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Merck
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Documenti fondamentali

SML3368

Sigma-Aldrich

CP-673451

≥95% (HPLC)

Sinonimo/i:

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

Formula empirica (notazione di Hill):
C24H27N5O2
Numero CAS:
343787-29-1
Peso molecolare:
417.50
Numero MDL:
MFCD11100329
Codice UNSPSC:
12352200
NACRES:
NA.77

Livello qualitativo

100

Saggio

≥95% (HPLC)

Stato

powder

Colore

white to beige

Solubilità

DMSO: 2 mg/mL, clear

Temperatura di conservazione

−20°C

Stringa SMILE

N5(CCC(CC5)N)c1c2nc(ccc2ccc1)[n]3c4c(nc3)cc(cc4)OCCOC

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
DEEOXSOLTLIWMG-UHFFFAOYSA-N

Azioni biochim/fisiol

ATP-competitive, potent and selective platelet-derived growth factor receptor (PDGFR) inhibitor against tumor growths in vivo.
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.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

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Certificati d'analisi (COA)

Lot/Batch Number
0000184176
0000175862
0000184174

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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
Yuling Xi et al.
OncoTargets and therapy, 7, 1215-1221 (2014-07-23)
Lung cancer is the leading cause of cancer mortality in the world. Although some advances in lung cancer therapy have been made, patient survival is still poor. The platelet-derived growth factor receptors (PDGFRs) and their ligands play critical roles in
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
Feng He et al.
Journal of hepatology, 72(6), 1182-1195 (2020-02-28)
Hepatomegaly can be triggered by insulin and insulin-unrelated etiologies. Insulin acts via AKT, but how other challenges cause hepatomegaly is unknown. Since many hepatomegaly-inducing toxicants and stressors activate NRF2, we examined the effect of NRF2 activation on liver size and
Lu Yang et al.
Cell death and differentiation, 27(7), 2066-2080 (2020-01-24)
Lack of insight into the identity of the cells that initiate metastasis hampers the development of antimetastatic therapies. Only a tiny fraction of tumor cells termed metastasis-initiating cells (MICs) are able to successfully seed metastases, causing recurrence and therapeutic resistance.

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