11)
Cholangiocarcinoma (CCA) is an aggressive tumour with a poor prognosis due to its late clinical presentation and the lack of effective non-surgical therapies. Previous studies have reported that platelets are implicated in tumour invasion and metastasis, while their role and

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