1338542-14-5

Name	OTS964
CAS	1338542-14-5
Molecular Formula	C23H24N2O2S
MDL Number	MFCD29918155
Molecular Weight	392.51
MOL File	1338542-14-5.mol

Synonyms

OTS964(free base) Thieno[2,3-c]quinolin-4(5H)-one, 9-[4-[(1R)-2-(dimethylamino)-1-methylethyl]phenyl]-8-hydroxy-6-methyl-

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Chemical Properties

Boiling point	501.7±50.0 °C(Predicted)
density	1.232±0.06 g/cm3(Predicted)
pka	9.46±0.20(Predicted)

Hazard Information

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

Supplier

Jinan Jiuli Biotechnology Co. , Ltd.

Telephone 15865264761

Websitehttps://www.chemicalbook.com/ShowSupplierProductsList89365/0_EN.htm

InvivoChem

Telephone 13549236410

Websitehttps://www.invivochem.cn/

Shanghai Yifei Biotechnology Co. , Ltd.

Telephone021-65675885 18964387627

Websitehttp://www.efebio.com

TargetMol Chemicals Inc.

Telephone 15002134094

Websitehttps://www.targetmol.cn/

Shanghai Fengyong Biotechnology Co., Ltd.

Telephone021-10000000 13000000000

Websitehttps://www.abmole.cn

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