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Datasheet of OTS514

Description:.
OTS-514 is a novel TOPK(PDZ binding kinase; PBK) inhibitor,IC50:2.6nM. The compound can inhibit TOPK kinase activity.
TOPK (T-lymphokine-activated killer cell-originated protein kinase) is a protein that is found in a wide range of human cancers
and is believed to work as an oncogene, promoting tumor growth.The enzyme shows highly elevated expression in several
cancers including lymphomas, breast cancer and lung cancer. Its activity peaks in the M phase of the cell-division cycle, during
which it phosphorylates several proteins involved in cancer cell cytokinesis, such as histone H3, protein regulator of cytokinesis
1 (PRC1), G protein signaling modulator 2 (GPSM2) and valosin containing protein.Many cancer cells upregulate TOPK and
require its activity to drive their rapidly progressing cell cycles. Because the kinase is either not expressed or expressed at
relatively low levels in most healthy tissues, targeting it in cancer cells could eliminate some of the risks associated with other
cytokinesis enzymes. It has been reported that OTS514 strongly inhibited the growth of the TOPK-positive cancer cell lines with
low IC50 values ranging from 1.5 to 14 nM. While in HT29 cells, in which TOPK expression was little detectable, the IC50
value was 170 nM. Intravenous administration of free OTS514 at 1, 2.5, and 5mg/kg once a day for 2 weeks resulted in tumor
growth InhibitionTGIof 5.7, 43.3, and 65.3% on day 15, respectively, without anybody weight loss. However, this inhibition
also cause dysfunction in the differentiation process of hematopoietic stemcells (HSCs) to WBCs and RBCs but may enhance the
differentiation of HSCs to megakaryocytes and platelets. The antitumor effect of OTS514 in lung cancer xenograft model of
LU-99 cells has also been investigated. OTS514 was administered to mice bearing LU-99 cancer cells after the tumor size
reached about 200mm3. Intravenous administration of OTS514 (5 mg/kg) once a day for 2 weeks achieved good
growth-suppressive effect with TGI of 104% without any body weight loss. However, the antitumor effect of OTS514 against
LU-99 xenograft caused a significant reduction of WBCs. For the detailed information of OTS514, the solubility of OTS514 in
water, the solubility of OTS514 in DMSO, the solubility of OTS514 in PBS buffer, the animal experiment (test) of OTS514, the
cell expriment (test) of OTS514, the in vivo, in vitro and clinical trial test of OTS514, the EC50, IC50,and affinity,of OTS514,
For the detailed information of OTS514, the solubility of OTS514 in water, the solubility of OTS514 in DMSO, the solubility of
OTS514 in PBS buffer, the animal experiment (test) of OTS514, the cell expriment (test) of OTS514, the in vivo, in vitro and
clinical trial test of OTS514, the EC50, IC50,and affinity,of OTS514, Please contact DC Chemicals.

Chemical Information
Catalog

DC8043

Purity of current batch:

>98%

Molecular Weight (MW)

350.43

Molecular Formula

C20H18N2O2S

CAS No.
Solubility (25C)

DMSO

Storage

Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.