Певонедистат
Певонедистат атрибут
Температура плавления: |
161-163°C |
Температура кипения: |
721.0±70.0 °C(Predicted) |
плотность: |
1.62 |
температура хранения: |
-20°C Freezer |
растворимость: |
Растворим в ДМСО (до 10 мг/мл). |
форма: |
Твердый |
пка: |
9.35±0.70(Predicted) |
цвет: |
белый |
Стабильность:: |
Срок годности 2 года с даты покупки в состоянии поставки. Растворы в ДМСО можно хранить при температуре -20° до 3 месяцев. |
Словарь онкологических терминов NCI: |
pevonedistat |
FDA UNII: |
S3AZD8D215 |
Словарь наркотиков NCI: |
pevonedistat |
безопасность
- Заявления о рисках и безопасности
- код информации об опасности(GHS)
Певонедистат химические свойства, назначение, производство
Химические свойства
White Solid
Ферментативный ингибитор
This first-in-class small molecule inhibitor (FW = 443.52 g/mol; CAS 905579-51-3; Solubility = 10 mg/mL DMSO), also named MLN4924 and [(1S,2S,4R)-4-[4-[[(1S)-2,3-dihydro-1H-inden-1-yl]amino]-7H-pyrrolo[2,3- d]pyrimidin-7-yl]-2-hydroxycyclopentyl]sulfamate methyl ester, targets Nedd8 activating enzyme, or NAE (IC50 = 4.7 nM), with much weaker action against UAE (IC50 = 1.5 μM), SAE (IC50 = 8.2 μM), and UBA6 (IC50 = 1.8 μM). In most cancer cells, pevonedistat treatment results in the induction of DNA re-replication, resulting in DNA damage and cell death. MLN4924 also exhibits an alternative mechanism of action. Treatment of activated B cell-like (ABC) diffuse large B-cell lymphoma (DLBCL) cells with pevonedistat resulted in rapid accumulation of pIkBa, decrease in nuclear p65 content, reduction of transcriptional activity of NF-kB (or nuclear factor k-light-chain-enhancer of activated B cells), and G1 arrest, ultimately resulting in apoptosis induction, events consistent with potent NF-kB pathway inhibition. Treatment of germinal-center B cell-like (GCB) DLBCL cells resulted in an increase in cellular Cdt-1 and accumulation of cells in S-phase, consistent with cells undergoing DNA rereplication. Pevonedistat also inhibits Vpx/Vpr-induced SAMHD1 degradation by inhibiting the neddylation of E3 ubiquitin-ligase and blocking SIVmac replication in myeloid cells, therebyindicating the potential efficacy of inhibiting neddylation as an antiretroviral strategy
Певонедистат препаратная продукция и сырье
сырьё
препарат
Певонедистат поставщик
Global( 110)Suppliers
905579-51-3(Певонедистат)подобный поиск: