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Tirbanibulin

产品编号 T6345 CAS 897016-82-9

别名: KX2-391, KX-01

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。

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Tirbanibulin, CAS 897016-82-9

规格	价格/CNY	货期
1 mg	￥ 243	现货
2 mg	￥ 339	现货
5 mg	￥ 523	现货
10 mg	￥ 652	现货
25 mg	￥ 1,330	现货
50 mg	￥ 2,570	现货
100 mg	￥ 3,880	现货
1 mL * 10 mM (in DMSO)	￥ 597	现货

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其他形式的 Tirbanibulin:

Tirbanibulin Mesylate
现货
Tirbanibulin dihydrochloride
询价

选择批次

纯度: 99.67%

纯度: 99.43%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Tirbanibulin (KX2-391) is a highly selective Src kinase inhibitor that has demonstrated efficacy in pre-Clinicalal animal models of colon, pancreatic, prostate and breast cancer. It is a substrate-targeted kinase inhibitor. KX2-391, belongs to an emerging new family of targeted cancer treatments called protein kinase inhibitors.
靶点活性	Src (HuH-7):9 nM(GI50), Src (HepG2):60 nM(GI50), Src (Hep3B):26 nM(GI50), Src (PLC/PRF/5):13 nM(GI50)
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]
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)

别名	KX2-391, KX-01
分子量	431.53
分子式	C26H29N3O3
CAS No.	897016-82-9

存储

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)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3173 mL	11.5867 mL	23.1734 mL	57.9334 mL
	5 mM	0.4635 mL	2.3173 mL	4.6347 mL	11.5867 mL
	10 mM	0.2317 mL	1.1587 mL	2.3173 mL	5.7933 mL
	20 mM	0.1159 mL	0.5793 mL	1.1587 mL	2.8967 mL
	50 mM	0.0463 mL	0.2317 mL	0.4635 mL	1.1587 mL
	100 mM	0.0232 mL	0.1159 mL	0.2317 mL	0.5793 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Lau GM, et al, Dig Dis Sci, 2009, 54(7), 1465-1474. 2. Fallah-Tafti A, et al, Eur J Med Chem, 2011, 46(10), 4853-4858. 3. Zhang X, Xu H, Bi X, et al. Src acts as the target of matrine to inhibit the proliferation of cancer cells by regulating phosphorylation signaling pathways[J]. 2020

文献引用

1. Chen J, Lei C, Nie D, et al.Inorganic arsenic exposure promotes malignant progression by HDAC6‐mediated down‐regulation of HTRA1.Journal of Applied Toxicology.2023

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Tirbanibulin 897016-82-9 Angiogenesis Cytoskeletal Signaling Tyrosine Kinase/Adaptors Src Microtubule Associated Microtubule/Tubulin Inhibitor inhibit KX 01 KX2-391 KX-01 KX01 inhibitor

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Tirbanibulin

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords