OTS964

OTS964 is an orally active, high affinity and selective TOPK inhibitor with an IC50 of 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11, which binds to CDK11B with a Kd of 40 nM.

Product information

CAS Number: 1338542-14-5

Molecular Weight: 392.51

Formula: C23H24N2O2S

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

Smiles: CC1=CC(O)=C(C2=C1NC(=O)C1SC=CC=12)C1C=CC(=CC=1)[C@@H](C)CN(C)C

InChiKey: XCFRUAOZMVFDPQ-AWEZNQCLSA-N

InChi: InChI=1S/C23H24N2O2S/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)/t14-/m0/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: Soluble in DMSO

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

OTS964 (10 nM; 48 hours) suppresses cancer cell proliferation. OTS964 (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 (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 (oral administration; 50 or 100 mg/kg/day for 2 weeks) achieves complete tumor regression.

References:

1. Yang Y, Wu ZX, Wang JQ, Teng QX, Lei ZN, Lusvarghi S, Ambudkar SV, Chen ZS, Yang DH. OTS964, a TOPK Inhibitor, Is Susceptible to ABCG2-Mediated Drug Resistance. Front Pharmacol. 2021 Feb 15;12:620874.
2. Sugimori M, Hayakawa Y, Koh M, Hayashi T, Tamura R, Kuroda S. Targeting the T-Lak cell originated protein kinase by OTS964 shrinks the size of power-law coded heterogeneous glioma stem cell populations. Oncotarget. 2017 Dec 9;9(3):3043-3059.

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