УКН-01
- английское имяUCN-01
- CAS №112953-11-4
- CBNumberCB2972499
- ФормулаC28H26N4O4
- мольный вес482.53044
- номер MDLMFCD26960886
- файл Mol112953-11-4.mol
химическое свойство
Температура кипения | 705.7±60.0 °C(Predicted) |
плотность | 1.63±0.1 g/cm3(Predicted) |
температура хранения | 2-8°C |
растворимость | DMSO: >5mg/mL |
форма | Tan solid |
пка | 12.25±0.70(Predicted) |
цвет | light yellow |
оптическая активность | [α]20/D 130 to 160°, c = 0.2 in DMSO |
Словарь онкологических терминов NCI | UCN-01 |
FDA UNII | 7BU5H4V94A |
Словарь наркотиков NCI | 7-hydroxystaurosporine |
WGK Германия | 3 |
RTECS | KC6600010 |
Токсичность | mouse,LD50,intraperitoneal,25mg/kg (25mg/kg),Journal of Antibiotics. Vol. 42, Pg. 571, 1989. |
УКН-01 химические свойства, назначение, производство
Описание
UCN-01 is a synthetic derivative of staurosporine with antiproliferative activity against several in vitro and in vivo cancer models. It inhibits a variety of kinases, including Akt, protein kinase C (IC50 = 30 nM), PDK1 (IC50 = 6 nM) and cyclin-dependent kinases (IC50s = 300-600 nM for Cdk1 and Cdk2). UCN-01 arrests tumor cells in the G1/S phase of the cell cycle and prevents nucleotide excision repair by inhibiting the G2 checkpoint kinase Chk1 (IC50 = 7 nM), leading to apoptosis.Использование
UCN-01 is an indolocarbazole isolated from a high staurosporine-producing Streptomyces culture. UCN-01 inhibits protein kinase C (PKC) and cyclin-dependant kinase 2 (CDK2), resulting in accumulation of cells in the G1 phase and induction of apoptosis. UCN-01 also enhances the cytotoxicity of other anti-cancer drugs, such as DNA-damaging agents and anti-metabolite drugs, through putative abrogation of G2 and/or S phase accumulation induced by the latter agents.Общее описание
A cell-permeable Staurosporine (Cat. No. 569397) derived anticancer agent that reversibly and ATP-competitively inhibits several protein kinases (IC50 = 29 nM, 34 nM, 30 nM, 590 nM and 530 nM for PKCα, PKCβ, PKCγ, PKCδ and PKCε; IC50 = 7 nM, 27 nM, 50 nM, 50 nM, 150 nM and 1.04 M for Chk1, Cdc25C-associated protein kinase 1, Cdk1, PAK4, Cdk5/p25 and Chk2; IC50 = 33 nM, 50 nM, 95 nM, 500 nM, 500 nM and 1.0 M for PDK1, lck, MAPKAP kinase-2, Akt, GSK-3β and PKA, respectively). At higher concentrations (>15 M), affects the activities of Src, PIM-1, CKII, DNA-PK, ErK1, ILK-1 and MAPKK1). Reported to suppress thymidylate synthase expression, induce apoptosis with caspase activation, and sensitize tumor cells to a range of DNA-damaging agents.УКН-01 поставщик
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