SML2194

SNS-314 mesylate

≥98% (HPLC)

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₈H₁₅ClN₆OS₂ · CH₄O₃S
• Numer CAS: 1146618-41-8
• Masa cząsteczkowa: 527.04
• Numer MDL: MFCD16621142
• Kod UNSPSC: 12352200

Właściwości

• Próba: ≥98% (HPLC)
• Postać: powder
• warunki przechowywania: desiccated; under inert gas
• kolor: white to beige
• rozpuszczalność: DMSO: 2 mg/mL, clear
• temp. przechowywania: −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)
• Klucz InChI: FYCODPVDEFFWSR-UHFFFAOYSA-N

Opis

Działania biochem./fizjol.

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).

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Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable