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Merck
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Key Documents

Autres documents

SML2572

Sigma-Aldrich

AZM475271

≥98% (HPLC)

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About This Item

Formule empirique (notation de Hill):
C23H27ClN4O3
Numéro CAS:
476159-98-5
Poids moléculaire :
442.94
Numéro MDL:
MFCD19690925
Code UNSPSC :
12352200

Pureté

≥98% (HPLC)

Forme

powder

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

−20°C

Chaîne SMILES 

ClC1=CC=C(C=C1NC2=NC=NC3=CC(OCC4CCN(CC4)C)=C(C=C32)OC)OC

InChI

1S/C23H27ClN4O3/c1-28-8-6-15(7-9-28)13-31-22-12-19-17(11-21(22)30-3)23(26-14-25-19)27-20-10-16(29-2)4-5-18(20)24/h4-5,10-12,14-15H,6-9,13H2,1-3H3,(H,25,26,27)

Clé InChI

WPOXAFXHRJYEIC-UHFFFAOYSA-N

Actions biochimiques/physiologiques

AZM475271 (M475271) is an orally active, potent and selective inhibitor against src family kinases src and yes (IC50 = 25 nM & 10 nM, respectively; lck/VEGFR2/EGFR/csk/FGFR1 IC50 = 0.2/0.5/0.6/7.6/∼20 μM) that effectively suppresses src-dependent cellular signaling events (26%/48% inhibition of 50 ng/mL VEGF-induced HUVEC proliferation/migration at 100 nM; 31%/72% inhibition of 10 ng/mL VEGF-induced Flk-1/Src phosphorylation in HUVECs at 300 nM) and exbihits anticancer efficacy both in cultures (70% PC-9/30% A549 proliferation inhibition at 1 μM) and in vivo (78%/100% PC-9 tumor growth suppression in mice via 10/50 mg/kg/day p.o.).

Code de la classe de stockage

11 - Combustible Solids

Classe de danger pour l'eau (WGK)

WGK 3

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable

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Rui Zheng et al.
Clinical & experimental metastasis, 22(3), 195-204 (2005-09-15)
Src, a proto-oncogene, has been strongly implicated in the growth, progression and metastasis of a number of human cancers. Its role in lung cancer is, however, still unknown. In the present study, we assessed the expression of Src in three
Yacine Merrouche et al.
Oncotarget, 7(33), 53350-53361 (2016-07-28)
Estrogen receptor-, progesterone receptor- and HER2-negative breast cancers, also known as triple-negative breast cancers (TNBCs), have poor prognoses and are refractory to current therapeutic agents, including epidermal growth factor receptor (EGFR) inhibitors. Resistance to anti-EGFR therapeutic agents is often associated
Suhrid Banskota et al.
PloS one, 11(1), e0148133-e0148133 (2016-01-30)
5-Hydroxytryptamine (5-HT) induces proliferation of cancer cells and vascular cells. In addition to 5-HT production by several cancer cells including gastrointestinal and breast cancer, a significant level of 5-HT is released from activated platelets in the thrombotic environment of tumors
Christine Rivat et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 17(12), 1721-1723 (2003-09-06)
The matrix metalloprotease matrilysin is expressed in premalignant polyps and plays a key role in local invasion during the progression of digestive tumors. In the present work, we investigated the possible relationships between the activity of the mouse and human
Tobias Bartscht et al.
Anti-cancer agents in medicinal chemistry, 17(7), 966-972 (2016-09-28)
Earlier results from our group have shown that in pancreatic ductal adenocarcinoma (PDAC)-derived cells transforming growth factor (TGF)-β1-dependent epithelial-mesenchymal transition (EMT) and cell motility was inhibited by the Src inhibitors PP2 and PP1 both of which targeted the TGF-β receptors
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