Onalespib (Synonyms: AT13387)

目录号: HY-14463 纯度: 99.62%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Onalespib (AT13387) 是一种长效的二代 Hsp90 抑制剂，K_d 值为 0.71 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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

Onalespib Chemical Structure

CAS No. : 912999-49-6

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	￥1190	In-stock
1 mg	￥490	In-stock
5 mg	￥1080	In-stock
10 mg	￥1674	In-stock
50 mg	￥4200	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Onalespib:

Onalespib lactate 询价
AT13387 trifluoroacetate 询价

MCE 顾客使用本产品发表的 9 篇科研文献

Proliferation Assay

: Onalespib purchased from MCE. Usage Cited in: Sci Rep. 2017 Mar 15;7(1):201. [Abstract]; For the caspase 3/7 assay, the HSP90 inhibitor-treated 5637 or SV-HUC cells are stained with Nexcelom ViaStain Caspase 3/7 reagent and Hoechst 33342. Caspase 3/7 positive cells are identified using the Celigo imaging cytometer, and the percentage of apoptotic caspase 3/7 positive cells is calculated with the Celigo software.

Onalespib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HSP 亚型特异性产品:

查看所有亚型

HSP40 HSP70 HSP90 HSP105 HSF1 HSP HSPA5

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Onalespib (AT13387) is a long-acting second-generation Hsp90 inhibitor with a K_d of 0.71 nM.

IC₅₀ & Target^[1]

HSP90

0.71 nM (Kd)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.05 μM Compound: 8; AT13387	Antiproliferative activity against human A549 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human A549 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
A549	IC₅₀	0.44 μM Compound: AT13387	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30784881]
BT-474	IC₅₀	0.032 μM Compound: 8; AT13387	Antiproliferative activity against human BT-474 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human BT-474 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
GIST430	IC₅₀	34 nM Compound: 8; AT-13387	Cytotoxicity against imatinib-resistant human GIST430 cells assessed as decrease in cell viability after 7 days by alamar blue assay Cytotoxicity against imatinib-resistant human GIST430 cells assessed as decrease in cell viability after 7 days by alamar blue assay	[PMID: 26844689]
GIST48	IC₅₀	55 nM Compound: 8; AT-13387	Cytotoxicity against imatinib-resistant human GIST48 cells assessed as decrease in cell viability after 7 days by alamar blue assay Cytotoxicity against imatinib-resistant human GIST48 cells assessed as decrease in cell viability after 7 days by alamar blue assay	[PMID: 26844689]
HCT-116	IC₅₀	0.07 μM Compound: 8; AT13387	Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
HCT-116	IC₅₀	0.08 μM Compound: AT-13387	Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 48 hrs by MTT assay	[PMID: 24763261]
HCT-116	IC₅₀	48 nM Compound: 35	Cytotoxicity against human HCT116 cells by Alamar blue assay Cytotoxicity against human HCT116 cells by Alamar blue assay	[PMID: 20662534]
HepG2	IC₅₀	0.018 μM Compound: 8; AT13387	Antiproliferative activity against human HepG2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human HepG2 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
K562	IC₅₀	0.038 μM Compound: 8; AT13387	Antiproliferative activity against human K562 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human K562 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
L02	IC₅₀	11.64 μM Compound: 8; AT13387	Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MCF7	IC₅₀	0.02 μM Compound: 8; AT13387	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MCF7	IC₅₀	0.032 μM Compound: AT13387	Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells incubated for 72 hrs by MTT assay	[PMID: 29028527]
MCF7	IC₅₀	0.28 μM Compound: AT-13387	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay	[PMID: 24763261]
MCF7	IC₅₀	0.29 μM Compound: AT13387	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30784881]
MDA-MB-231	IC₅₀	0.038 μM Compound: 8; AT13387	Antiproliferative activity against human MDA-MB-231 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MDA-MB-468	IC₅₀	0.066 μM Compound: 8; AT13387	Antiproliferative activity against human MDA-MB-468 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-468 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MKN-28	IC₅₀	0.129 μM Compound: 8; AT13387	Antiproliferative activity against human MKN-28 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MKN-28 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
MV4-11	IC₅₀	0.011 μM Compound: 8; AT13387	Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human MV4-11 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
NCI-H1299	IC₅₀	0.37 μM Compound: AT13387	Antiproliferative activity against human NCI-H1299 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H1299 cells after 72 hrs by MTT assay	[PMID: 30784881]
NCI-H3122	IC₅₀	52 nM Compound: AT13387	Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB assay	[PMID: 29698859]
SK-BR-3	IC₅₀	0.045 μM Compound: AT13387	Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human SKBR3 cells incubated for 72 hrs by MTT assay	[PMID: 29028527]
SK-BR-3	IC₅₀	0.071 μM Compound: 8; AT13387	Antiproliferative activity against human SK-BR-3 assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human SK-BR-3 assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
SK-BR-3	IC₅₀	0.14 μM Compound: AT-13387	Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay Antiproliferative activity against human SKBR3 cells after 48 hrs by MTT assay	[PMID: 24763261]
T47D	IC₅₀	0.024 μM Compound: 8; AT13387	Antiproliferative activity against human T47D assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human T47D assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]
U2OS	IC₅₀	0.067 μM Compound: 8; AT13387	Antiproliferative activity against human U2OS assessed as reduction in cell viability incubated for 72 hrs by MTT assay Antiproliferative activity against human U2OS assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 27933959]

体外研究
(In Vitro)

Onalespib (Compound 35) is a potent inhibitor of Hsp90, with K_d of 0.71 nM. Onalespib shows potent antiproliferative activity in HCT116 cells, with an IC₅₀ of 31 nM. Onalespib also strongly inhibits the proliferation of a panel of human tumor cell lines, showing IC₅₀ of < 100 nM^[1]. Onalespib exhibits cytotoxic activity against many of the PPTP cell lines, with median IC₅₀ of 41 nM^[2].

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

体内研究
(In Vivo)

Onalespib (60 mg/kg, ip 3 days on and 3 days off for four cycles) shows antitumor activity in nude BALB/c mice bearing early stage HCT116 human colon carcinoma xenografts^[1]. Onalespib (40 or 60 mg/kg, i.p.) induces significant differences in EFS distribution compared to controls in 17% evaluable solid tumor xenografts, but in none of the ALL xenografts^[2].

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

Clinical Trial

分子量

409.52

Formula

C₂₄H₃₁N₃O₃

CAS 号

912999-49-6

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 : 50 mg/mL (122.09 mM; 超声助溶 (<60°C); 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	2.4419 mL	12.2094 mL	24.4188 mL
5 mM	0.4884 mL	2.4419 mL	4.8838 mL
10 mM	0.2442 mL	1.2209 mL	2.4419 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： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.10 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 (6.10 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 (6.10 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： 50% PEG300 50% Saline
Solubility: 16.67 mg/mL (40.71 mM); 悬浊液; 超声助溶

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: 99.62%

选择批次：

Data Sheet (625 KB) SDS (393 KB)

COA (285 KB) LCMS (260 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Woodhead AJ, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53 [Content Brief]

[2]. Kang MH, et al. Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Jul 15;59(1):185-8. [Content Brief]

Cell Assay ^[2]	In vitro testing is performed using DIMSCAN. Cells are incubated in the presence of Onalespib for 96 hours at concentrations from 1 nM to 10 μM^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	HCT116 cells are injected SC into the right hind flank of male nude BALB/c mice. Tumours are apparent 7 to 10 days later. Mice are arranged into matched groups of 12 according to tumour volume giving a group mean of approximately 100 mm^[3] at initiation of dosing. Tumour volumes are measured every 2 days. Statistical significance between groups is assessed using nonparametric one-way ANOVA. Mice are given the lactate salt of Onalespib using a repeated cycle of dosing of once per day for three days, no dose for three days, once per day for three days etc., for four dosing cycles at 60 mg/kg/dose (as free base equivalents) dissolved in 17.5% hydroxypropyl-β-cyclodextrin via the IP route. Control mice receive dose vehicle only via the same route. Tolerability is assessed by recording body weight, clinical observations and survival^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Woodhead AJ, et al. Discovery of (2,4-dihydroxy-5-isopropylphenyl)-[5-(4-methylpiperazin-1-ylmethyl)-1,3-dihydroisoindol-2-yl]methanone (AT13387), a novel inhibitor of the molecular chaperone Hsp90 by fragment based drug design. J Med Chem. 2010 Aug 26;53 [Content Brief] [2]. Kang MH, et al. Initial testing (Stage 1) of AT13387, an HSP90 inhibitor, by the pediatric preclinical testing program. Pediatr Blood Cancer. 2012 Jul 15;59(1):185-8. [Content Brief]

Onalespib 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	2.4419 mL	12.2094 mL	24.4188 mL	61.0471 mL
	5 mM	0.4884 mL	2.4419 mL	4.8838 mL	12.2094 mL
	10 mM	0.2442 mL	1.2209 mL	2.4419 mL	6.1047 mL
	15 mM	0.1628 mL	0.8140 mL	1.6279 mL	4.0698 mL
	20 mM	0.1221 mL	0.6105 mL	1.2209 mL	3.0524 mL
	25 mM	0.0977 mL	0.4884 mL	0.9768 mL	2.4419 mL
	30 mM	0.0814 mL	0.4070 mL	0.8140 mL	2.0349 mL
	40 mM	0.0610 mL	0.3052 mL	0.6105 mL	1.5262 mL
	50 mM	0.0488 mL	0.2442 mL	0.4884 mL	1.2209 mL
	60 mM	0.0407 mL	0.2035 mL	0.4070 mL	1.0175 mL
	80 mM	0.0305 mL	0.1526 mL	0.3052 mL	0.7631 mL
	100 mM	0.0244 mL	0.1221 mL	0.2442 mL	0.6105 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:

Onalespib912999-49-6AT13387AT 13387AT-13387HSPHeat shock proteinsInhibitorinhibitorinhibit

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.

Onalespib (Synonyms: AT13387)

Customer Review

Other Forms of Onalespib:

MCE 顾客使用本产品发表的 9 篇科研文献

Onalespib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HSP 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

Onalespib 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.

Onalespib (Synonyms: AT13387)

Customer Review

Other Forms of Onalespib:

Onalespib 相关抗体

MCE 顾客使用本产品发表的 9 篇科研文献

Onalespib 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 HSP 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

Onalespib 相关抗体:

摩尔计算器

稀释计算器

Onalespib 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