OTS-964
- Optical Purity: 99% e.e.
- Soluble in DMSO
- MF: C23H24N2O2S
- MW: 392.51
Description
TOPK (T–lymphokine-activated killer cell–originated protein kinase), an enzyme that is heavily and frequently transactivated in various cancer tissues, including lung and triple-negative breast cancers, plays a vital role in the mitosis of cancer cells. Optically pure OTS-964 is a TOPK small molecular inhibitor, binding to the enzyme potently and selectively with IC50 at lower nM. The inhibition causes a cytokinesis defect and the subsequent apoptosis of cancer cells in vitro as well as in xenograft models of human lung cancer. The drug delivered in a liposomal formulation effectively caused complete regression of transplanted tumors without any detectable side effects in mice. The salt OTS964 hydrochloride (Axon 4097) is also available.
More Information
| Parent CAS No. | 1338542-14-5 |
|---|---|
| Chemical Name | (R)-9-(4-(1-(dimethylamino)propan-2-yl)phenyl)-8-hydroxy-6-methylthieno[2,3-c]quinolin-4(5H)-one |
| extra_info | Sold in collaboration with Chemietek |
| SMILES | C1(C2C=CC([C@@H](C)CN(C)C)=CC=2)C(O)=CC(C)=C2NC(=O)C3SC=CC=3C=12 |&1:5,r| |
| MFCD | N.A. |
| 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 |
| InChiKey | XCFRUAOZMVFDPQ-AWEZNQCLSA-N |
| CID | 67448186 |
| Short Description | TOPK inhibitor |
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