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| | N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) Basic information |
| Product Name: | N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) | | Synonyms: | SNS-314 mesylate, >=98%;N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1);SNS-314 Mesylate;M1-(3-chlorophenyl)-3-(5-(2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl)thiazol-2-yl)urea Mesylate;N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) SNS-314 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;SNS-314 MESYLATE; SNS314; SNS 314 | | CAS: | 1146618-41-8 | | MF: | C19H19ClN6O4S3 | | MW: | 527.03996 | | EINECS: | | | Product Categories: | Inhibitors;Inhibitor | | Mol File: | 1146618-41-8.mol | ![N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) Structure](CAS/20180906/GIF/1146618-41-8.gif) |
| | N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) Chemical Properties |
| 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. |
| | N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) Usage And Synthesis |
| 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] JOHAN D. OSLOB. Discovery of a potent and selective Aurora kinase inhibitor[J]. Bioorganic & Medicinal Chemistry Letters, 2008, 18 17: Pages 4880-4884. DOI:10.1016/j.bmcl.2008.07.073 [2] JENNIFER P ARBITRARIO. SNS-314, a pan-Aurora kinase inhibitor, shows potent anti-tumor activity and dosing flexibility in vivo.[J]. Cancer Chemotherapy and Pharmacology, 2010: 707-717. DOI:10.1007/s00280-009-1076-8 [3] ERICA C VANDERPORTEN. The Aurora kinase inhibitor SNS-314 shows broad therapeutic potential with chemotherapeutics and synergy with microtubule-targeted agents in a colon carcinoma model.[J]. Molecular Cancer Therapeutics, 2009: 930-939. DOI:10.1158/1535-7163.mct-08-0754 [4] FUCHEN LIU. Targeting high Aurora kinases expression as an innovative therapy for hepatocellular carcinoma.[J]. Oncotarget, 2017: 27953-27965. DOI:10.18632/oncotarget.15853 |
| | N-(3-Chlorophenyl)-N'-[5-[2-(thieno[3,2-d]pyrimidin-4-ylamino)ethyl]-2-thiazolyl]urea methanesulfonate (1:1) Preparation Products And Raw materials |
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