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Tirbanibulin Mesylate (KX2-391 (Mesylate)) Sale

(Synonyms: KX2-391 Mesylate; KX01 Mesylate) 目录号 : GC34109

A Src kinase inhibitor

Tirbanibulin Mesylate (KX2-391 (Mesylate)) Chemical Structure

Cas No.:1080645-95-9

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥675.00
现货
5mg
¥585.00
现货
10mg
¥720.00
现货
50mg
¥2,790.00
现货
100mg
¥4,770.00
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

KX2-391 is an inhibitor of Src kinase (IC50 = ~20 nM).1 It is selective for Src over PDGFR, EGFR, JAK1, JAK2, Lck, and ZAP-70. KX2-391 induces cell cycle arrest at the G2/M phase and apoptosis in breast cancer cells expressing estrogen receptor α (ERα).2 It inhibits the growth of Huh7, PLC/PRF/5, Hep3B, and HepG2 cells (GI50s = 9, 13, 26, and 60 nM, respectively).3 KX2-391 (10 mg/kg) decreases spleen weight and the number of splenic leukemia cells in a mouse model of FLT3 bearing internal-tandem duplication and F691L mutant (FLT3-ITD-F691L) acute myeloid leukemia (AML).4

1.Naing, A., Cohen, R., Dy, G.K., et al.A phase I trial of KX2-391, a novel non-ATP competitive substrate-pocket- directed SRC inhibitor, in patients with advanced malignanciesInvest. New Drugs31(4)967-973(2013) 2.Anbalagan, M., Carrier, L., Glodowski, S., et al.KX-01, a novel Src kinase inhibitor directed toward the peptide substrate site, synergizes with tamoxifen in estrogen receptor α positive breast cancerBreast Cancer Res. Treat.132(2)391-409(2012) 3.Lau, G.M., Lau, G.M., Yu, G.-L., et al.Expression of Src and FAK in hepatocellular carcinoma and the effect of Src inhibitors on hepatocellular carcinoma in vitroDig. Dis. Sci.54(7)1465-1474(2009) 4.Wang, P., Xiao, X., Zhang, Y., et al.A dual inhibitor overcomes drug-resistant FLT3-ITD acute myeloid leukemiaJ. Hematol. Oncol.14(1)105(2021)

Chemical Properties

Cas No. 1080645-95-9 SDF
别名 KX2-391 Mesylate; KX01 Mesylate
Canonical SMILES O=C(NCC1=CC=CC=C1)CC2=NC=C(C3=CC=C(OCCN4CCOCC4)C=C3)C=C2.CS(=O)(O)=O
分子式 C27H33N3O6S 分子量 527.63
溶解度 DMSO : ≥ 57 mg/mL (108.03 mM) 储存条件 Store at -20°C, protect from light, stored under nitrogen
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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 1.8953 mL 9.4763 mL 18.9527 mL
5 mM 0.3791 mL 1.8953 mL 3.7905 mL
10 mM 0.1895 mL 0.9476 mL 1.8953 mL
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