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HDAC6-IN-1 Sale

目录号 : GC33317

SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.

HDAC6-IN-1 Chemical Structure

Cas No.:1815580-06-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥3,036.00
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1mg
¥1,339.00
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5mg
¥3,481.00
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10mg
¥4,909.00
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50mg
¥16,065.00
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100mg
¥24,990.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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实验参考方法

Cell experiment:

A375, A2780s, SKBR3, HepG2, HeLa, HCT116, A549, and SKOV-3 cells are cultured in DMEM. RPMI8226, K562, H460, HT29, and Ramos cells are cultured in RPMI-1640 medium. MV4-11 cells are cultured in IMDM. All media contains 10% fetal bovine serum (FBS), 100 units/mL Penicillin, and 100 μg/mL Streptomycin. Cells are incubated at 37 °C in a humidified atmosphere of 5% CO2. Cells in logarithmic phase are seeded into 96-well culture plates at densities of 3000-5000 cells per well and subsequently treated with various concentrations of compounds (e.g., SKLB-23bb;10, 100, 1000, and 10000 nM) for 72 h in final volumes of 200 μL. Upon end point, 20 μL of MTT (5 mg/mL) is added to each well, and the cells are incubated for an additional 1-3 h. After carefully removal of the medium, the precipitates are dissolved in 150 μL of DMSO via mechanically shaking, and then absorbance values at a wavelength of 570 nm are taken on a spectrophotometer. IC50 values are calculated using percentage of growth versus untreated control[1].

Animal experiment:

Mice[1]For the MV4-11 and Ramos xenograft models, MV4-11 and Ramos cells (107 cells in 100 μL of serum-free IMDM) are injected subcutaneously into the right flanks of 5- to 6-week-old female NOD/SCID mice. For the HCT116 xenograft, HCT116 cells (107 cells in 100 μL of serum-free DMEM) are injected subcutaneously into the right flanks of 5- to 6-week-old female Balb/c nude mice. When the size of the formed xenografts reach 100-150 mm3, the mice are randomly divided (6 mice per group in MV4-11 model, 8 mice per group in Ramos model, and 7 mice per group in HCT116 model) into control group and treated groups. The mice in the experimental groups receive intravenous (iv) injection (50 mg/kg) or oral administration (25 mg/kg) of SKLB-23bb every 2 days. The mice in the vehicle group receive iv injection or oral administration of equal amount of physiological saline containing 5% ethanol and 5% Cremophor EL. Those in the SAHA or LBH-589 or ACY-1215 groups (positive controls) receive ip injection (50 mg/kg for SAHA and 10 mg/kg for LBH-589, dissolved in physiological saline containing 10% DMSO and 45% PEG400 to a concentration of 10 mg/mL) or oral administration (100 mg/kg for SAHA and 40 mg/kg for ACY-1215, dissolved in the same way described above) every 2 days. Tumor burden is measured every 2 days by a caliper. Tumor volume (TV) is calculated. The day that treatment started is defined as day 0. At the end of the experiment, mice are sacrificed and tumors are collected and weighed[1]. Rats[1]SKLB-23bb is administered to SD rats ntravenously (iv) at 12 mg/kg body weight and orally at 12 mg/kg body weight. Blood samples are taken, and the plasma is analyzed for concentration of SKLB-23bb using an LC-MS/MS system[1].

References:

[1]. Yang Z, et al. Discovery of Selective Histone Deacetylase 6 Inhibitors Using the Quinazoline as the Cap for the Treatment of Cancer. J Med Chem. 2016 Feb 25;59(4):1455-70.

产品描述

SKLB-23bb is an orally bioavailable HDAC6-selective inhibitor with IC50 values under 100 nmol/L, against most of the cell lines checked. It also has microtubule-disrupting ability.

SKLB-23bb shows cytotoxic effects against a panel of solid and hematologic tumor cell lines at the low submicromolar level. In contrast to the reported HDAC6-selective inhibitors, SKLB-23bb is more efficient against solid tumor cells. SKLB-23bb selectively inhibits cellular HDAC6, but the antitumor activity of SKLB-23bb is independent of HDAC6. SKLB-23bb could bind to the colchicine site in β-tubulin and act as a microtubule polymerization inhibitor. It blocks tumor cell cycle at G2-M phase and triggers cellular apoptosis[1].

In solid tumor xenografts, oral administration of SKLB-23bb efficiently inhibits tumor growth. SKLB-23bb has good pharmacokinetic profiles and is orally bioavailable[1].

[1] Wang F, et al. Mol Cancer Ther. 2018, 17(4):763-775.

Chemical Properties

Cas No. 1815580-06-3 SDF
Canonical SMILES CN(C1=CC(OCCCC(NO)=O)=C(OC)C=C1)C2=NC(C)=NC3=CC=CC=C32
分子式 C21H24N4O4 分子量 396.44
溶解度 DMSO : 32 mg/mL (80.72 mM) 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
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1 mM 2.5224 mL 12.6122 mL 25.2245 mL
5 mM 0.5045 mL 2.5224 mL 5.0449 mL
10 mM 0.2522 mL 1.2612 mL 2.5224 mL
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