Synonyms: 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
Molecular Formula: C18H15ClN6OS2 · CH4O3S
Molecular Weight: 527.04
Linear Structural Formula: C18H15ClN6OS2 · CH4O3S
MDL Number: MFCD16621142
Purity: >=98% (HPLC)
Storage: -20C
Biochem Physiol Actions: 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 g i.p. dosage) and suppresses tumor growth (100 mg g ay, 5 days on, 9 days off; 150 mg g biweekly x3), as well as potentiates docetaxel antitumor efficacy in a mouse hct116 xenograft model in vivo (42.5 mg sns-314 g followed by 10 mg docetaxel g 24 hr later; biweekly x3).<>