GSK2879552 dihydrochloride

目录号: HY-18632A 纯度: 99.19%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

GSK2879552 dihydrochloride是一种可口服的，不可逆的 LSD1/ KDM1A 抑制剂，具有抗肿瘤活性。

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GSK2879552 dihydrochloride Chemical Structure

CAS No. : 1902123-72-1

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥970	In-stock
1 mg	￥400	In-stock
5 mg	￥880	In-stock
10 mg	￥1400	In-stock
25 mg	￥2500	In-stock
50 mg	￥4000	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

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Customer Review

Other Forms of GSK2879552 dihydrochloride:

GSK2879552 In-stock

MCE 顾客使用本产品发表的 15 篇科研文献

: GSK2879552 dihydrochloride purchased from MCE. Usage Cited in: Cancer Chemother Pharmacol. 2019 Feb;83(2):277-287. [Abstract]; The protein expression of LSD1, PRB and H3K4me2 is detected through Western blot with GSK2879552 treatment in different cells.

GSK2879552 dihydrochloride 相关产品

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KDM1/LSD1 KDM2 KDM3 KDM4 KDM5 KDM6 KDM7

生物活性
纯度 & 产品资料
参考文献

生物活性

GSK2879552 dihydrochloride an orally active, selective and irreversible inhibitor of lysine specific demethylase 1 (LSD1/KDM1A), with potential antineoplastic activity^[1]^[2].

IC₅₀ & Target

KDM1/LSD1

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
DU-145	GI₅₀	> 10 μM Compound: GSk2879552; 2	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
ECa-109 cell line	IC₅₀	> 50 μM Compound: GSK2879552	Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay Cytotoxicity against human EC109 cells assessed as growth inhibition by MTT assay	[PMID: 27769034]
Kasumi 1	GI₅₀	0.02 μM Compound: 3; GSK2879552	Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay Growth inhibition on human Kasumi-1 cells measured upto 12 days by Cell Titer-Glo luminescent cell viability assay	[PMID: 32551003]
MGC-803	IC₅₀	> 125 μM Compound: GSK2879552	Antiproliferative activity against human MGC803 cells after 5 days by MTT assay Antiproliferative activity against human MGC803 cells after 5 days by MTT assay	[PMID: 28435523]
MGC-803	IC₅₀	> 50 μM Compound: GSK2879552	Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay Cytotoxicity against human MGC803 cells assessed as growth inhibition by MTT assay	[PMID: 27769034]
MV4-11	EC₅₀	0.023 μM Compound: 5; GSK2879552	Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis Activation of CD86 expression in human MV4-11 cells incubated for 24 hrs by qRT-PCR analysis	[PMID: 35200034]
MV4-11	EC₅₀	0.054 μM Compound: 3; GSK2879552	Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method Inhibition of LSD1 in human MV4-11 cells assessed as induction of LY96 mRNA expression incubated for 16 hrs by chemiluminescent method	[PMID: 32551003]
MV4-11	IC₅₀	1.16 μM Compound: GSK2879552	Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay Antiproliferative activity against human MV4-11 cells after 240 hrs by MTS assay	[PMID: 30713023]
MV4-11	IC₅₀	1.19 μM Compound: 5; GSK2879552	Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay	[PMID: 35200034]
PC-3	GI₅₀	> 10 μM Compound: GSk2879552; 2	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
RPMI-8226	IC₅₀	> 20 μM Compound: 5; GSK2879552	Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay Antiproliferative activity against human RPMI-8226 cells assessed as inhibition of cell growth incubated for 240 hrs by MTS assay	[PMID: 35200034]

体外研究
(In Vitro)

GSK2879552 dihydrochloride 抑制 KDM1A 组蛋白去甲基化酶活性，诱导索拉非尼耐药细胞的分化并减弱干细胞特性。GSK2879552 dihydrochloride 在索拉非尼耐药细胞中抑制 Wnt 拮抗剂的转录并下调 β-catenin 信号活性^[1]。

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

Cell Viability Assay^[2].

Cell Line:	9/28 small cell lung carcinoma (SCLC) lines and 20/29 AML lines.
Concentration:	0-10000 nM.
Incubation Time:	6 days.
Result:	Inhibited cell proliferation.

RT-PCR^[1].

Cell Line:	Resistant HCC cells (PLC/PRF/5 and Huh7).
Concentration:	0, 1, 2 μM.
Incubation Time:	24 h.
Result:	Displayed reduced mRNA expression levels of stem cell markers, such as Lgr5, Sox9, Nanog and CD90, and elevated mRNA expression levels of differentiation markers Alb and Hnf4.

体内研究
(In Vivo)

GSK2879552 dihydrochloride (1.5 mg/kg，po) 处理在携带 SCLC 异种移植物的小鼠中表现出肿瘤生长抑制^[2]。

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

Animal Model:	NCI-H526 and NCI-H1417 xenografts^[2].
Dosage:	1.5 mg/kg.
Administration:	PO daily for 25-35 days.
Result:	There was 57% and 83% tumor growth inhibition (TGI) in NCI-H526 and NCI-H1417 tumor bearing mice respectively. NCI-H510 and NCI-H69 tumor bearing mice also demonstrated partial TGI (38% and 49% respectively) in response to GSK2879552, while no significant TGI was observed for SHP77 bearing mice.

Clinical Trial

分子量

437.40

Formula

C₂₃H₃₀Cl₂N₂O₂

CAS 号

1902123-72-1

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

细胞实验：

H₂O 中的溶解度 : 100 mg/mL (228.62 mM; 超声助溶)

DMSO 中的溶解度 : 31.25 mg/mL (71.44 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	2.2862 mL	11.4312 mL	22.8624 mL
5 mM	0.4572 mL	2.2862 mL	4.5725 mL
10 mM	0.2286 mL	1.1431 mL	2.2862 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

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: ≥ 2.5 mg/mL (5.72 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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: ≥ 2.5 mg/mL (5.72 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.72 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。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： PBS
Solubility: 8.33 mg/mL (19.04 mM); 澄清溶液; 超声助溶 (<60°C)

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

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

计算结果

工作液所需浓度 : mg/mL

该产品水溶性佳，请具体参考实测水 / PBS / Saline 中的溶解度数据。

您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。

纯度 & 产品资料

纯度: 99.19%

选择批次：

Data Sheet (631 KB) SDS (393 KB)

COA (190 KB) LCMS (96 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Huang M, et al. Targeting KDM1A attenuates Wnt/β-catenin signaling pathway to eliminate sorafenib-resistant stem-like cells in hepatocellular carcinoma. Cancer Lett. 2017 Apr 2;398:12-21. [Content Brief]

[2]. Mohammad HP, et al. A DNA Hypomethylation Signature Predicts Antitumor Activity of LSD1 Inhibitors in SCLC. Cancer Cell. 2015 Jul 13;28(1):57-69. [Content Brief]

GSK2879552 dihydrochloride 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO / H₂O	1 mM	2.2862 mL	11.4312 mL	22.8624 mL	57.1559 mL
	5 mM	0.4572 mL	2.2862 mL	4.5725 mL	11.4312 mL
	10 mM	0.2286 mL	1.1431 mL	2.2862 mL	5.7156 mL
	15 mM	0.1524 mL	0.7621 mL	1.5242 mL	3.8104 mL
	20 mM	0.1143 mL	0.5716 mL	1.1431 mL	2.8578 mL
	25 mM	0.0914 mL	0.4572 mL	0.9145 mL	2.2862 mL
	30 mM	0.0762 mL	0.3810 mL	0.7621 mL	1.9052 mL
	40 mM	0.0572 mL	0.2858 mL	0.5716 mL	1.4289 mL
	50 mM	0.0457 mL	0.2286 mL	0.4572 mL	1.1431 mL
	60 mM	0.0381 mL	0.1905 mL	0.3810 mL	0.9526 mL
H₂O	80 mM	0.0286 mL	0.1429 mL	0.2858 mL	0.7144 mL
H₂O	100 mM	0.0229 mL	0.1143 mL	0.2286 mL	0.5716 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

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:

GSK28795521902123-72-1GSK 2879552GSK-2879552Histone DemethylasestemcellSCLCInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

GSK2879552 dihydrochloride

Customer Review

Other Forms of GSK2879552 dihydrochloride:

MCE 顾客使用本产品发表的 15 篇科研文献