LCH-7749944(Synonyms: GNF-PF-2356) | 赛默飞Alfa aesar官网

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LCH-7749944 (Synonyms: GNF-PF-2356) 纯度: 99.43%

LCH-7749944 (GNF-PF-2356) 是一种有效的 PAK4 抑制剂，IC₅₀ 为 14.93 μM。LCH-7749944通过下调 PAK4/c-Src/EGFR/cyclin D1 途径有效抑制人胃癌细胞的增殖，并诱导凋亡 (apoptosis)。

LCH-7749944 Chemical Structure

CAS No. : 796888-12-5

规格	价格	是否有货
Free Sample (0.1-0.5 mg)		Apply now
10 mM * 1 mL in DMSO	￥2500	In-stock
5 mg	￥2200	In-stock
10 mg	￥3500	In-stock
50 mg	￥10500	In-stock
100 mg		询价
200 mg		询价

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LCH-7749944 相关产品

•相关化合物库:

Covalent Screening Library Plus
Bioactive Compound Library Plus
Apoptosis Compound Library
Cell Cycle/DNA Damage Compound Library
Kinase Inhibitor Library
Anti-Cancer Compound Library
Anti-Aging Compound Library
Covalent Screening Library
Cytoskeleton Compound Library

生物活性

LCH-7749944 (GNF-PF-2356) is a potent PAK4 inhibitor with an IC₅₀ of 14.93 μM. LCH-7749944 effectively suppresses the proliferation of human gastric cancer cells through downregulation of PAK4/c-Src/EGFR/cyclin D1 pathway and induces apoptosis^[1].

IC₅₀ & Target^[1]

PAK4

14.93 μM (IC₅₀)

体外研究
(In Vitro)

LCH-7749944 (GNF-PF-2356; 5-50 μM; 24 hours) inhibits the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner^[1].
LCH-7749944 (5-20 μM; 12-48 hours) induces apoptosis of SGC7901 cells^[1].
LCH-7749944 (5-20 μM; 12-48 hours) prominently induces a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase^[1].
LCH-7749944 (5-30 μM; 24 hours) dramatically decreases levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner^[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:	MKN-1, BGC823, SGC7901 and MGC803 human gastric cancer cells
Concentration:	5, 10, 15, 20, 25, 30, 35, 40, 45, 50 μM
Incubation Time:	24 hours
Result:	Inhibited the proliferation of MKN-1, BGC823, SGC7901 and MGC803 cells in a concentration dependent manner.

Apoptosis Analysis^[1]

Cell Line:	SGC7901 cells
Concentration:	5, 10, 20 μM
Incubation Time:	12, 24, 48 hours
Result:	Induced apoptosis of SGC7901 cells.

Cell Cycle Analysis^[1]

Cell Line:	SGC7901 cells
Concentration:	5, 10, 20 μM
Incubation Time:	12, 24, 48 hours
Result:	Prominently induced a dose-dependent increase in the percentage of cells in G1 phase and decrease in S phase.

Western Blot Analysis^[1]

Cell Line:	SGC7901 cells
Concentration:	5, 10, 20, 30 μM
Incubation Time:	24 hours
Result:	Dramatically decreased levels of phosphoPAK4, phospho-c-Src, phospho-EGFR and cyclin D1 protein expression in a dose-dependent manner.

分子量

350.41

Formula

C₂₀H₂₂N₄O₂

CAS 号

796888-12-5

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	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 250 mg/mL (713.45 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.8538 mL	14.2690 mL	28.5380 mL
5 mM	0.5708 mL	2.8538 mL	5.7076 mL
10 mM	0.2854 mL	1.4269 mL	2.8538 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: ≥ 2.17 mg/mL (6.19 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (6.19 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 21.7 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% (20% SBE-β-CD in saline)

Solubility: ≥ 2.17 mg/mL (6.19 mM); Clear solution

此方案可获得 ≥ 2.17 mg/mL (6.19 mM，饱和度未知) 的澄清溶液。

以 1 mL 工作液为例，取 100 μL 21.7 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。

将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. Zhang J, et al. LCH-7749944, a novel and potent p21-activated kinase 4 inhibitor, suppresses proliferation and invasion in human gastric cancer cells. Cancer Lett. 2012 Apr 1;317(1):24-32.

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