10mM in DMSO 최소한의 기준선 간섭이 필요한 민감한 크로마토그래피 및 분석 워크플로우용.
Store at -80°C Dry ice packs + Cold packs 출고. 정확한 사양은 로트별 COA를 확인하세요.
SDS, COA, 데이터시트, 사양서를 다운로드할 수 있습니다. 로트별 COA는 로트 번호 조회를 통해 확인할 수 있습니다.
크로마토그래피, 유기 합성 및 교차 커플링 반응 분야의 동료 심사 논문 0편에서 인용되었습니다.
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
위험성, 취급, 보관 및 규제 준수를 포괄하는 종합 문서.
<<<<<<< HEAD SDS 다운로드 → ======= SDS 다운로드 → >>>>>>> release248-p3Taxonomy Tree
| Kingdom | Organic compounds |
|---|---|
| Superclass | Organoheterocyclic compounds |
| 분류 | 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 |
| 설명 | 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) 최대 용해도 | 85 |
|---|---|
| DMSO(mM) 최대 용해도 | 198.1490547 |
| 물(mg/mL) 최대 용해도 | ＜1 |
| 분자량 | 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 |
