OTS-964
OTS-964
CAS: 1338545-07-5
Molecular Formula: C23H24N2O2S
OTS-964 - Names and Identifiers
OTS-964 - Physico-chemical Properties
| Molecular Formula | C23H24N2O2S |
| Molar Mass | 392.51386 |
| Solubility | 10 mM in DMSO |
| Storage Condition | -20℃ |
| In vitro study | OTS964 can inhibit the growth of TOPK positive cells, with low IC50 values: A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDAMB- 231 (73 nM), t47D (72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116 (33 nM),MKN1 (38 nM), MKN45 (39 nM), HepG2 (19 nM), MIAPaca-2 (30 nM), and 22 Rv1 (50 nM), while its growth inhibitory effect on TOPK negative HT29 cancer cells was relatively significantly reduced, with an IC50 of 290 nM. Although OTS964 has some inhibitory effect on Src kinase family, the inhibitory effect of OTS964 on the growth of these cancer cells is not related to the expression of Src kinase c-Src, Fyn and Lyn, but acts through TOPK. OTS964 induces a defect in cytokinesis in T47D cells, leading to apoptosis. |
| In vivo study | Although administration of the Free compound caused hematopoietic side effects (leukopenia, thrombocytosis), The liposomal formulation of OTS964 was effective in regressing tumor inhibition without causing other side effects in mice. OTS964 inhibits TOPK activity, causes subsequent apoptosis by causing defects in cytokinesis, and inhibits tumor growth. The hematopoietic toxicity caused by oral administration of OTS964 is only a transient effect, and the negative effect of leukopenia will be repaired naturally. The anticancer effect of oral administration of the compound is similar to that of its liposome preparation, and the oral route of administration is more practical. |
OTS-964 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.331 ml | 11.656 ml | 23.311 ml |
| 5 mM | 0.466 ml | 2.331 ml | 4.662 ml |
| 10 mM | 0.233 ml | 1.166 ml | 2.331 ml |
| 5 mM | 0.047 ml | 0.233 ml | 0.466 ml |
Last Update：2024-01-02 23:10:35
OTS-964 - Reference Information
| biological activity | OTS964 is an effective TOPK inhibitor with high affinity and selectivity to TOPK, IC50 is 28 nM. OTS964 is also a potent inhibitor of cyclin-dependent kinase CDK11 with a Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts. |
| target | TargetValue TOPK (cell-free say) 28 nM CDK11B (cell-free say) 40 nM (kd) |
| Target | Value |
| TOPK (Cell-free assay) | 28 nM |
| CDK11B (Cell-free assay) | 40 nM(Kd) |
| in vitro study | OTS964 can inhibit the growth of TOPK positive cells with low IC50 values: A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDAMB- 231 (73 nM), T47D (72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116 (33 nM),MKN1 (38 nM), MKN45 (39 nM), HepG2 (19 nM), MIAPaca-2 (30 nM), and 22 Rv1 (50 nM), while its growth inhibition effect on TOPK negative HT29 cancer cells is relatively significantly weakened, IC50 is 290 nM. Although OTS964 has a certain inhibitory effect on the Src kinase family, the inhibitory effect of OTS964 on the growth of these cancer cells is not related to the expression of Src kinase c-Src, Fyn and Lyn, but through TOPK. OTS964 can induce cytokinesis defects in T47D cells, thus causing apoptosis. |
| In vivo studies | Although the administration of free compounds can cause hematopoietic side effects (leukopenia, thrombocytosis), the liposome preparation of OTS964 can effectively subside and inhibit tumors without causing other side effects in mice. OTS964 inhibits TOPK activity, causes subsequent apoptosis by causing cytokinesis defects, and inhibits tumor growth. The hematopoietic toxicity caused by oral administration of OTS964 is only a transient effect, and the negative effect of leukopenia will be repaired naturally. The anti-cancer effect of oral administration of this compound is similar to that of liposome preparations, and oral administration is more practical. |
Last Update：2024-04-10 22:29:15
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