2. TGF-beta/Smad
  3. TGF-β Receptor
  4. Galunisertib

Galunisertib  (Synonyms: LY2157299)

目录号: HY-13226 纯度: 99.84%
COA 产品使用指南 技术支持

Galunisertib (LY2157299) 是一种选择性的 TGF-β 受体 I 型 (TGF-βRI) 激酶抑制剂，IC50 为 56 nM。

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Galunisertib Chemical Structure

Galunisertib Chemical Structure

CAS No. : 700874-72-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥610
In-stock
2 mg ￥330
In-stock
5 mg ￥550
In-stock
10 mg ￥820
In-stock
50 mg ￥2600
In-stock
100 mg ￥3600
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Galunisertib:

Galunisertib 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 47 篇科研文献

查看 TGF-β Receptor 亚型特异性产品:

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.

IC50 & Target

IC50: 56 nM (TGF-βRI)[4]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
4T1 IC50
> 0.1 μM
Compound: 5, LY-2157299
Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
Inhibition of ALK5 in mouse 4T1 cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
[PMID: 24786585]
HaCaT IC50
> 0.1 μM
Compound: 5, LY-2157299
Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
Inhibition of ALK5 in human HaCaT cells assessed as inhibition of TGFbeta1-induced luciferase activity after 24 hrs by luciferase reporter gene assay
[PMID: 24786585]
Sf9 IC50
0.119 μM
Compound: 3; LY-2157299
Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay
Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by radiometric assay
[PMID: 31299584]
Sf9 IC50
0.129 μM
Compound: 3; LY-2157299
Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method
Inhibition of human recombinant GST-tagged ALK5 expressed in Sf9 insect cells using casein as substrate incubated for 60 mins in presence of [33P]-ATP by scintillation counting method
[PMID: 31303386]
Sf9 IC50
69.4 nM
Compound: 4; LY-2157299
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay
Inhibition of human recombinant GST-fused ALK5 expressed in Sf9 insect cells using casein as substrate by proprietary radioisotopic protein kinase assay
[PMID: 26483198]
体外研究
(In Vitro)

Galunisertib (LY2157299) (0.1、1、10 和 100 μM) 在 SK-Sora、HepG2 和 Hep3B 细胞系中显示出对 Bay 43-9006 的轻微剂量依赖性增强，但在 JHH6、SK-HEP1 和 HuH7 细胞系中没有表现出此作用[2]。

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

Galunisertib 相关抗体:
体内研究
(In Vivo)

将人异种移植瘤 Calu6（非小细胞肺癌）和 MX1（乳腺癌）植入裸鼠皮下。口服 75 mg/kg 剂量的 Galunisertib (LY2157299) 后，两种细胞系的 pSmad 均下降 70%。给药后约 6 小时，pSmad 恢复至基线水平的 80%[3]。

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

369.42

Formula

C22H19N5O
CAS 号
性状

固体

颜色

White to yellow

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 : 100 mg/mL (270.69 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 2.7069 mL 13.5347 mL 27.0695 mL
5 mM 0.5414 mL 2.7069 mL 5.4139 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： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 5.75 mg/mL (15.56 mM); 澄清溶液

  • 方案 二

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

    Solubility: ≥ 2.08 mg/mL (5.63 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。
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

纯度: 99.95%

COA (197 KB) LCMS (121 KB) 元素分析报告 (214 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

Cell survival is determined using the MTT assay. The conversion of yellow water-soluble tetrazolium MTT into purple insoluble formazan is catalyzed by mitochondrial dehydrogenases and used to estimate the number of viable cells. In brief, cells are seeded in 96-well tissue culture plates at a density of 2×103 cells/well. After drug exposure, cells are incubated with 0.4 mg/mL MTT for 4 hours at 37°C. After incubation, the supernatant is discarded, insoluble formazan precipitates are dissolved in 0.1 mL of DMSO, and the absorbance is measured at 560 nm by use of a microplate reader. Wells with untreated cells or with drug-containing medium without cells are used as positive and negative controls respectively. For proliferation assay, MTT assay is done daily to determine the number of viable cells in untreated control andGalunisertib (LY2157299) (0.1, 1, 10, and 10 μM)-treated group[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Mice[3]
Charles River nude mice (weight 25 mg) are used. Galunisertib (LY2157299) is given orally as a single dose or in a multiple dosing design. The value of the dose levels given in a single dose manner is 10 (n=3), 30 (n=8), 50 (n=26), 75 (n=69), 100 (n=3), 150 (n=21) and 300 (n=3) mg/kg. Animals are sacrificed at the following times: 0.5, 1, 1.5, 2, 4, 8 and 16 h after administration, then the tumor is removed and blood is recovered. In the multiple dosing study, Galunisertib (LY2157299) is administered twice a day (bid) at the dose of 75 mg/kg every 12 h for 20 consecutive days to 31 mice. Animals are sacrificed at 2 h after the last administration at days 10, 15, 20 and 25, and the tumor is removed for pSmad determination and the blood is recovered for determination of drug levels in plasma.

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

Galunisertib 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 2.7069 mL 13.5347 mL 27.0695 mL 67.6736 mL
5 mM 0.5414 mL 2.7069 mL 5.4139 mL 13.5347 mL
10 mM 0.2707 mL 1.3535 mL 2.7069 mL 6.7674 mL
15 mM 0.1805 mL 0.9023 mL 1.8046 mL 4.5116 mL
20 mM 0.1353 mL 0.6767 mL 1.3535 mL 3.3837 mL
25 mM 0.1083 mL 0.5414 mL 1.0828 mL 2.7069 mL
30 mM 0.0902 mL 0.4512 mL 0.9023 mL 2.2558 mL
40 mM 0.0677 mL 0.3384 mL 0.6767 mL 1.6918 mL
50 mM 0.0541 mL 0.2707 mL 0.5414 mL 1.3535 mL
60 mM 0.0451 mL 0.2256 mL 0.4512 mL 1.1279 mL
80 mM 0.0338 mL 0.1692 mL 0.3384 mL 0.8459 mL
100 mM 0.0271 mL 0.1353 mL 0.2707 mL 0.6767 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:

Galunisertib700874-72-2LY2157299LY 2157299LY-2157299TGF-β ReceptorTransforming growth factor beta receptorsInhibitorinhibitorinhibit

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