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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
-10 to -25°C
SMILES字符串
N4(CCOCC4)c1nc2[n](c(nc2c(n1)c3cnc(nc3)N)C)C(C)C
InChI key
QYBGBLQCOOISAR-UHFFFAOYSA-N
生化/生理作用
Orally active, potent and highly selective mTOR and class I phosphoinositide 3-kinases (PI 3-kinases; PI3K) inhibitor with anti-cancer efficacy in vitro and in vivo.
VS-5584 (SB2343) is an orally active, potent and highly selective mTOR (IC50 = 37 nM) and class I phosphoinositide 3-kinases (PI 3-kinases; PI3K IC50 = 16 nM/α, 68 nM/β, 25 nM/γ, 42 nM/δ; little activity toward 400 other lipid and protein kinases) inhibitor with broad-spectrum anti-proliferation activity in cancer cultures (IC50 post 48h treatment from 48 nM to 1.75 μM among 50 cancer lines) by inhibiting PI3K and mTOR downstream substrates phosphorylation. VS-5584 displays tumor growth inhibition efficacy in various rapalog-sensitive and -resistant human xenograft models in mice in vivo (PC3 TGI = 79% and 113%, respectively, post 28-day 11 mg/kg or 25 mg/kg daily p.o. treatment).
VS-5584 (SB2343) is an orally active, potent and highly selective mTOR (IC50 = 37 nM) and class I phosphoinositide 3-kinases (PI 3-kinases; PI3K IC50 = 16 nM/α, 68 nM/β, 25 nM/γ, 42 nM/δ; little activity toward 400 other lipid and protein kinases) inhibitor with broad-spectrum anti-proliferation activity in cancer cultures (IC50 post 48h treatment from 48 nM to 1.75 μM among 50 cancer lines) by inhibiting PI3K and mTOR downstream substrates phosphorylation. VS-5584 displays tumor growth inhibition efficacy in various rapalog-sensitive and -resistant human xenograft models in mice in vivo (PC3 TGI = 79% and 113%, respectively, post 28-day 11 mg/kg or 25 mg/kg daily p.o. treatment).
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
PI3K/mTOR dual inhibitor VS-5584 preferentially targets cancer stem cells
Cancer Research, 75(2), 446-455 (2015)
Structure and ligand-based design of mTOR and PI3-kinase inhibitors leading to the clinical candidates VS-5584 (SB2343) and SB2602
Journal of Chemical Information and Modeling, 54(11), 3238-3250 (2014)
Stefan Hart et al.
Molecular cancer therapeutics, 12(2), 151-161 (2012-12-29)
Dysregulation of the PI3K/mTOR pathway, either through amplifications, deletions, or as a direct result of mutations, has been closely linked to the development and progression of a wide range of cancers. Moreover, this pathway activation is a poor prognostic marker
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