LB-100

For research use only. Not for use in humans.

目录号：S7537

CAS No. 1026680-07-8

LB-100是水溶性的protein phosphatase 2A (PP2A)抑制剂，在BxPc-3和Panc-1细胞中，IC50分别为0.85 μM和3.87 μM。

规格

价格

库存

购买数量

5mg	RMB 1198.13	现货
25mg	RMB 3884.02	现货
100mg	RMB 8151.45	现货
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客户使用Selleck生产的LB-100发表文献29篇：

Mol Cell, 2021, S1097-2765(21)00624-9

PubMed: 34453890 ( click the link to review the publication )

J Clin Invest, 2021, 144318

PubMed: 34403361 ( click the link to review the publication )

Cell Death Dis, 2021, 12(9):849

PubMed: 34521817 ( click the link to review the publication )

Mol Cancer Ther, 2021, molcanther.0013.2021

PubMed: 34253596 ( click the link to review the publication )

Clin Sci (Lond), 2021, CS20210315

PubMed: 34402501 ( click the link to review the publication )

Front Cell Dev Biol, 2021, 9:675562

PubMed: 34055807 ( click the link to review the publication )

Neurosci Lett, 2021, S0304-3940(21)00480-8

PubMed: 34237414 ( click the link to review the publication )

Neurotherapeutics, 2021, 10.1007/s13311-021-01089-4

PubMed: 34339019 ( click the link to review the publication )

JCI Insight, 2021, 6(9)141426

PubMed: 33986191 ( click the link to review the publication )

bioRxiv, 2021, 10.1101/2021.05.07.442906

PubMed: None ( click the link to review the publication )

J Cell Biol, 2020, 219(4)

PubMed: 32050025 ( click the link to review the publication )

Cancer Res, 2020, 10;canres.57.2020

PubMed: 32522823 ( click the link to review the publication )

Int J Mol Sci, 2020, 21(18)E6642

PubMed: 32927892 ( click the link to review the publication )

PLoS One, 2020, 29;15(5):e0233863

PubMed: 32470053 ( click the link to review the publication )

Neurosci Lett, 2020, 721:134817

PubMed: 32032748 ( click the link to review the publication )

Biochem Biophys Res Commun, 2020, 526(1):1-7

PubMed: 32192773 ( click the link to review the publication )

Sci Rep, 2020, 10(1):10992

PubMed: 32620893 ( click the link to review the publication )

Int J Mol Sci, 2019, 20(11)E2748

PubMed: 31167510 ( click the link to review the publication )

World J Gastroenterol, 2019, 25(45):6607-6618

PubMed: 31832001 ( click the link to review the publication )

Eur J Pharmacol, 2019, 852:99-106

PubMed: 30851273 ( click the link to review the publication )

Mol Cell, 2018, 71(1):11-24

PubMed: 29937341 ( click the link to review the publication )

Mol Cancer, 2018, 17(1):44

PubMed: 29455644 ( click the link to review the publication )

Exp Mol Med, 2018, 50(7):83

PubMed: 30050113 ( click the link to review the publication )

Anticancer Res, 2018, 38(10):5791-5798

PubMed: 30275201 ( click the link to review the publication )
Am J Pathol, 2017, 187(8):1736-1749

PubMed: 28627412 ( click the link to review the publication )

Mediators Inflamm, 2017, 2017:5706152

PubMed: 29056830 ( click the link to review the publication )

PLoS One, 2017, 12(3):e0173386

PubMed: 28267764 ( click the link to review the publication )

Oncotarget, 2017, 9(7):7312-7321

PubMed: 29484112 ( click the link to review the publication )

Oncotarget, 2017, 8(56):95810-95823

PubMed: 29221169 ( click the link to review the publication )

质量管理及产品安全说明书

PP2A抑制剂选择性比较

生物活性

产品描述

LB-100是水溶性的protein phosphatase 2A (PP2A)抑制剂，在BxPc-3和Panc-1细胞中，IC50分别为0.85 μM和3.87 μM。

靶点

PP2A ^[1]

体外研究

LB-100 可有效抑制BxPc-3和Panc-1细胞的生长，IC50值分别为2.3 μM和1.7 μM。BxPc-3、Panc-1和SW1990细胞经LB-100处理后，PP2A活性下降30-50%。LB-100提高细胞内的阿霉素浓度(约为对照组的2.5倍)，并使肿瘤细胞对阿霉素的细胞毒性更加敏感。LB-100增加VEGF分泌，从而提高HIF-1α-VEGF介导的血管生成。^[1]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Activity Description	PMID
U251 cells	MmHISpVv[3Srb36gZZN{[Xl?	NVPhWVNjOiEQvF2=	M4nadFMhcG:3coOgZY5lKDZiaH;1dpM>	MWL0doVifG2nboSge4l1cCB{IN88UUBNSjFyMDDy[YR2[2WmIGDQNmEh[WO2aY\peJkhfG9iNkGlJI9nKGOxboTyc4wh[2WubIOgZYZ1\XJiYn;0bEB1cHKnZTDhcoQhe2m6IHjveZJ{KG:oIFzCNVAxKGW6cH;zeZJmNg>?	NU\TdIw1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkW5N\|k4PjJpPkK1PVM6PzZ{PD;hQi=>
D283 cells	MULD[YxtKH[rYXLpcIl1gSCjc4PhfS=>			MlnuTWM2OD1yLkmg{txONCC3c3nu[{BZXFRiYYPzZZl{	NGfGTY89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke5PVY4OCd-Mk[3PVk3PzB:L3G+
DAOY cells	NVHTfmRoS2WubDD2bYFjcWyrdImgZZN{[Xl?			M{PFW2lEPTB;Mj65JO69VSxidYPpcochYFSWIHHzd4F6ew>?	NHH0R5o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{Nke5PVY4OCd-Mk[3PVk3PzB:L3G+
D341 cells	MVTD[YxtKH[rYXLpcIl1gSCjc4PhfS=>			MkjhTWM2OD1zLkmg{txONCC3c3nu[{BZXFRiYYPzZZl{	MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPjd7OU[3NEc,OjZ5OUm2O\|A9N2F-
CH-157 cells	MYXGeY5kfGmxbjDhd5NigQ>?	MmTYNk42KM7:TR?=	NUfVNZhIOyCqb4Xydy=>	M3\0cWxDNTFyMDDzbYdvcW[rY3HueIx6KGWwaHHuZ4VlKHSqZTDwdo9xd3K2aX;uJI9nKGOnbHzzJIlvKEd{L12u	M2D6flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7MUm5NFA3Lz5{OUG5PVAxPjxxYU6=
SKOV-3	MXfDfZRwfG:6aXPpeJkh[XO\|YYm=		NHew[Yw4OiCq	NW\X[FJbUUN3MDC9JFExNjFiwsGgNU45KM7:TR?=	Mmm2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|N{[2NFgoRjJ3M{e2OlA5RC:jPh?=
OVCAR-8	MWjDfZRwfG:6aXPpeJkh[XO\|YYm=		MVO3NkBp	M3fVe2lEPTBiPTC1MlUhyrFiMD61JO69VQ>?	M1y2OFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3M{e2OlA5Lz5{NUO3OlYxQDxxYU6=
PEO-4	MkjrR5l1d3SxeHnjbZR6KGG\|c3H5		MlnRO\|IhcA>?	M4DoO2lEPTBiPTC1JOKyKDBwNjFOwG0>	NILsdYY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO3OlYxQCd-MkWzO\|Y3ODh:L3G+
PEO-6	NGDRTo1EgXSxdH;4bYNqfHliYYPzZZk>		M2\5SlczKGh?	M361N2lEPTBiPTC1MlEhyrFiMD6yJO69VQ>?	NFTQVJI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUO3OlYxQCd-MkWzO\|Y3ODh:L3G+
PEO1-Brca2 Missense	MWHDfZRwfG:6aXPpeJkh[XO\|YYm=		MljXO\|IhcA>?	MkjaTWM2OCB;IE[uNkDDuSBzLkWg{txO	NX7JNXFwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWzO\|Y3ODhpPkK1N\|c3PjB6PD;hQi=>
PEO1-Brca2 STOP	MoOwR5l1d3SxeHnjbZR6KGG\|c3H5		M2PBeFczKGh?	MUHJR\|UxKD1iNj6yJOKyKDFwMDFOwG0>	MlO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV\|N{[2NFgoRjJ3M{e2OlA5RC:jPh?=
Huh-7	NE\vbHNRWDKDIHHjeIl3cXS7IHHzd4F6ew>?	M2LKfFUh\|ryvb3yvUC=>	M162SFIhcA>?	NES3NFJz\WS3Y3XkJJRp\SCjY4Tpeol1gSCxZjDQVFJCKHSxIHHic5V1KDdyJR?=	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDh4N{K0PUc,OjR6NkeyOFk9N2F-
HepG2	Mm\IVHAzSSCjY4Tpeol1gSCjc4PhfZM>	MnjKOUDPxG2xbD;M	M1;Le\|IhcA>?	NV\1RVdZemWmdXPl[EB1cGViYXP0bZZqfHlib3[gVHAzSSC2bzDhZo92fCB5MDW=	NYHmRnpkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS4OlczPDlpPkK0PFY4OjR7PD;hQi=>
HL-7702	MUTQVFJCKGGldHn2bZR6KGG\|c3H5dy=>	MWK1JO69dW:uL1y=	NXLCfFB2OiCq	MW\y[YR2[2WmIITo[UBi[3Srdnn0fUBw\iCSUELBJJRwKGGkb4X0JFcxLQ>?	NED3XI49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEi2O\|I1QSd-MkS4OlczPDl:L3G+

... Click to View More Cell Line Experimental Data

Assay

Methods	Test Index	PMID
Western blot	p-AMPKα1 / AMPKα1 / p-ACC / ACC / p-p70S6K1 / p-4EBP1 ; PubMed: 29221169 Oncotarget HCT-116 cells were treated with LB-100 at 10 μM, cells were further cultured for the designated time. Expressions of listed proteins were tested by Western blotting assay. Cyclin D1 / c-myc / mcl-1 / Hsp90 ; PubMed: 29199006 Cancer Lett LB-100 down-regulates expression of STAT3 target genes. Western blot analysis of IOMM-LEE, GAR and CH-157 cells treated with increasing LB100 concentration demonstrates dose-dependent decrease in STAT3 target genes, including mcl-1, c-myc, and cyclin D.	29221169 29199006
Growth inhibition assay	Cell division ; PubMed: 29844427 Nat Commun In vitro proliferation of CD4+ T cells in the presence of LB-100 dose titration, measured by dilution of the cytosolic CFSE. Percentage of cells divided was plotted against concentration of LB-100. Cell viability ; PubMed: 29199006 Cancer Lett Three meningioma cell lines IOMM-LEE, GAR and CH-157 were used in vitro. XTT assays were performed after 48 hours of treatment. Increasing concentrations of LB-100 reduced cell viability, but cytotoxic effect was seen only at high drug concentration with 䲧疝Ỵ疞㧀	29844427 29199006

体内研究

在小鼠胰腺癌异种移植模型中，LB-100 (2毫克/千克，腹腔注射)提高了化疗药物阿霉素的疗效。LB-100提高了肿瘤微血管密度和肿瘤表面的血流速度。^[1]

激酶实验： ^[1]	- 合并 PP2A 酶活性检测: 人工培养的胰腺癌细胞用IC50浓度下的LB-100处理，对每种细胞系或等体积的载体对照分别处理2小时，然后进行PP2A活性测试使用丝氨酸/苏氨酸磷酸酶试剂盒。细胞通过超声波细胞粉碎机裂解，PP2A浓度使用丝氨酸/苏氨酸磷酸酶试剂盒根据说明测量。每个细胞系进行三个平行试验。
细胞实验： ^[1]	- 合并 Cell lines: BxPc-3 和 Panc-1 细胞系 Concentrations: ~ 10 μM Incubation Time: 48小时 Method: 使用细胞计数试剂盒-8（CCK-8）检测细胞毒性。细胞以3000/孔的密度接种至96孔板中，处理后按照CCK-8的步骤检测。相对的细胞毒性以特定对照组的百分比表示。 (Only for Reference)
动物实验： ^[1]	- 合并 Animal Models: 负荷 Panc-1 异种移植物的 BALB/c 裸鼠 Dosages: 2 毫克/千克 Administration: 腹腔注射 (Only for Reference)

参考文献

[1] Bai X, et al. Cancer Lett. 2014, 355(2), 281-287.

溶解度 (25°C)

体外	Water	53 mg/mL (197.53 mM)
	DMSO	Insoluble
	Ethanol	Insoluble

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据 Download LB-100 SDF

分子量	268.31
化学式	C₁₃H₂₀N₂O₄
CAS号	1026680-07-8
储存条件	3年-20°C 粉状 2年-80°C 溶于溶剂
别名	N/A

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量

mg/kg

动物平均体重

g

每只动物给药体积

ul

动物数量

只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO+ % + % Tween 80+ % ddH₂O

计算重置

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

质量

浓度

体积

分子量
=

×

×

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入输出 )

C1

V1

C2

V2
×

=

×

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

分子量计算器

通过输入化合物的化学式来计算其分子量：

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×
计算

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03886662	Unknown status	Drug: LB-100	Myelodysplastic Syndromes	Lixte Biotechnology Holdings Inc.	April 2019	Phase 1\|Phase 2
NCT03027388	Recruiting	Drug: LB-100	Astrocytoma Grades II III and IV\|Glioblastoma Multiforme\|Giant Cell Glioblastoma\|Glioma\|Oligodendrogliomas	National Cancer Institute (NCI)\|National Institutes of Health Clinical Center (CC)	January 9 2019	Phase 2
NCT01837667	Completed	Drug: LB-100 for Injection\|Drug: Docetaxel	Tumors\|Neoplasms\|Cancer	Lixte Biotechnology Holdings Inc.	February 2013	Phase 1

研究领域

产品类型

定制您的化合物库

LB-100

客户使用Selleck生产的LB-100发表文献29篇：

质量管理及产品安全说明书

PP2A抑制剂选择性比较

生物活性

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

参考文献

溶解度 (25°C)

化学数据 Download LB-100 SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2021-09-06)

技术支持