2. Protein Tyrosine Kinase/RTK Cytoskeleton Cell Cycle/DNA Damage
  3. Src Microtubule/Tubulin
  4. Tirbanibulin

Tirbanibulin  (Synonyms: KX2-391; KX-01)

目录号: HY-10340 纯度: 99.56%
COA 产品使用指南

摩尔计算器

Tirbanibulin (KX2-391) 是一种拟肽类 Src 抑制剂，靶向 Src 的多肽底物结合位点，对多种癌细胞株 GI50 为 9-60 nM。

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Tirbanibulin Chemical Structure

Tirbanibulin Chemical Structure

CAS No. : 897016-82-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥720
In-stock
1 mg ￥295
In-stock
5 mg ￥650
In-stock
10 mg ￥800
In-stock
25 mg ￥1680
In-stock
50 mg ￥3100
In-stock
100 mg ￥4565
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Other Forms of Tirbanibulin:

Tirbanibulin 相关抗体

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Lck Fyn Blk

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

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

IC50 & Target

GI50: 9 nM (Src, in HuH7 cells), 13 nM (Src, in PLC/PRF/5 cells), 26 nM (Src, in Hep3B cells), 60 nM (Src, in HepG2 cells)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HT-29 IC50
23 nM
Compound: 1; KX2-391; KX-01
Antiproliferative activity against human HT-29 cells in presence of 1.5% FCS by BrdU incorporation assay
Antiproliferative activity against human HT-29 cells in presence of 1.5% FCS by BrdU incorporation assay
[PMID: 29617135]
K562 IC50
18.2 nM
Compound: KX01; KX2-391
Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 34081857]
NIH3T3 GI50
0.023 μM
Compound: KX01, KX2 391
Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay
Inhibition of constitutively active human c-SRC527F mutant-induced growth inhibition in mouse NIH3T3 cells after 3 days by MTT assay
[PMID: 21852023]
Ramos IC50
15.7 nM
Compound: KX01; KX2-391
Antiproliferative activity against human Ramos cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human Ramos cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 34081857]
SK-OV-3 IC50
6.8 nM
Compound: KX01; KX2-391
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
Antiproliferative activity against human SK-OV-3 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
[PMID: 34081857]
体外研究
(In Vitro)

Tirbanibulin (KX2-391) is a Src inhibitor that is directed to the Src substrate pocket. Tirbanibulin (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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Tirbanibulin 相关抗体:
体内研究
(In Vivo)

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

431.53

Formula

C26H29N3O3
CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMSO 中的溶解度 : 41.67 mg/mL (96.56 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3173 mL 11.5867 mL 23.1734 mL
5 mM 0.4635 mL 2.3173 mL 4.6347 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.82 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.82 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料
参考文献
Cell Assay
[1]

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

Tirbanibulin 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 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
15 mM 0.1545 mL 0.7724 mL 1.5449 mL 3.8622 mL
20 mM 0.1159 mL 0.5793 mL 1.1587 mL 2.8967 mL
25 mM 0.0927 mL 0.4635 mL 0.9269 mL 2.3173 mL
30 mM 0.0772 mL 0.3862 mL 0.7724 mL 1.9311 mL
40 mM 0.0579 mL 0.2897 mL 0.5793 mL 1.4483 mL
50 mM 0.0463 mL 0.2317 mL 0.4635 mL 1.1587 mL
60 mM 0.0386 mL 0.1931 mL 0.3862 mL 0.9656 mL
80 mM 0.0290 mL 0.1448 mL 0.2897 mL 0.7242 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tirbanibulin897016-82-9KX2-391 KX-01KX01KX 01KX-01SrcMicrotubule/TubulinInhibitorinhibitorinhibit

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