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LY364947
TGF-β I型受体激酶结构域抑制剂,LY-364947 是一种有效的,ATP 竞争性的 TGFβR-I 抑制剂,IC50 值为 59 nM,是对 TGFβR-II 选择性的 7 倍。
目录号: PC15958 纯度: ≥98%
CAS No. :396129-53-6
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PC15958-10mM (in 1mL DMSO) 10mM (in 1mL DMSO) ¥793.80 请登录
Medlife所售产品仅用于科学研究(非临床研究),非药品不可食用,不可用于人体或动物的临床诊断和治疗,我们不为个人提供产品及服务。产品COA等资料,可至下方“质量控制”中下载。
中文名称
LY364947
中文别名
4-[3-(2-吡啶基)-1H-吡唑-4-基]喹啉;4-(3-吡啶-2-基-1H-吡唑-4-基)喹啉;LY-364947 抑制剂
英文名称
LY364947
英文别名
4-(3-(Pyridin-2-yl)-1H-pyrazol-4-yl)quinoline;LY-364947;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]-quinoline;[3-(Pyridin-2-yl)-4-(4-quinonyl)]-1H-pyrazole;LY364947;4-(3-Pyridin-2-yl-1H-pyrazol-4-yl)quinoline;LY364947 (LY-364947, HTS 466284);4-(5-pyridin-2-yl-1H-pyrazol-4-yl)quinoline;HTS466284;Transforming Growth Factor-β Type I Receptor Kinase Inhibitor;E 616451;TGF-beta RI Kinase Inhibitor;HTS 466284;TbetaR-I Inhibitor;LY 364947;4-[3-(pyridin-2-yl)-1H-pyrazol-4-yl]quinoline;4-[5-(pyridin-2-yl)-1H-pyrazol-4-yl]quinoline;Quinoline, 4-[3-(2-pyridinyl)-1H-pyrazol-4-yl]-;Transforming Growth Factor-beta Type I Receptor Kinase Inhibitor;4-[3-(2-Pyridinyl)-1H-pyrazol-4-yl]quinoline;4-(3-pyridin-2-yl)(1h)-pyra
Cas No.
396129-53-6
分子式
C17N4H12
分子量
272.30
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.

性状

Solid

IC50 & Target[1][2]

IC50: 59 nM (TGFβR-I)

体外研究(In Vitro)

LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with Ki of 28 nM. LY-364947 inhibits in vivo Smad2 phosphorylation within the NMuMg cells with IC50 of 135 nM. LY-364947 reverses TGF-β-mediated growth inhibition in NMuMg cells with IC50 of 0.218 μM. LY-364947 potentiates the xVent2-lux BMP4 response in NMuMg cells by 30% at concentrations as low as 0.25 μM. LY-364947 (2 μM) prevents TGF-β-induced epithelial?mesenchymal transition in NMuMg cells. LY-364947 (3 μM) induces expression of Prox1 and LYVE-1 in almost all HDLECs after 24 hours. LY-364947 promotes nuclear export of Foxo3a, with low Smad2/3 and high Akt phosphorylation levels in leukaemia-initiating cells. LY-364947 (< 20 μM) suppresses leukaemia-initiating cells colony-forming ability after co-culture with OP-9 stromal cells.

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

体内研究(In Vivo)

LY-364947 (1 mg/kg, i.p.) accelerates lymphangiogenesis, as evidence by significantly increasing the LYVE-1-positive areas in a mouse model of chronic peritonitis. LY-364947 (1 mg/kg, i.p.) significantly increases the LYVE-1-positive areas in tumor tissues in tumor xenograft models using BxPC3 pancreatic adenocarcinoma cells. LY-364947 (25 mg/kg) increases p-Akt and decreases nuclear Foxo3a in leukaemia-initiating cells in CML-affected mice.

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

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
参考文献
溶解度数据
体外研究: 

DMSO : 16.67 mg/mL (61.22 mM; ultrasonic and warming and heat to 60°C)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6724 mL 18.3621 mL 36.7242 mL
5 mM 0.7345 mL 3.6724 mL 7.3448 mL
10 mM 0.3672 mL 1.8362 mL 3.6724 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 1.25 mg/mL (4.59 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (4.59 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (4.59 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (4.59 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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