OTS-964


Catalog No. size PriceQuantity
M6621-2 2mg solid $90
M6621-10 10mg solid $360

Description

Cas:1338545-07-5

Product Information:

OTS964 is a potent and selective TOPK inhibitor with potential anticancer activity. OTS964 inhibits TOPK kinase activity with high affinity and selectivity. Similar to the knockdown effect of TOPK small interfering RNAs (siRNAs), this inhibitor causes a cytokinesis defect and the subsequent apoptosis of cancer cells in vitro as well as in xenograft models of human lung cancer. Although administration of the free compound induced hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis), the drug delivered in a liposomal formulation effectively caused complete regression of transplanted tumors without showing any adverse reactions in mice. ( Sci Transl Med. 2014 Oct 22;6(259):259ra145. )

 

Chemical Formula: 23H25ClN2O2S

 

Molecular Weight: 428.975

 

Elemental Analysis: C, 64.40; H, 5.87; Cl, 8.26; N, 6.53; O, 7.46; S, 7.47

 

Synonym:

 

OTS964

OTS964

OTS 964

OTS964 HCl

OTS964 hydrochloride

 

Chemical Name: (R)-9-(4-(1-(dimethylamino)propan-2-yl)phenyl)-8-hydroxy-6-methylthieno[2,3-c]quinolin-4(5H)-one hydrochloride

 

InChi Key:

YHPWOYBWUWSJDW-UQKRIMTDSA-N

 

InChi Code: InChI=1S/C23H24N2O2S.ClH/c1-13-11-18(26)19(16-7-5-15(6-8-16)14(2)12-25(3)4)20-17-9-10-28-22(17)23(27)24-21(13)20;/h5-11,14,26H,12H2,1-4H3,(H,24,27);1H/t14-;/m0./s1

 

Smiles Code:

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

 

 

Technical Data:

 

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, not in water

Shelf Life: >5 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

 

In Vitro

OTS964 hydrochloride (10 nM; 48 hours) suppresses cancer cell proliferation.

OTS964 hydrochloride (10 nM; 48 hours) increases cancer cell death.

OTS964 (0.1-2 μM; 24 and 48 hours) increases the expression of LC3-II and decreases the expression of P62, both in a dose-dependent manner.

 

In Vivo

OTS964 hydrochloride (intravenously; 40 mg/kg on days 1, 4, 8, 11, 15, and 18) makes tumors shrinking even after the treatment and finally revealing complete regression.

OTS964 hydrochloride (oral administration; 50 or 100 mg/kg/day for 2 weeks) ultimately achieves complete tumor regression.

 

 

References

 

  1. Novel molecule targets cytokinesis. Cancer Discov. 2015 Jan;5(1):OF8. doi: 10.1158/2159-8290.CD-NB2014-170. Epub 2014 Nov 13. PubMed PMID: 25583820.

 

  1. Matsuo Y, Park JH, Miyamoto T, Yamamoto S, Hisada S, Alachkar H, Nakamura Y. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145. doi: 10.1126/scitranslmed.3010277. PubMed PMID: 25338756.

 

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

 

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