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KX2-391 dihydrochloride Sale

(Synonyms: 5-[4-[2-(4-吗啉基)乙氧基]苯基]-N-(苯基甲基)-2-吡啶乙酰胺盐酸盐,KX2-391 2HCl; KX2-391) 目录号 : GC10222

A Src kinase inhibitor

KX2-391 dihydrochloride Chemical Structure

Cas No.:1038395-65-1

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥457.00
现货
5mg
¥441.00
现货
10mg
¥720.00
现货
50mg
¥2,105.00
现货
250mg
¥7,119.00
现货

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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment:

Liver cell lines including Huh7, PLC/PRF/5, Hep3B, and HepG2 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 Tirbanibulin (KX2-391), at concentrations ranging from 6,564 to 0.012 nM in triplicates. Treated cells are incubated for 3 days. Ten μLs 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. For comparison of activity and potency, parallel experiments are performed using Tirbanibulin (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.

References:

[1]. Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci, 2009, 54(7), 1465-1474.
[2]. Fallah-Tafti A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem, 2011, 46(10), 4853-4858.

产品描述

Tirbanibulin (dihydrochloride) (KX2-391 (dihydrochloride)) is an inhibitor of Src that targets the peptide substrate site of Src, with GI50 of 9-60 nM in cancer cell lines.

Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. KX2-391 shows steep dose-response curves against Huh7 (GI50=9 nM), PLC/PRF/5 (GI50=13 nM), Hep3B (GI50=26 nM), and HepG2 (GI50=60 nM), four hepatic cell cancer (HCC) cell lines[1]. Tirbanibulin (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. Tirbanibulin (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].

Orally administered Tirbanibulin (KX2-391) is shown to inhibit primary tumor growth and to suppress metastasis, in pre-clinical animal models of cancer[2].

Reference:
[1]. Lau GM, et al. Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitro. Dig Dis Sci, 2009, 54(7), 1465-1474.
[2]. Fallah-Tafti A, et al. Thiazolyl N-benzyl-substituted acetamide derivatives: synthesis, Src kinase inhibitory and anticancer activities. Eur J Med Chem, 2011, 46(10), 4853-4858.

Chemical Properties

Cas No. 1038395-65-1 SDF
别名 5-[4-[2-(4-吗啉基)乙氧基]苯基]-N-(苯基甲基)-2-吡啶乙酰胺盐酸盐,KX2-391 2HCl; KX2-391
化学名 N-benzyl-2-[5-[4-(2-morpholin-4-ylethoxy)phenyl]pyridin-2-yl]acetamide;dihydrochloride
Canonical SMILES C1COCCN1CCOC2=CC=C(C=C2)C3=CN=C(C=C3)CC(=O)NCC4=CC=CC=C4.Cl.Cl
分子式 C26H31Cl2N3O3 分子量 504.45
溶解度 ≥ 25.2 mg/mL in DMSO, ≥ 48.8 mg/mL in EtOH with gentle warming 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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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9824 mL 9.9118 mL 19.8236 mL
5 mM 0.3965 mL 1.9824 mL 3.9647 mL
10 mM 0.1982 mL 0.9912 mL 1.9824 mL
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