OTS514 hydrochloride(1338540-63-8(free base))

SKU: orb1218359

Description

OTS514 is a highly effective TOPK(T-LAK cell-originated protein kinase) inhibitor (IC50: 2.6 nM).

Key Properties

• CAS Number: 2319647-76-0
• MW: 400.92
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₀N₂O₂S.HCl
• SMILES: Cl.C[C@@H](CN)c1ccc(cc1)-c1c(O)cc(C)c2[nH]c(=O)c3sccc3c12
• Target: TOPK
• Solubility: DMSO:10 mM

Bioactivity

• 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). Animal model: Female BALB/cSLC-nu/nu mice bearing a xenograft model of A549 cells. 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.
• 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. Cell Viability Assay 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

OTS-514 hydrochloride

Quick Database Links

Gene Symbol

TOPK