10mM in DMSO ベースライン干渉を最小限に抑える必要がある、感度の高いクロマトグラフィーおよび分析ワークフロー向け。
Store at -80°C Dry ice packs + Cold packs に出荷。正確な仕様については、ロット固有の COA をご確認ください。
SDS、COA、データシート、仕様書をダウンロードできます。ロット固有の COA はロット番号検索で入手可能です。
クロマトグラフィー、有機合成、クロスカップリング反応に関する 0 件の査読済み論文で引用されています。
Information
OTS964 OTS964 is a potent TOPK inhibitor with high affinity and selectivity and IC50 value is 28 nM. OTS964 is also a potent inhibitor of the cyclin-dependent kinase CDK11 with Kd of 40 nM. OTS964 treatment activates autophagy in glioma cells and induces apoptosis of human lung cancer cells in mouse xenografts.
Targets
TOPK (Cell-free assay); CDK11B (Cell-free assay) 28 nM; 40 nM(Kd)
In vitro
OTS964 inhibits 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 22Rv1 (50 nM)], whereas its growth inhibitory effect against TOPK-negative HT29 cancer cells is significantly weaker, with IC50 of 290nM. Although OTS964 reveals some suppressive effect on Src family kinases, the response to OTS964 in these cancer cells is not correlated with the expression of Src family kinases c-Src, Fyn, and Lyn, supporting the TOPK-dependent growth inhibitory effects of OTS964. Time lapse imaging in T47D cells shows that treatment with OTS964 induces cytokinesis defects followed by apoptosis.
In vivo
Although administration of the free compound induces hematopoietic adverse reactions (leukocytopenia associated with thrombocytosis), the drug delivered in a liposomal formulation effectively causes complete regression of transplanted tumors without showing any adverse reactions in mice. Inhibition of TOPK activity with the liposomal OTS964 suppresses tumor growth through induction of cytokinesis defects and subsequent apoptosis. Although oral administration of OTS964 causes some hematopoietic toxicity, this is a transient effect. The spontaneous recovery from leukocytopenia is occured and the anticancer effectiveness of the oral drug is similar to that of the liposomal formulation, oral administration of the drug may prove to be more practical.
Cell Research(from reference)
Cell lines：A549 cells, LU-99 cells, DU4475 cells, MDA-MB-231 cells, T47D cells, Daudi cells, UM-UC-3 cells, HCT-116 cells, MKN1 cells, MKN45 cells, HepG2 cells, MIAPaca-2 cells, 22Rv1 cells and HT29 cells
Incubation Time：72 h
危険性、取扱い、保管、および規制遵守を網羅した包括的な文書。
<<<<<<< HEAD SDS をダウンロード → ======= SDS をダウンロード → >>>>>>> release248-p3Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| 分類 | Quinolines and derivatives |
| Subclass | Quinolones and derivatives |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Thienoquinolines |
| Alternative Parents | Phenylquinolines Hydroquinolones Hydroxyquinolines Aromatic monoterpenoids Hydroquinolines Phenylpropylamines Thienopyridines Aralkylamines 1-hydroxy-2-unsubstituted benzenoids Pyridinones Thiophenes Heteroaromatic compounds Lactams Trialkylamines Azacyclic compounds Organooxygen compounds Organic oxides Hydrochlorides Hydrocarbon derivatives |
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Phenylquinoline - Thienoquinoline - Dihydroquinolone - Hydroxyquinoline - P-cymene - Aromatic monoterpenoid - Phenylpropylamine - Dihydroquinoline - Monoterpenoid - Thienopyridine - 1-hydroxy-2-unsubstituted benzenoid - Aralkylamine - Pyridinone - Phenol - Monocyclic benzene moiety - Pyridine - Benzenoid - Heteroaromatic compound - Thiophene - Lactam - Tertiary aliphatic amine - Tertiary amine - Azacycle - Amine - Hydrochloride - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Organonitrogen compound - Organooxygen compound - Organic nitrogen compound - Aromatic heteropolycyclic compound |
| 説明 | This compound belongs to the class of organic compounds known as thienoquinolines. These are heterocyclic compounds containing a thiophene ring fused to a quinoline. Quinoline or benzo[b]pyridine is a bicyclic compound that consists of benzene fused to a pyridine. |
| External Descriptors | Not available |
| DMSO（mg / mL） 最大溶解度 | 85 |
|---|---|
| DMSO（mM） 最大溶解度 | 198.1490547 |
| 水（mg / mL） 最大溶解度 | ＜1 |
| 分子量 | 429.000 g/mol |
| XLogP3 | |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 4 |
| Exact Mass | 428.133 Da |
| Monoisotopic Mass | 428.133 Da |
| Topological Polar Surface Area | 80.800 Ų |
| Heavy Atom Count | 29 |
| Formal Charge | 0 |
| Complexity | 563.000 |
| Isotope Atom Count | 0 |
| Defined Atom Stereocenter Count | 1 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| The total count of all stereochemical bonds | 0 |
| Covalently-Bonded Unit Count | 2 |
