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检测方案
≥97% (HPLC)
质量水平
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
yellow
溶解性
DMSO: 50 mg/mL
储存温度
−20°C
一般描述
A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic α-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC50 = 11 nM for [14C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t1/2 = 3.03 h, Tmax = 0.667 h & Cmax = 17.5 mg/L; 100 mg/kg, i.p.: t1/2 = 3.19 h, Tmax = 0.5 h & Cmax = 61.333 mg/L).
A cell-permeable, orally bioavailable, water-soluble (~1 mg/ml), non-toxic α-cyanocinnamate analog that acts as a potent and reversible inhibitor of MCT1 activity (IC50 = 11 nM for [14C]-lactate uptake in rat brain endothelial cell line RBE4). Shown to suppress colorectal adenocarcinoma (WiDr cell line) tumor growth in female BALB/c nude mice (% inhibition at the end of 3-weeks = 29, 45, 45 & 56 administered at 10 mg/kg, b.i.d., i.p., 50 mg/kg, b.i.d., p.o., 50 mg/kg, b.i.d., i.p. and 100 mg/kg, q.i.d., p.o., respectively). Displays favorable PK profile in mice (100 mg/kg, p.o.: t1/2 = 3.03 h, Tmax = 0.667 h & Cmax = 17.5 mg/L; 100 mg/kg, i.p.: t1/2 = 3.19 h, Tmax = 0.5 h & Cmax = 61.333 mg/L).
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
生化/生理作用
Cell permeable: yes
Primary Target
MCT1
MCT1
Reversible: yes
Target IC50: 11 nM for [¹⁴C]-lactate uptake in rat brain endothelial cell line RBE4
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Gurrapu, S., et al. 2015. ACS Med. Chem. Lett.6, 558.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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
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