N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)
Synonym(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; mesylate; mesylate
- CAS NO.:1146618-41-8
- Empirical Formula: C19H19ClN6O4S3
- Molecular Weight: 527.03996
- MDL number: MFCD16621142
- SAFETY DATA SHEET (SDS)
- Update Date: 2023-05-18 11:31:10
What is N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)?
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.
The Uses of N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)
SNS-314 Mesylate is a potent and selective Aurora kinase inhibitor for the treatment of advanced solid tumors.
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
Properties of N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)
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. |
Safety information for N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)
Computed Descriptors for N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1)
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