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. OTS514 hydrochloride induces cell cycle arrest and apoptosis.

Product information

CAS Number: 2319647-76-0

Molecular Weight: 400.92

Formula: C21H21ClN2O2S

Chemical Name: 9-{4-[(2R)-1-aminopropan-2-yl]phenyl}-8-hydroxy-6-methyl-4H,5H-thieno[2,3-c]quinolin-4-one; chlorohydrogen

Smiles: Cl.CC1=CC(O)=C(C2=C1NC(=O)C1SC=CC=12)C1C=CC(=CC=1)[C@@H](C)CN

InChiKey: CQPRMBOOBXSZSP-YDALLXLXSA-N

InChi: InChI=1S/C21H20N2O2S.ClH/c1-11-9-16(24)17(14-5-3-13(4-6-14)12(2)10-22)18-15-7-8-26-20(15)21(25)23-19(11)18;/h3-9,12,24H,10,22H2,1-2H3,(H,23,25);1H/t12-;/m0./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: 10 mM in DMSO

Shipping Condition: Shipped under ambien...

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

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.

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).

References:

1. Kato T, et al. Oncotarget. 2016, 7(14):17652-64.
2. Matsuo Y, et al. Sci Transl Med. 2014, 6(259):259ra145.

Products are for research use only. Not for human use.