Tirbanibulin Mesylate (KX2-391 (Mesylate))
(Synonyms: KX2-391 Mesylate; KX01 Mesylate) 目录号 : GC34109A Src kinase inhibitor
Cas No.:1080645-95-9
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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. |
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)
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 |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 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。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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