產(chǎn)品目錄

規(guī)格	5mg 25mg 100mg
CAS	1454682-72-4
別名
化學(xué)名	1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(2-methyl-7-(methylamino)pyrido[2,3-d]pyrimidin-3-yl)phenyl)urea
分子式	C23H29FN6O
分子量	424.51
溶解度	≥ 4.25mg/mL in DMSO with ultrasonic and warming
儲(chǔ)存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

LY3009120 is a pan-RAF and RAF dimer inhibitor. It inhibits BRAF WT, CRAF, WT, BRAFV600E, and BRAFV600E+G468A with the IC50 values of 9.1, 15, 5.8, and 17 nM, respectively. [1]

RAF is family of serine/threonine-protein kinase mediates Ras GTPases and the MAPK/ERK cascade. It involves in proliferation, differentiation, apoptosis, survival and oncogenic transformation. [1]

In NRAS mutant SK-Mel2 cells or KRAS mutant HCT116 cells, LY3009120 inhibits the kinase activity of CRAF in a dose-dependent manner and induces BRAF/CRAF heterodimerization. It also blocks Phospho-MEK and -ERK and induces minimal paradoxical activation in RAS mutant Cells. Moreover, treatment of BRAF V600E A375 melanoma cells by LY3009120 for 24 hr predominantly induces a G0/G1 arrest with more than 95% cells in G0/G1 phase. [1]

In nude rats bearing A375 xenograft tumors, oral LY3001920 treatment exerts a dose-dependent inhibition of phospho-MEK and –ERK. 15 or 30 mg/kg LY3009120 shows near complete tumor regression in nude rats bearing PDX tumors.

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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