化合物KX2-391 T6345
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
100 mg | 897016-82-9 | ¥3,880.00 | 询底价 |
25 mg | 897016-82-9 | ¥1,330.00 | 询底价 |
2 mg | 897016-82-9 | ¥339.00 | 询底价 |
1 mL | 897016-82-9 | ¥597.00 | 询底价 |
10 mg | 897016-82-9 | ¥652.00 | 询底价 |
50 mg | 897016-82-9 | ¥2,570.00 | 询底价 |
5 mg | 897016-82-9 | ¥523.00 | 询底价 |
1 mg | 897016-82-9 | ¥243.00 | 询底价 |
Product Introduction
Bioactivity
英文名: Tirbanibulin
描述: Tirbanibulin (KX2-391) 是一种高度选择性的 Src 激酶抑制,靶向 Src 的多肽底物结合位点,对多种癌症有疗效。
细胞实验: Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 (NutriCyte, Buffalo, NY) are routinely cultured and maintained in basal medium containing 2% fetal bovine serum (FBS) at 37 °C and 5% CO2. Cells are seeded at 4.0 × 103/190 μL and 8.0 × 103/190 μL per well of 96-well plate in basal medium containing 1.5% FBS. These are cultured overnight at 37 °C and 5% CO2 prior to the addition of KX2-391, at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten microliters of 3-(4,5-dimethylthiazol- 2-yl)-2,5-diphenyltetrazolium bromide (MTT) solution (5 mg/mL) is then added to each well on day 3 and cells incubated for 4 hours. The formazan product is dissolved with 10% SDS in dilute HCl. Optical density at 570 nm is measured by using BioTek Synergy HT multiplatform microplate reader. For comparison of activity and potency, parallel experiments are performed using KX2-391. Growth inhibition curves, 50% inhibition concentration (GI50), and 80% inhibition concentration (GI80) are determined using GraphPad Prism 5 statistical software. Data are normalized to represent percentage of maximum response as well as reported in optical density at wavelength of 570 nm (OD570) signal format.</ (Only for Reference)
体外活性: KX2-391 is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI 50 = 9 nM), PLC/PRF/5 (GI 50 = 13 nM), Hep3B (GI 50 = 26 nM), and HepG2 (GI 50 = 60 nM), four hepatic cell cancer (HCC) cell lines. [1] KX2-391 is found to inhibit certain leukemia cells that are resistant to current commercially available drugs, such as those derived from chronic leukemia cells with the T3151 mutation. KX2-391 is evaluated in engineered Src driven cell growth assays inNIH3T3/c-Src527F and SYF/c-Src527F cells and exhibits GI50 with 23 nM and 39 nM, respectively. [2]
体内活性: In pre-Clinicalal animal models of cancer, orally administered KX2-391 is shown to inhibit primary tumor growth and to suppress metastasis. [2]
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 80 mg/mL (185.4 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)
关键字: Microtubule/Tubulin | Inhibitor | inhibit | KX 01 | Tirbanibulin | Src | KX01
相关产品: Indibulin | MPT0B014 | TAI-1 | Docetaxel trihydrate | Ixabepilone | D-64131 | Entasobulin | L-Clausenamide | CID-663143 | KHS101 hydrochloride
相关库: Drug Repurposing Compound Library | FDA-Approved Kinase Inhibitor Library | Microtubule-Targeted Compound Library | Anti-Cancer Drug Library | Anti-Cancer Clinical Compound Library | Inhibitor Library | Kinase Inhibitor Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途