AES-135

目录号: HY-114483 纯度: 98.21%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

AES-135 是一种基于羟肟酸的泛 HDAC 抑制剂，可延长胰腺癌原位小鼠模型的存活时间。AES-135 抑制 HDAC3、HDAC6、HDAC8 和 HDAC11，IC₅₀ 范围为190-1100 nM。

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AES-135 Chemical Structure

CAS No. : 2361659-61-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥4807	In-stock
1 mg	￥1200	In-stock
5 mg	￥3150	In-stock
10 mg	￥4600	In-stock
25 mg	现货	询价
50 mg		询价
100 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

•Cell Death Dis. 2021 May 18;12(6):501. [Abstract]

AES-135 相关产品

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HDAC HDAC1 HDAC2 HDAC3 HDAC4 HDAC5 HDAC6 HDAC7 HDAC8 HDAC9 HDAC10 HDAC11 HD1 HD2

生物活性
纯度 & 产品资料
参考文献

生物活性

AES-135, a hydroxamic acid-based pan-HDAC inhibitor, prolongs survival in an orthotopic mouse model of pancreatic cancer. AES-135 inhibits HDAC3, HDAC6, HDAC8, and HDAC11 with IC₅₀s ranging from 190-1100 nM^[1].

IC₅₀ & Target^[1]

HDAC6

190 nM (IC₅₀)

HDAC11

636 nM (IC₅₀)

HDAC3

654 nM (IC₅₀)

HDAC8

1100 nM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
MDA-MB-231	IC₅₀	2.62 μM Compound: 5; AES-135	Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay	[PMID: 31938464]
MDA-MB-231	IC₅₀	2.72 μM Compound: AES-135	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by CellTiter-Blue assay	[PMID: 30776234]
MDA-MB-468	IC₅₀	4.21 μM Compound: 5; AES-135	Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay Cytotoxicity against human MDA-MB-468 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay	[PMID: 31938464]
MOLM-13	IC₅₀	2.1 μM Compound: 5; AES-135	Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay Cytotoxicity against human MOLM13 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay	[PMID: 31938464]
MV4-11	IC₅₀	1.88 μM Compound: 5; AES-135	Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay Cytotoxicity against human MV4-11 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer blue assay	[PMID: 31938464]
MV4-11	IC₅₀	1.88 μM Compound: AES-135	Cytotoxicity against human MV4-11 cells after 72 hrs by CellTiter-Blue assay Cytotoxicity against human MV4-11 cells after 72 hrs by CellTiter-Blue assay	[PMID: 30776234]
Pa03C	IC₅₀	1.22 μM Compound: AES-135	Cytotoxicity against human Pa03C cells assessed as reduction in tumor spheroid area after 72 hrs by Alamar Blue assay Cytotoxicity against human Pa03C cells assessed as reduction in tumor spheroid area after 72 hrs by Alamar Blue assay	[PMID: 30776234]
Pa03C	IC₅₀	1.33 μM Compound: AES-135	Cytotoxicity against human Pa03C cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay Cytotoxicity against human Pa03C cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay	[PMID: 30776234]
Pa03C	IC₅₀	1.41 μM Compound: AES-135	Cytotoxicity against human Pa03C cells assessed as reduction in tumor spheroid area after 72 hrs in presence of human CAF19 cells by Alamar Blue assay Cytotoxicity against human Pa03C cells assessed as reduction in tumor spheroid area after 72 hrs in presence of human CAF19 cells by Alamar Blue assay	[PMID: 30776234]
Pa03C	IC₅₀	1.56 μM Compound: AES-135	Cytotoxicity against human Pa03C cells assessed as reduction in tumor spheroid intensity after 72 hrs in presence of human CAF19 cells by Alamar Blue assay Cytotoxicity against human Pa03C cells assessed as reduction in tumor spheroid intensity after 72 hrs in presence of human CAF19 cells by Alamar Blue assay	[PMID: 30776234]
Pa03C	IC₅₀	3.4 μM Compound: AES-135	Cytotoxicity against human Pa03C monolayer cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay Cytotoxicity against human Pa03C monolayer cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay	[PMID: 30776234]
Panc1005	IC₅₀	0.5 μM Compound: AES-135	Cytotoxicity against human Panc 10.05 cells assessed as reduction in tumor spheroid intensity after 72 hrs in presence of human CAF19 cells by Alamar Blue assay Cytotoxicity against human Panc 10.05 cells assessed as reduction in tumor spheroid intensity after 72 hrs in presence of human CAF19 cells by Alamar Blue assay	[PMID: 30776234]
Panc1005	IC₅₀	0.6 μM Compound: AES-135	Cytotoxicity against human Panc 10.05 cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay Cytotoxicity against human Panc 10.05 cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay	[PMID: 30776234]
Panc1005	IC₅₀	0.94 μM Compound: AES-135	Cytotoxicity against human Panc 10.05 cells assessed as reduction in tumor spheroid area after 72 hrs in presence of human CAF19 cells by Alamar Blue assay Cytotoxicity against human Panc 10.05 cells assessed as reduction in tumor spheroid area after 72 hrs in presence of human CAF19 cells by Alamar Blue assay	[PMID: 30776234]
Panc1005	IC₅₀	0.97 μM Compound: AES-135	Cytotoxicity against human Panc 10.05 cells assessed as reduction in tumor spheroid area after 72 hrs by Alamar Blue assay Cytotoxicity against human Panc 10.05 cells assessed as reduction in tumor spheroid area after 72 hrs by Alamar Blue assay	[PMID: 30776234]
Panc1005	IC₅₀	3.9 μM Compound: AES-135	Cytotoxicity against human Panc 10.05 monolayer cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay Cytotoxicity against human Panc 10.05 monolayer cells assessed as reduction in tumor spheroid intensity after 72 hrs by Alamar Blue assay	[PMID: 30776234]
Sf9	IC₅₀	> 1 μM Compound: 5; AES-135	Inhibition of recombinant full length human HDAC8 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC8 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 3 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	> 1 μM Compound: AES-135	Inhibition of recombinant human HDAC8 expressed in SF9 baculoviral system using FAM-labeled acetylated peptide as substrate by EMSA Inhibition of recombinant human HDAC8 expressed in SF9 baculoviral system using FAM-labeled acetylated peptide as substrate by EMSA	[PMID: 30776234]
Sf9	IC₅₀	0.19 μM Compound: 5; AES-135	Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 5 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC6 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 5 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.19 μM Compound: AES-135	Inhibition of recombinant human HDAC6 expressed in SF9 baculoviral system using FAM-labeled acetylated peptide as substrate by EMSA Inhibition of recombinant human HDAC6 expressed in SF9 baculoviral system using FAM-labeled acetylated peptide as substrate by EMSA	[PMID: 30776234]
Sf9	IC₅₀	0.636 μM Compound: 5; AES-135	Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 17 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC11 expressed in baculovirus infected Sf9 cells using FAM-RHKK-TFAc as substrate incubated for 17 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.636 μM Compound: AES-135	Inhibition of recombinant human HDAC11 expressed in SF9 baculoviral system using FAM-labeled acetylated peptide as substrate by EMSA Inhibition of recombinant human HDAC11 expressed in SF9 baculoviral system using FAM-labeled acetylated peptide as substrate by EMSA	[PMID: 30776234]
Sf9	IC₅₀	0.654 μM Compound: 5; AES-135	Inhibition of recombinant full length human HDAC3 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 3 hrs by electrophoretic mobility shift assay Inhibition of recombinant full length human HDAC3 expressed in baculovirus infected Sf9 cells using FAM-RHKK-Ac as substrate incubated for 3 hrs by electrophoretic mobility shift assay	[PMID: 31938464]
Sf9	IC₅₀	0.654 μM Compound: AES-135	Inhibition of recombinant human HDAC3 expressed in SF9 baculoviral system using FAM-labeled acetylated peptide as substrate by EMSA Inhibition of recombinant human HDAC3 expressed in SF9 baculoviral system using FAM-labeled acetylated peptide as substrate by EMSA	[PMID: 30776234]

体外研究
(In Vitro)

AES-135 inhibits cancer cells growth with IC₅₀ values of 2.3 µM, 1.4 µM, 0.27 µM, 0.94 µM, 1.9 µM, 2.72 µM, 2.1 µM, 15.0 µM, 1.6 µM and 19.2 µM for BT143, BT189, D425, D458, MV4-11, MOLM-13, MDA-MB-231, K562, PC-3 and MRC-9 cells, respectively^[1].

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

体内研究
(In Vivo)

AES-135 (50 mg/kg; intraperitoneal injection; 5 days a week; for 1 month) treatment significantly increases survival of C57Bl/6 mice implanted with KPC2 cells^[1].
NSG mice are dosed with a single 20 mg/kg intraperitoneal (IP) injection, and blood is taken at 0.5 h, 1 h, 2 h, 4 h, 8 h, and 24 h. AES-135 achieved μM concentrations in the blood, reaching C_max 7452 ng/mL (10.74 μM) within 30 min, which is sustained for 8 h. The blood concentration of AES-135 is dose dependent, achieving an average of 323 ng/mL (0.47 μM) with 10 mg/kg dosing and 1829 ng/mL (2.64 μM) with 40 mg/kg. AES-135 shows an impressive pharmacokinetic profile in mice with an in vivo half-life of 5.0 h^[1].

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

Animal Model:	C57Bl/6 mice injected with KPC2 cells^[1]
Dosage:	50 mg/kg
Administration:	Intraperitoneal injection; 5 days a week; for 1 month
Result:	Significantly increased survival of mice.

分子量

693.66

Formula

C₃₃H₂₉F₆N₃O₅S

CAS 号

2361659-61-0

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

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (144.16 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	1.4416 mL	7.2081 mL	14.4163 mL
5 mM	0.2883 mL	1.4416 mL	2.8833 mL
10 mM	0.1442 mL	0.7208 mL	1.4416 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。-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。

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 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.60 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。

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

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

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

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 98.21%

选择批次：

Data Sheet (627 KB) SDS (251 KB)

COA (179 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Shouksmith AE, et al. Identification and Characterization of AES-135, a Hydroxamic Acid-Based HDAC Inhibitor That Prolongs Survival in an Orthotopic Mouse Model of Pancreatic Cancer. J Med Chem. 2019 Mar 14;62(5):2651-2665. [Content Brief]

AES-135 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	1 mM	1.4416 mL	7.2081 mL	14.4163 mL	36.0407 mL
	5 mM	0.2883 mL	1.4416 mL	2.8833 mL	7.2081 mL
	10 mM	0.1442 mL	0.7208 mL	1.4416 mL	3.6041 mL
	15 mM	0.0961 mL	0.4805 mL	0.9611 mL	2.4027 mL
	20 mM	0.0721 mL	0.3604 mL	0.7208 mL	1.8020 mL
	25 mM	0.0577 mL	0.2883 mL	0.5767 mL	1.4416 mL
	30 mM	0.0481 mL	0.2403 mL	0.4805 mL	1.2014 mL
	40 mM	0.0360 mL	0.1802 mL	0.3604 mL	0.9010 mL
	50 mM	0.0288 mL	0.1442 mL	0.2883 mL	0.7208 mL
	60 mM	0.0240 mL	0.1201 mL	0.2403 mL	0.6007 mL
	80 mM	0.0180 mL	0.0901 mL	0.1802 mL	0.4505 mL
	100 mM	0.0144 mL	0.0721 mL	0.1442 mL	0.3604 mL

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:

AES-1352361659-61-0AES135AES 135HDACHistone deacetylasesHDAC3HDAC6HDAC11anti-tumorpancreaticInhibitorinhibitorinhibit

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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）

AES-135

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献