LY-364947 HTS466284|cas:396129-53-6|西域试剂

LY-364947 HTS466284,98.86%

产品编号：Bellancom-13462| CAS NO：396129-53-6| 分子式：C₁₇H₁₂N₄| 分子量：272.30

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货号	价格	库存与货期
Bellancom-13462	￥550.00	杭州北京（现货）
Bellancom-13462	￥760.00	杭州北京（现货）
Bellancom-13462	￥2750.00	杭州北京（现货）

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LY-364947 HTS466284

产品介绍

LY-364947 (HTS466284) 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。

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.

体外研究

LY-364947 is an ATP competitive and tight-binding inhibitor, inhibiting phosphorylation of P-Smad3 by TGFβR-I Kinase with K_i 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.

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

体内研究

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.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

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

配制储备液

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

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, 6 months; -20°C, 1 month。-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。

In Vivo:

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

1.

请依序添加每种溶剂： 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 ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 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。