OTS514 hydrochloride
Modify Date: 2024-01-12 18:30:34
OTS514 hydrochloride structure
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Common Name | OTS514 hydrochloride | ||
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| CAS Number | 2319647-76-0 | Molecular Weight | 400.92 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C21H21ClN2O2S | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of OTS514 hydrochlorideOTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells[1]. OTS514 hydrochloride induces cell cycle arrest and apoptosis[2]. |
| Name | OTS514 hydrochloride |
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| Description | OTS514 hydrochloride is a highly potent TOPK inhibitor, which inhibits TOPK kinase activity with a median inhibitory concentration (IC50) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positive cancer cells[1]. OTS514 hydrochloride induces cell cycle arrest and apoptosis[2]. |
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| Related Catalog | |
| Target |
IC50: 2.6 nM (TOPK)[1] |
| In Vitro | OTS514 (1.5625-100 nM) induces cell cycle arrest and apoptosis at nanomolar concentrations in a series of human myeloma cell lines (HMCL) and prevents outgrowth of a putative CD138+ stem cell population from multiple myeloma (MM) patient-derived peripheral blood mononuclear cells[2]. Cell Viability Assay[2] Cell Line: Human myeloma cell lines (MM1.S, MM1.R, RPMI 8226, 8226Dox40, KMS34, KMS34CFZ, KMS11, JJN3, LP-1, NCI H929, U266B1) Concentration: 1.5625, 3.125, 6.25, 12.5, 25, 50, and 100 nM Incubation Time: 72 hours Result: IC50 values ranged from 11.6 to 29.4 nM in parental cell lines, indicating a potent inhibitory effect. Only the RPMI 8226-Dox40 cell line, which overexpresses the multi-drug resistance transporter gene ABCB1, was resistant. |
| 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. |
| References |
| Molecular Formula | C21H21ClN2O2S |
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| Molecular Weight | 400.92 |
| Storage condition | -20°C |