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1146618-41-8

1146618-41-8 Structure

1146618-41-8 Structure
IdentificationBack Directory
[Name]

N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)
[CAS]

1146618-41-8
[Synonyms]

SNS-314 Mesylate
SNS-314 mesylate, >=98%
SNS-314 MESYLATE; SNS314; SNS 314
M1-(3-chlorophenyl)-3-(5-(2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl)thiazol-2-yl)urea Mesylate
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
N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)
N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) ISO 9001:2015 REACH
N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) SNS-314 Mesylate
[Molecular Formula]

C19H19ClN6O4S3
[MDL Number]

MFCD16621142
[MOL File]

1146618-41-8.mol
[Molecular Weight]

527.04
Chemical PropertiesBack Directory
[storage temp. ]

-20°
[solubility ]

Soluble in DMSO (up to at least 25 mg/ml).
[form ]

solid
[color ]

Off-white
[Stability:]

Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Hazard InformationBack Directory
[Description]

SNS-314 is a pan-Aurora kinase inhibitor (IC50s = 9, 31, and 3.4 nM for Aurora A, B, and C, respectively). In a panel of 219 kinases, SNS-314 also inhibits TRKB, TRKA, FLT4, FMS, DDR2, AXL, and C-RAF (IC50s = 5-100 nM). SNS-314 inhibits Aurora B phosphorylation of histone H3 in HCT116 human colorectal carcinoma cells in vitro (EC50 = <16 nM) and in a mouse xenograft model at a dose of 50 mg/kg. It also inhibits tumor growth in A2780 ovarian, A375 melanoma, H1299 lung, MDA-MB-231 breast, and PC3 prostate cancer mouse xenograft models when administered biweekly for six weeks at a dose of 170 mg/kg.
[Uses]

SNS-314 Mesylate is a potent and selective Aurora kinase inhibitor for the treatment of advanced solid tumors.
[in vivo]

In the HCT116 human colon cancer xenograft model, administration of 50 and 100 mg/kg SNS-314 leads to dose-dependent inhibition of histone H3 phosphorylation for at least 10 h. SNS-314 shows significant tumor growth inhibition in a dose dependent manner under a variety of dosing schedules including weekly, bi-weekly, and 5 days on/9 days off[2].

[IC 50]

Aurora A: 9 nM (IC50); Aurora B: 31 nM (IC50); Aurora C: 6 nM (IC50)
[References]

1) Oslob?et al.?(2008)?Discovery of a potent and selective aurora kinase inhibitor; Bioorg. Med. Chem. Lett.?18?4880 2) Arbitrario?et al.?(2010)?SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo; Cancer Chemother. Pharmacol.?65?707 3) VanderPorten?et al.?(2009)?The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model; Mol. Cancer Ther.?8?930 4) Liu?et al.?(2017)?Targeting high Aurora kinases expression as an innovative therapy for hepatocellular carcinoma; Oncotarget?8?27953
Spectrum DetailBack Directory
[Spectrum Detail]

N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)(1146618-41-8)1HNMR
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