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PLX4032
- русский язык имя
- английское имяPLX4032
- CAS №918504-65-1
- CBNumberCB02550000
- ФормулаC23H18ClF2N3O3S
- мольный вес489.92
- номер MDLMFCD18074504
- файл Mol918504-65-1.mol
химическое свойство
плотность | 1.46 |
температура хранения | -20°C |
растворимость | Soluble in DMSO (up to 100 mg/ml) |
форма | White powder. |
пка | 6.26±0.10(Predicted) |
цвет | White or off-white |
Стабильность | Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months. |
Справочник по базе данных CAS | 918504-65-1 |
FDA UNII | 207SMY3FQT |
кода HS | 29339900 |
Банк данных об опасных веществах | 918504-65-1(Hazardous Substances Data) |
рисовальное письмо(GHS)
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рисовальное письмо(GHS)
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сигнальный язык
предупреждение
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вредная бумага
H410:Чрезвычайно токсично для водных организмов с долгосрочными последствиями.
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оператор предупредительных мер
P273:Избегать попадания в окружающую среду.
P391:Ликвидировать просыпания/проливы/утечки.
P501:Удалить содержимое/ контейнер на утвержденных станциях утилизации отходов.
PLX4032 химические свойства, назначение, производство
Описание
In August 2011, the United States FDA approved vemurafenib (PLX- 4032, RO-5185426) for the treatment of patients with metastatic melanoma with the BRAFV600E mutation. Vemurafenib has been developed as a targeted therapy for patients with the BRAF gene mutation since oncogenic B-raf signaling is implicated in approximately 50% of melanomas. Vemurafenib was identified based on an initial high-throughput screen followed by the extensive use of structure-based drug design. Vemurafenib is a potent inhibitor of B-RafV600E kinase (IC50=13 nM) compared to its potency against wildtype B-raf (IC50=160 nM) and is fairly selective versus a panel of 200 kinases. It does inhibit other kinases (RAF1, SRMS, ACK1, MAP4K5, and FGR) and mutant B-raf kinases (BRAFV600K, BRAFV600D, and BRAFV600R) with enzyme IC50's of <100 nM.Химические свойства
Off-White SolidИспользование
Vemurafenib selective BRAFV600E kinase inhibitor; an antitumor agent. Vemurafenib functions by inhibiting the proliferation and mitogen-activated protein/extracellular signal-regulated kinase (ERK) kinase and ERK phosphorylation in a panel of tumor cell lines, including melanoma cell lines expressing BRAFV600E or other mutant BRAF proteins altered at codon 600.Определение
ChEBI: A pyrrolopyridine that is 1H-pyrrolo[2,3-b]pyridine which is substituted at position 5 by a p-chlorophenyl group and at positions 3 by a 3-amino-2,6-difluorobenzoyl group, the amino group of which has undergone ormal condensation with propane-1-sulfonic acid to give the corresponding sulfonamide. An inhibitor of BRAF and other kinases.PLX4032 поставщик
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