OTS514 Hydrochloride

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CAS NO:

2319647-76-0

OTS5144 hydrochloride 是一种高效的TOPK抑制剂，IC₅₀为 2.6 nM。OTS514 hydrochloride 强效抑制 TOPK 阳性的肿瘤细胞生长。OTS514 hydrochloride 诱导细胞周期停滞和凋亡 (apoptosis)。

生物活性

OTS514 hydrochloride is a highly potentTOPKinhibitor, which inhibitsTOPKkinase activity with a median inhibitory concentration (IC₅₀) value of 2.6 nM. OTS514 hydrochloride strongly suppresses the growth of TOPK-positivecancercells^[1]. OTS514 hydrochloride induces cell cycle arrest andapoptosis^[2].

IC₅₀& Target

IC50: 2.6 nM (TOPK)^[1]

体外研究
(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:	IC₅₀values 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.

体内研究
(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.

分子量

400.92

Formula

C₂₁H₂₁ClN₂O₂S

CAS 号

2319647-76-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.