| Identification | Back Directory | [Name]
OTS514 | [CAS]
1338540-63-8 | [Synonyms]
CS-2532
OTS514 HCl
OTS514;OTS 514;OTS-514
9-[4-[(1R)-2-Amino-1-methylethyl]phenyl]-8-hydroxy-6-methylthieno[2,3-c]quinolin-4(5H)-one
Thieno[2,3-c]quinolin-4(5H)-one, 9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl- | [EINECS(EC#)]
604-604-1 | [Molecular Formula]
C21H20N2O2S | [MDL Number]
MFCD29924710 | [MOL File]
1338540-63-8.mol | [Molecular Weight]
364.46 |
| Questions And Answer | Back Directory | [Uses]
OTS514 is a potent T-lymphokine-activated killer cell-originated protein kinase (TOPK) inhibitor. TOPK is involved with cancer cell proliferation and cancer stem cell maintenance. OTS514 also downregulates the oncogenic transcriptional factor, forkhead box protein M1 (FOXM1). |
| Chemical Properties | Back Directory | [Boiling point ]
501.3±50.0 °C(Predicted) | [density ]
1.293±0.06 g/cm3(Predicted) | [solubility ]
DMF: 30 mg/ml; DMSO: 30 mg/ml; DMSO:PBS (pH 7.2) (1:2): 0.25 mg/ml | [form ]
A crystalline solid | [pka]
9.35±0.20(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [in vivo]
OTS514 (1-5 mg/kg; once a day for 2 weeks; intravenous administration) induces tumor regression in a xenograft model of A549 cells (TOPK-positive lung cancer cells)[1]. | Animal Model: | Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells[1] | | Dosage: | 1, 2.5, and 5 mg/kg | | Administration: | Intravenously treated; once every day for 2 weeks | | Result: | Resulted in tumor growth inhibition (TGI) of 5.7, 43.3, and 65.3% on day 15, respectively, without any body weight loss. |
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