| Identification | Back Directory | [Name]
OTS964 | [CAS]
1338542-14-5 | [Synonyms]
OTS964(free base)
Thieno[2,3-c]quinolin-4(5H)-one, 9-[4-[(1R)-2-(dimethylamino)-1-methylethyl]phenyl]-8-hydroxy-6-methyl- | [Molecular Formula]
C23H24N2O2S | [MDL Number]
MFCD29918155 | [MOL File]
1338542-14-5.mol | [Molecular Weight]
392.51 |
| Hazard Information | Back Directory | [Uses]
OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM[1]. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM[2]. | [in vivo]
OTS964 (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[1].
OTS964 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression[1]. | Animal Model: | Nude mice bearing LU-99 lung cancer cells[1] | | Dosage: | 40 mg/kg | | Administration: | Intravenously; on days 1, 4, 8, 11, 15, and 18 | | Result: | The tumors continued shrinking even after the treatment and finally revealed complete regression.
|
| Animal Model: | Nude mice bearing LU-99 lung cancer cells[1] | | Dosage: | 50 or 100 mg/kg | | Administration: |
Oral administration; once every day for 2 weeks | | Result: | Achieved complete tumor regression.
|
| [IC 50]
TOPK: 28 nM (IC50); CDK11B: 40 nM (Kd) | [References]
[1] Matsuo Y , et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancerthrough inhibition of cytokinesis. Sci Transl Med. 2014 Oct 22;6(259):259ra145. DOI:10.1126/scitranslmed.3010277
[2] Lin A, et al. Off-target toxicity is a common mechanism of action of cancer drugs undergoing clinical trials. Sci Transl Med. 2019 Sep 11;11(509). DOI:10.1126/scitranslmed.aaw8412
[3] Lu H, et al. TOPK inhibits autophagy by phosphorylating ULK1 and promotes glioma resistance to TMZ. Cell Death Dis. 2019 Aug 5;10(8):583. DOI:10.1038/s41419-019-1805-9 |
|
| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
|