A-485

目录号: HY-107455 纯度: 99.87%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

A-485 是 p300/CBP 的强效选择性催化抑制剂，对 p300 和 CBP 组蛋白乙酰转移酶 (HAT) 的 IC₅₀ 值分别为 9.8 nM 和 2.6 nM。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

A-485 Chemical Structure

CAS No. : 1889279-16-6

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3895	In-stock
1 mg	￥1100	In-stock
5 mg	￥3300	In-stock
10 mg	￥5000	In-stock
50 mg	现货	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 53 篇科研文献

: A-485 purchased from MCE. Usage Cited in: Nat Immunol. 2023 Jan;24(1):162-173. [Abstract]; A485 (10 μM; 24 h) leads to the downregulation of H3K9bhb and CPS1 in BHB-treated CD8⁺ T_M cells; however, the use of 3-TYP (10 μM; 24 h) or Trichostatin A (TSA; 5 nM; 24 h) result in the increase of H3K9bhb and CPS1.

: A-485 purchased from MCE. Usage Cited in: Biomed Pharmacother. 2023 Feb 13;160:114402. [Abstract]; A485 (1, 3 µM; 4 h) reduces endogenous acetylation of NPM1 in HA-NPM1-transfected Huh7/SR NPM1 KD cells.

A-485 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Histone Acetyltransferase 亚型特异性产品:

查看所有亚型

CBP/p300 GCN5/PCAF TIP60 MOZ/MORF HBO1

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

A-485 is a potent and selective catalytic inhibitor of p300/CBP with IC₅₀s of 9.8 nM and 2.6 nM for p300 and CBP histone acetyltransferase (HAT), respectively^[1].

IC₅₀ & Target

CBP/p300

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	490 nM Compound: A-485	Antiproliferative activity against human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
K562	IC₅₀	457 nM Compound: A-485	Antiproliferative activity against human K562 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human K562 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
Kasumi 1	EC₅₀	0.33 μM Compound: A-485	Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability incubated for 5 days by XTT assay Antiproliferative activity against human Kasumi-1 cells assessed as reduction in cell viability incubated for 5 days by XTT assay	[PMID: 32314924]
Kasumi 1	IC₅₀	607.9 nM Compound: A-485	Antiproliferative activity against human Kasumi-1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human Kasumi-1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
LNCaP	EC₅₀	0.26 μM Compound: A-485	Antiproliferative activity against human LNCaP cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human LNCaP cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
LNCaP-Clone-FGC	EC₅₀	0.35 μM Compound: 1; A-485	Antiproliferative activity against AR-positive human LNCaP-Clone-FGC cells assessed as inhibition of cell proliferation measured after 5 days by luminiscent plate reader method Antiproliferative activity against AR-positive human LNCaP-Clone-FGC cells assessed as inhibition of cell proliferation measured after 5 days by luminiscent plate reader method	[PMID: 34055218]
LNCaP-Clone-FGC	IC₅₀	215 nM Compound: A-485	Antiproliferative activity against human LNCaP-FGC cells measured after 5 days by celltiter-glo luminescence assay Antiproliferative activity against human LNCaP-FGC cells measured after 5 days by celltiter-glo luminescence assay	[PMID: 31910017]
Maver1	IC₅₀	226.1 nM Compound: A-485	Antiproliferative activity against human Maver1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human Maver1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
MCF7	EC₅₀	> 30 μM Compound: A-485	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by Celigo-insitu cell cytometer analysis Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 6 days by Celigo-insitu cell cytometer analysis	[PMID: 32314924]
MCF7	EC₅₀	> 30 μM Compound: A-485	Antiproliferative activity against human tamoxifen-resistant MCF7 cells assessed as reduction in cell viability incubated for 6 days by Celigo-insitu cell cytometer analysis Antiproliferative activity against human tamoxifen-resistant MCF7 cells assessed as reduction in cell viability incubated for 6 days by Celigo-insitu cell cytometer analysis	[PMID: 32314924]
MDA-MB-231	EC₅₀	> 10 μM Compound: A-485	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
MM1.S	EC₅₀	139 nM Compound: A-485	Antiproliferative activity against human MM1.S cells assessed as reduction in cell proliferation incubated for 72 hrs by MTS assay Antiproliferative activity against human MM1.S cells assessed as reduction in cell proliferation incubated for 72 hrs by MTS assay	[PMID: 35814928]
MOLM-13	EC₅₀	0.35 μM Compound: A-485	Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human MOLM-13 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
MV4-11	IC₅₀	255.2 nM Compound: A-485	Antiproliferative activity against human MV4-11 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human MV4-11 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 31910017]
OVCAR-3	EC₅₀	5.44 μM Compound: A-485	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 120 hrs by Cell-titre glo assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell proliferation measured after 120 hrs by Cell-titre glo assay	[PMID: 34801827]
PANC-1	EC₅₀	> 30 μM Compound: A-485	Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability incubated for 5 days by MTT assay Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability incubated for 5 days by MTT assay	[PMID: 32314924]
PC-3	EC₅₀	2.1 μM Compound: A-485	Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human PC-3 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
RPMI-8226	EC₅₀	0.16 μM Compound: A-485	Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay Antiproliferative activity against human RPMI-8226 cells assessed as reduction in cell growth incubated for 3 to 5 days by CellTiter-Glo luminescent cell viability assay	[PMID: 35512565]
Sf9	IC₅₀	0.06 μM Compound: A-485	Inhibition of recombinant human N-terminal 6His-FLAG-tagged p300 BHC domain (1036 to 1822 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H4 peptide as substrate preincubated for 30 mins followed by substrate additi Inhibition of recombinant human N-terminal 6His-FLAG-tagged p300 BHC domain (1036 to 1822 residues) expressed in baculovirus infected Sf9 insect cells using biotinylated-histone H4 peptide as substrate preincubated for 30 mins followed by substrate additi	[PMID: 31910017]

体外研究
(In Vitro)

A three-hour treatment of prostate adenocarcinoma PC-3 cells with A-485 results in a dose-dependent decrease in H3K27Ac, with a half maximal effective concentration (EC₅₀) of 73 nM. Treatment with A-485 does not alter p300 or CBP protein levels.
The broadest sensitivity is observed in haematological tumours, where A-485 exhibits potent activity in most multiple myeloma cell lines, and in a subset of acute myeloid leukaemia lines and non-Hodgkin’s lymphoma lines. A-485 induces a comparable decrease in H3K27Ac in all five prostate cancer cell lines^[1].

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

体内研究
(In Vivo)

After tumours are established in SCID male mice, twice daily intraperitoneal injections of A-485 induce 54% tumour growth inhibition after 21 days of dosing (P<0.005 as compare to vehicle control). In addition, in tumour-bearing animals, dosing with A-485 for seven days induces a decrease in the mRNA levels of MYC and the AR-dependent gene SLC45A3 at three hours post-dosing, and (for MYC) a decrease in the protein level, indicating that A-485 inhibits p300-mediated transcriptional activity in vivo. However, at 16 hours post-dosing on the seventh day, A-485 drug levels in the plasma and tumour are decreased as compare to 3 hours. A-485 induces a moderate 9% body weight loss, and the animals recover rapidly upon completion of the A-485 dosing regimen^[1].

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

分子量

536.48

Formula

C₂₅H₂₄F₄N₄O₅

CAS 号

1889279-16-6

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 125 mg/mL (233.00 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	1.8640 mL	9.3200 mL	18.6400 mL
5 mM	0.3728 mL	1.8640 mL	3.7280 mL
10 mM	0.1864 mL	0.9320 mL	1.8640 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

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： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 11 mg/mL (20.50 mM); 悬浊液; 超声助溶
方案二

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.88 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
方案三

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.88 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
方案四

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.88 mM); 澄清溶液

此方案可获得 ≥ 2.08 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 20.8 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: 99.87%

选择批次：

Data Sheet (628 KB) SDS (393 KB)

COA (288 KB) LCMS (93 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Lasko LM, et al. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature. 2017 Oct 5;550(7674):128-132. [Content Brief]

Cell Assay ^[1]	Cell lines are plated in 96 well or 384 well plates and allowed to adhere for 24 h. The cells are then treated with A-485 for 3, 4, or 5 days. Experiments are run in triplicate and the fraction of viable cells is determined using the Cell Viability Assay according to the manufacturer’s recommendations. For Thymidine incorporation assays, cells are treated with A-485 for 1, 2, 3, or 4 days. Twenty four hours prior to the time point, tritiated thymidine is added and cells are incubated for an additional 24 h. Genomic DNA is then isolated on filter plates^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	The LuCap-77 CR prostate PDX model is used in this study. Donor tumors are dissociated and injected as a brie (1:2) into the right flank of 16 week old male C.B.-17 SCID mice on day 0 in a volume of 0.2 mL. Tumors are size matched on day 26 post-inoculation with a mean tumor volume of 211±3 (SEM) mm³ with dosing beginning on day 28. Mice are randomized into treatment groups using Studylog software based on tumor volume. LuCap-77 CR xenograft tumors are established in SCID mice and animals are dosed with A-485 as for 7 days. Three hours post the final dose, tumors are harvested and snap frozen on dry ice^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Lasko LM, et al. Discovery of a selective catalytic p300/CBP inhibitor that targets lineage-specific tumours. Nature. 2017 Oct 5;550(7674):128-132. [Content Brief]

A-485 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	1.8640 mL	9.3200 mL	18.6400 mL	46.6001 mL
	5 mM	0.3728 mL	1.8640 mL	3.7280 mL	9.3200 mL
	10 mM	0.1864 mL	0.9320 mL	1.8640 mL	4.6600 mL
	15 mM	0.1243 mL	0.6213 mL	1.2427 mL	3.1067 mL
	20 mM	0.0932 mL	0.4660 mL	0.9320 mL	2.3300 mL
	25 mM	0.0746 mL	0.3728 mL	0.7456 mL	1.8640 mL
	30 mM	0.0621 mL	0.3107 mL	0.6213 mL	1.5533 mL
	40 mM	0.0466 mL	0.2330 mL	0.4660 mL	1.1650 mL
	50 mM	0.0373 mL	0.1864 mL	0.3728 mL	0.9320 mL
	60 mM	0.0311 mL	0.1553 mL	0.3107 mL	0.7767 mL
	80 mM	0.0233 mL	0.1165 mL	0.2330 mL	0.5825 mL
	100 mM	0.0186 mL	0.0932 mL	0.1864 mL	0.4660 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:

A-4851889279-16-6A485A 485Epigenetic Reader DomainHistone AcetyltransferaseHATsHATInhibitorinhibitorinhibit

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

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）
Copyright © 2013-2024 MedChemExpress. All Rights Reserved.

A-485

Customer Review

MCE 顾客使用本产品发表的 53 篇科研文献

A-485 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Histone Acetyltransferase 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

A-485 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

A-485

Customer Review

A-485 相关抗体

MCE 顾客使用本产品发表的 53 篇科研文献

A-485 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Histone Acetyltransferase 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

A-485 相关抗体:

摩尔计算器

稀释计算器

A-485 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z