SML2194
SNS-314 mesylate
≥98% (HPLC)
동의어(들):
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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모든 사진(1)
About This Item
실험식(Hill 표기법):
C18H15ClN6OS2 · CH4O3S
CAS Number:
Molecular Weight:
527.04
MDL number:
UNSPSC 코드:
12352200
추천 제품
분석
≥98% (HPLC)
형태
powder
저장 조건
desiccated
under inert gas
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
−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)
InChI key
FYCODPVDEFFWSR-UHFFFAOYSA-N
생화학적/생리학적 작용
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).
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point (°F)
Not applicable
Flash Point (°C)
Not applicable
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
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
Jennifer P Arbitrario et al.
Cancer chemotherapy and pharmacology, 65(4), 707-717 (2009-08-04)
The Aurora family of serine/threonine kinases (Aurora-A, Aurora-B, and Aurora-C) plays a key role in cells orderly progression through mitosis. Elevated expression levels of Aurora kinases have been detected in a high percentage of melanoma, colon, breast, ovarian, gastric, and
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.
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
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
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