| Identification | Back Directory | [Name]
OTS964 | [CAS]
1338545-07-5 | [Synonyms]
OTS964
CS-2531
OTS964 HCl
OTS964; OTS 964
OTS964+OTS964 HCl
OTS964 HYDROCHLORIDE
(R)-9-(4-(1-(dimethylamino)propan-2-yl)phenyl)-8-hydroxy-6-methylthieno[2,3-c]quinolin-4(5H)-one
(R)-9-[4-[1-(Dimethylamino)propan-2-yl]phenyl]-8-hydroxy-6-methylthieno[2,3-c]quinolin-4(5H)-one Hydrochloride | [Molecular Formula]
C23H24N2O2S | [MDL Number]
MFCD28386220 | [MOL File]
1338545-07-5.mol | [Molecular Weight]
392.514 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
≥88.6 mg/mL in DMSO; ≥2.15 mg/mL in EtOH with gentle warming and ultrasonic; ≥2.1 mg/mL in H2O with gentle warming and ultrasonic | [form ]
crystalline solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
OTS964 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 28 nM). It specifically blocks cytokinesis, leading to apoptosis, in a broad range of cancer cells. OTS964 induces apoptosis of human lung cancer cells in mouse xenografts. | [Uses]
OTS 964 works through cytokinesis and is an effective TOPK inhibitor which has been shown to cause tumor suppression in xenografts of human cancer. | [in vivo]
OTS964 hydrochloride (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression[1].
OTS964 hydrochloride (oral administration; 50 or 100 mg/kg/day for 2 weeks) ultimately achieves complete tumor regression[1]. | Animal Model: | Nude mice bearing LU-99 lung cancer cells[1] | | Dosage: | 40 mg/kg | | Administration: | Intravenously; on days 1, 4, 8, 11, 15, and 18 | | Result: | The tumors continued shrinking even after the treatment and finally revealed complete regression.
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| Animal Model: | Nude mice bearing LU-99 lung cancer cells[1] | | Dosage: | 50 or 100 mg/kg | | Administration: | Oral administration; once every day for 2 weeks | | Result: | Achieved complete tumor regression.
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| [IC 50]
TOPK: 28 nM (IC50); CDK11B: 40 nM (Kd) | [storage]
Store at -20°C | [References]
1. matsuo y, park jh2, miyamoto t, et al. topk inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. ci transl med. 2014 oct 22;6(259):259ra145. |
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