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MedKoo Cat#: 558256 | Name: OTS514 HCl
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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
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 Quantity
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.

Recalculate based on batch purity %
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:
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.
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.