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Autres documents

SML2194

Sigma-Aldrich

SNS-314 mesylate

≥98% (HPLC)

Synonyme(s) :

1-(3-Chlorophenyl)-3-(5-(2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl)thiazol-2-yl)urea methanesulfonate, N-(3-Chlorophenyl)-N′-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate, SNS 314, SNS 314 mesylate, SNS314, SNS314 mesylate

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About This Item

Formule empirique (notation de Hill):
C18H15ClN6OS2 · CH4O3S
Numéro CAS:
1146618-41-8
Poids moléculaire :
527.04
Numéro MDL:
MFCD16621142
Code UNSPSC :
12352200

Pureté

≥98% (HPLC)

Forme

powder

Conditions de stockage

desiccated
under inert gas

Couleur

white to beige

Solubilité

DMSO: 2 mg/mL, clear

Température de stockage

−20°C

InChI

1S/C18H15ClN6OS2.CH4O3S/c19-11-2-1-3-12(8-11)24-17(26)25-18-21-9-13(28-18)4-6-20-16-15-14(5-7-27-15)22-10-23-16;1-5(2,3)4/h1-3,5,7-10H,4,6H2,(H,20,22,23)(H2,21,24,25,26);1H3,(H,2,3,4)

Clé InChI

FYCODPVDEFFWSR-UHFFFAOYSA-N

Actions biochimiques/physiologiques

Potent and selective pan-aurora kinase inhibitor that binds aurora kinase in the DFG-in conformation and exhibits anticancer efficacy in vitro and in vivo.
SNS-314 is a potent pan-aurora kinases inhibitor (IC50 = 9/31/3 nM against aurora kinase A/B/C or aurora 2/1/3) that binds aurora kinase in the DFG-in conformation and exhibits great selectivity against a panel of 219 kinases (>5-, >12-, >14-, >15-, >82-, >84-fold selectivity for aurora A over TrkB, TrkA, Flt4, Fms, DDR2, Axl, respectively; >100-fold selectivity over c-Raf and the remaining kinases). SNS-314 downregulates cellular histone H3 Ser10 (HH3 Ser10) phosphorylation (IC50 <16 nM) and exhibits potent antiproliferation activity in HCT116 human colon cancer cultures in vitro (IC50 = 5 nM). When applied in vivo, HCT116 likewise reduces pHH3 (Ser10) level in tumor tissue (by 75-100% 6 hrs post 50 mg/kg i.p. dosage) and suppresses tumor growth (100 mg/kg/day, 5 days on, 9 days off; 150 mg/kg biweekly x3), as well as potentiates docetaxel antitumor efficacy in a mouse HCT116 xenograft model in vivo (42.5 mg SNS-314/kg followed by 10 mg docetaxel/kg 24 hr later; biweekly x3).

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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Consulter la Bibliothèque de documents

Fuchen Liu et al.
Oncotarget, 8(17), 27953-27965 (2017-04-22)
The Aurora kinases A and B control tumorigenesis by inhibiting apoptosis and promoting proliferation and metastasis, however, it remains unknown whether Aurora A and B overexpressed concomitantly and its clinical significance in hepatocellular carcinoma (HCC). Here, we obsearved Aurora A
Vincenzo Quagliariello et al.
Journal of cellular physiology, 231(8), 1784-1795 (2015-12-15)
The aim of this paper is based on the use of a hyaluronic acid hydrogel of Quercetin tested alone and in combination to an inhibitor of Aurora Kinase type A and B (SNS-314) on human medullary and papillary thyroid cancer
Johan D Oslob et al.
Bioorganic & medicinal chemistry letters, 18(17), 4880-4884 (2008-08-06)
This communication describes the discovery of a novel series of Aurora kinase inhibitors. Key SAR and critical binding elements are discussed. Some of the more advanced analogues potently inhibit cellular proliferation and induce phenotypes consistent with Aurora kinase inhibition. In
Raffaele Pezzani et al.
Investigational new drugs, 34(5), 531-540 (2016-05-15)
New therapeutic targets are needed to fight cancer. Aurora kinases (AK) were recently identified as vital key regulators of cell mitosis and have consequently been investigated as therapeutic targets in preclinical and clinical studies. Aurora kinase inhibitors (AKI) have been
Antonella Antignani et al.
PloS one, 11(8), e0161415-e0161415 (2016-08-25)
The intersection of small molecular weight drugs and antibody-based therapeutics is rarely studied in large scale. Both types of agents are currently part of the cancer armamentarium. However, very little is known about how to combine them in optimal ways.
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