OTS514 HCl | TOPK inhibitor | CAS#1338540-63-8

MedKoo Cat#: 558256 | Name: OTS514 HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

OTS514 is a potent TOPK (T-LAK cell-originated protein kinase) inhibitor. OTS514 exhibits growth suppressive effect on small cell lung cancer. TS514 effectively suppressed growth of SCLC cell lines (IC50 ; 0.4 ~ 42.6 nM) and led to their apoptotic cell death. Treatment with OTS514 suppressed forkhead box protein M1 (FOXM1) activity, which was involved in stemness of CSC. Furthermore, OTS514 treatment reduced CD90-positive SCLC cells and showed higher cytotoxic effect against lung sphere-derived CSC-like SCLC cells.

Chemical Structure

OTS514 HCl

CAS#2319647-76-0 (HCl)

Theoretical Analysis

MedKoo Cat#: 558256

Name: OTS514 HCl

CAS#: 2319647-76-0 (HCl)

Chemical Formula: C21H21ClN2O2S

Exact Mass: 0.0000

Molecular Weight: 400.92

Elemental Analysis: C, 62.91; H, 5.28; Cl, 8.84; N, 6.99; O, 7.98; S, 8.00

Price and Availability

Size	Price	Availability
50mg	USD 750.00	2 Weeks
100mg	USD 1,250.00	2 Weeks
200mg	USD 1,950.00	2 Weeks
500mg	USD 2,950.00	2 Weeks
1g	USD 4,650.00	2 Weeks

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Related CAS #

1338540-63-8 (free base) 1338544-87-8 (HBr) 1338541-25-5 (s-isomer) 1338545-92-8 (S-isomer HCl) 2319647-76-0 (HCl)

Synonym

OTS514; OTS 514; OTS-514; OTS514 HCl, OTS514 Hydrochloride.

IUPAC/Chemical Name

9-[4-[(1R)-2-amino-1-methylethyl]phenyl]-8-hydroxy-6-methyl-thieno[2,3-c]quinolin-4(5H)-one hydrochloride

InChi Key

CQPRMBOOBXSZSP-YDALLXLXSA-N

InChi Code

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

SMILES Code

O=C1NC2=C(C(C3=CC=C([C@@H](C)CN)C=C3)=C(O)C=C2C)C4=C1SC=C4.[H]Cl

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Product Data

Product Data

Instruction

View handling instruction

Biological target:

OTS514 is a potent TOPK (T-LAK cell-originated protein kinase) inhibitor.

In vitro activity:

OTS514 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 MM patient-derived peripheral blood mononuclear cells. In bone marrow cells from MM patients, OTS514 treatment exhibited preferential killing of the malignant CD138+ plasma cells compared with the CD138- compartment. Reference: Cancer Med. 2020 Jan;9(1):324-334. https://pubmed.ncbi.nlm.nih.gov/31714026/

In vivo activity:

Using the peritoneal dissemination model of ES-2 ovarian cancer cells, this study examined the in vivo efficacy of OTS514. Oral administration of OTS514 significantly elongated overall survival in the ES-2 abdominal dissemination xenograft model, compared with vehicle control (P < 0.001). Reference: Clin Cancer Res. 2016 Dec 15;22(24):6110-6117. https://pubmed.ncbi.nlm.nih.gov/27334838/

	Solvent	mg/mL	mM
Solubility
	DMSO	80.0	199.54
	Ethanol	5.0	12.47
	Water	80.0	199.54

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 400.92 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. Kato M, Ota A, Ono T, Karnan S, Hyodo T, Rahman ML, Hasan MN, Onda M, Kondo S, Ito K, Furuhashi A, Hayashi T, Konishi H, Tsuzuki S, Hosokawa Y, Kazaoka Y. PDZ-binding kinase inhibitor OTS514 suppresses the proliferation of oral squamous carcinoma cells. Oral Dis. 2023 Feb 17. doi: 10.1111/odi.14533. Epub ahead of print. PMID: 36799330. 2. Stefka AT, Johnson D, Rosebeck S, Park JH, Nakamura Y, Jakubowiak AJ. Potent anti-myeloma activity of the TOPK inhibitor OTS514 in pre-clinical models. Cancer Med. 2020 Jan;9(1):324-334. doi: 10.1002/cam4.2695. Epub 2019 Nov 12. PMID: 31714026; PMCID: PMC6943155. 3. Ota A, Hanamura I, Karnan S, Inaguma S, Takei N, Lam VQ, Mizuno S, Kanasugi J, Wahiduzzaman M, Rahman ML, Hyodo T, Konishi H, Tsuzuki S, Ikeda H, Takami A, Hosokawa Y. Novel Interleukin-6 Inducible Gene PDZ-Binding Kinase Promotes Tumor Growth of Multiple Myeloma Cells. J Interferon Cytokine Res. 2020 Aug;40(8):389-405. doi: 10.1089/jir.2020.0111. Epub 2020 Jul 23. PMID: 32721246; PMCID: PMC7462034. 4. Ikeda Y, Park JH, Miyamoto T, Takamatsu N, Kato T, Iwasa A, Okabe S, Imai Y, Fujiwara K, Nakamura Y, Hasegawa K. T-LAK Cell-Originated Protein Kinase (TOPK) as a Prognostic Factor and a Potential Therapeutic Target in Ovarian Cancer. Clin Cancer Res. 2016 Dec 15;22(24):6110-6117. doi: 10.1158/1078-0432.CCR-16-0207. Epub 2016 Jun 22. PMID: 27334838.

In vitro protocol:

In vivo protocol:

1. Ota A, Hanamura I, Karnan S, Inaguma S, Takei N, Lam VQ, Mizuno S, Kanasugi J, Wahiduzzaman M, Rahman ML, Hyodo T, Konishi H, Tsuzuki S, Ikeda H, Takami A, Hosokawa Y. Novel Interleukin-6 Inducible Gene PDZ-Binding Kinase Promotes Tumor Growth of Multiple Myeloma Cells. J Interferon Cytokine Res. 2020 Aug;40(8):389-405. doi: 10.1089/jir.2020.0111. Epub 2020 Jul 23. PMID: 32721246; PMCID: PMC7462034. 2. Ikeda Y, Park JH, Miyamoto T, Takamatsu N, Kato T, Iwasa A, Okabe S, Imai Y, Fujiwara K, Nakamura Y, Hasegawa K. T-LAK Cell-Originated Protein Kinase (TOPK) as a Prognostic Factor and a Potential Therapeutic Target in Ovarian Cancer. Clin Cancer Res. 2016 Dec 15;22(24):6110-6117. doi: 10.1158/1078-0432.CCR-16-0207. Epub 2016 Jun 22. PMID: 27334838.

1: Ikeda Y, Park JH, Miyamoto T, Takamatsu N, Kato T, Iwasa A, Okabe S, Imai Y, Fujiwara K, Nakamura Y, Hasegawa K. T-LAK Cell-Originated Protein Kinase (TOPK) as a Prognostic Factor and a Potential Therapeutic Target in Ovarian Cancer. Clin Cancer Res. 2016 Dec 15;22(24):6110-6117. PubMed PMID: 27334838. 2: Park JH, Inoue H, Kato T, Zewde M, Miyamoto T, Matsuo Y, Salgia R, Nakamura Y. TOPK (T-LAK cell-originated protein kinase) inhibitor exhibits growth suppressive effect on small cell lung cancer. Cancer Sci. 2017 Jan 11. doi: 10.1111/cas.13160. [Epub ahead of print] PubMed PMID: 28075524. 3: Kato T, Inoue H, Imoto S, Tamada Y, Miyamoto T, Matsuo Y, Nakamura Y, Park JH. Oncogenic roles of TOPK and MELK, and effective growth suppression by small molecular inhibitors in kidney cancer cells. Oncotarget. 2016 Apr 5;7(14):17652-64. doi: 10.18632/oncotarget.7755. PubMed PMID: 26933922; PubMed Central PMCID: PMC4951240. 4: Alachkar H, Mutonga M, Malnassy G, Park JH, Fulton N, Woods A, Meng L, Kline J, Raca G, Odenike O, Takamatsu N, Miyamoto T, Matsuo Y, Stock W, Nakamura Y. T-LAK cell-originated protein kinase presents a novel therapeutic target in FLT3-ITD mutated acute myeloid leukemia. Oncotarget. 2015 Oct 20;6(32):33410-25. doi: 10.18632/oncotarget.5418. PubMed PMID: 26450903; PubMed Central PMCID: PMC4741775.