Description
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:
- 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.
- 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.
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