Onalespib (AT13387)

For research use only. Not for use in humans.

目录号:S1163

Onalespib (AT13387) Chemical Structure

CAS No. 912999-49-6

Onalespib (AT13387)是一种有效的,选择性Hsp90抑制剂,在A375细胞中IC50为18 nM,具有长持续性抗肿瘤活性。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 3603.79 现货
RMB 2232.47 现货
RMB 3048.94 现货
RMB 8763.3 现货
RMB 16298.1 现货
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客户使用Selleck生产的Onalespib (AT13387)发表文献19篇:

产品安全说明书

HSP (HSP90)抑制剂选择性比较

生物活性

产品描述 Onalespib (AT13387)是一种有效的,选择性Hsp90抑制剂,在A375细胞中IC50为18 nM,具有长持续性抗肿瘤活性。Phase 2。
靶点
HSP90 [1]
(Cell-free assay)
18 nM
体外研究

AT13387抑制多种激酶,包括 CDK 1, CDK 2, CDK4, FGFR3, PKB-b, JAK2, VEGFR2, PDGFR-b ,和Aurora B。但是AT13387浓度低于30 μM时对实验激酶没有明显抑制效果。AT13387 有效抑制多种肿瘤细胞系(如 MES-SA 细胞系)增殖和存活。AT13387作用于一组30个肿瘤细胞系,有效抑制细胞增殖,GI50值为13-260 nM。AT13387抑制非致瘤性前列腺上皮细胞系PNT2增殖,GI50值为480 nM。[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human HCT116 cells Mn3XR5l1d3SxeHnjxsBie3OjeR?= NUK2OlFkS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hUEOWMUG2JINmdGy|IHL5JGFt[W2jcjDicJVmKGG|c3H5MEBKSzVyPUCuNFQ5KM7:TR?= NYHrTYFKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2OlI2OzRpPkKwOlYzPTN2PD;hQi=>
human HCT116 cells MUPGeY5kfGmxbjDhd5NigQ>? MlT0NVAhdk1? MnLsNVghcA>? MonpTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhfXC{ZXf1cIF1cW:wIH;mJGh{eDdyIHzleoVtKGG2IEGwJI5OKGGodHXyJFE5KGi{czDifUBqdW23bn;icI91fGmwZx?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ4MkWzOEc,OjB4NkK1N|Q9N2F-
human HCT116 cells Ml3wSpVv[3Srb36gZZN{[Xl? M1rxS|MxKG6P MVGxPEBp MUXJcoR2[3Srb36gc4Yh[XCxcITvd4l{KGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hd2ZiQ1TLOEBt\X[nbDDheEA{OCCwTTDh[pRmeiBzODDodpMh[nliaX3teY5w[myxdITpcoc> MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODZ4MkWzOEc,OjB4NkK1N|Q9N2F-
human HCT116 cells NHjPUHZHfW6ldHnvckBie3OjeR?= NXPjWXFmOzBibl2= MUixPEBp MonqTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMhemWmdXP0bY9vKG:oIGLh[k0yKGyndnXsJIF1KDNyIH7NJIFnfGW{IEG4JIhzeyCkeTDpcY12dm:kbH;0eIlv\w>? MnPDQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjB4NkK1N|QoRjJyNk[yOVM1RC:jPh?=
human HCT116 cells M3rkWnBzd2yrZnXyZZRqd25iYYPzZZk> Mo\TOFghcA>? M{DtcWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSFPUNVE3KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6wPEDPxE1? NV6wOYhRRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS3OlMzPjFpPkK0O|Y{OjZzPD;hQi=>
human SKBR3 cells MnjOVJJwdGmoZYLheIlwdiCjc4PhfS=> M3;VV|Q5KGh? NIXINFlCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLRnI{KGOnbHzzJIFnfGW{IES4JIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD6xOEDPxE1? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDd4M{K2NUc,OjR5NkOyOlE9N2F-
human MCF7 cells MnWwVJJwdGmoZYLheIlwdiCjc4PhfS=> NGT4dVg1QCCq NEfSfndCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF3DSlch[2WubIOgZYZ1\XJiNEigbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkK4JO69VQ>? M2TtZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2N{[zNlYyLz5{NEe2N|I3OTxxYU6=
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GIST430 M{D0cWN6fG:2b4jpZ4l1gSCjc4PhfS=> M4j2Vlch\GG7cx?= M1vFXGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGmvYYTpcoljNXKnc3nzeIFvfCCqdX3hckBIUVOWNEOwJINmdGy|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEeg[IF6eyCkeTDhcIFu[XJiYnz1[UBie3OjeTygTWM2OD1yLkCzOO69VS5? MoPaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjZ6NES2PFkoRjJ4OES0Olg6RC:jPh?=
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RD MnTHdWhVWyCjc4PhfS=> MYjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSSEBk\Wyucx?= NUX2OmNkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 NVj5WINteUiWUzDhd5NigQ>? Mn;tdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVogyQCClZXzsdy=> NWnC[VlDRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh30 M4XVZZFJXFNiYYPzZZk> M17hT5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOzBiY3XscJM> MlXNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH MnXkdWhVWyCjc4PhfS=> NVLwelZYeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= NYTx[Hd2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NCI-H3122 M3\YbWFvfGmycn;sbYZmemG2aY\lJIF{e2G7 NYXqVIE3PzJiaILz NEDUenpCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIF7DTU1JOzF{MjDj[YxteyCjZoTldkA4OiCqcoOgZpkhW1KEIHHzd4F6NCCLQ{WwQVAvODV{zszNMi=> M4foXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7Nkm4PFU6Lz5{OU[5PFg2QTxxYU6=
PANC1 M3;DcGZ2dmO2aX;uJIF{e2G7 NGTWSosyKHWP M4LWZVM3KGi{cx?= NGf4bodKdmirYnn0bY9vKG:oIFjTVFkx[WyyaHGgbY4hcHWvYX6gVGFPSzFiY3XscJMh[XO|ZYPz[YQh[XNidYCtdoVofWyjdHnvckBw\iCKc4C3NEBifCBzIIXNJIFnfGW{IEO2JIhzeyCkeTDX[ZN1\XKwIHLsc5Qh[W6jbInzbZM> NFjDWpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO1NVAxOSd-M{CzOVExODF:L3G+
PANC1 NYHIeWR7TnWwY4Tpc44h[XO|YYm= M3\Jc|EhfU1? MVGzOkBpenN? MXXJcohq[mm2aX;uJI9nKEiVUEmwZYxxcGFiaX6gbJVu[W5iUFHOR|Eh[2WubIOgZZN{\XO|ZXSgZZMh[Wu2IHTl[5Ji\GG2aX;uJIF1KDFidV2gZYZ1\XJiM{[gbJJ{KGK7IGfld5Rmem5iYnzveEBidmGueYPpdy=> NGDjPVA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO1NVAxOSd-M{CzOVExODF:L3G+
MCF7 NWXRb4g5SW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MXW3NkBpenN? MXXBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2FRkegZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjJ7zszNMi=> NH\wR4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEe4OFg5OSd-M{C3PFQ5QDF:L3G+
NCI-H1299 NILVV3VCdnSrcILvcIln\XKjdHn2[UBie3OjeR?= MXu3NkBpenN? M3\ydmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTlPJMWgyOjl7IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEmFNUC9NE4{P87:TT6= NYHkbJR3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C3PFQ5QDFpPkOwO|g1QDhzPD;hQi=>
A549 Ml7aRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? MVS3NkBpenN? MW\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEF3NEmgZ4VtdHNiYX\0[ZIhPzJiaILzJIJ6KE2WVDDhd5NigSxiSVO1NF0xNjR2zszNMi=> M4TLVlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyN{i0PFgyLz5|MEe4OFg5OTxxYU6=
Vero E6 NUDNcWRtTnWwY4Tpc44h[XO|YYm= M4K2bVQ5KGi{cx?= M2rme2lEPTBiZn;yJIFvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JHNCWlNvQ3;WMVIhcW5idHjlJHZmem9iRU[gZ4VtdCCuaX7lJIF1KDR6IHigZpkhcW2vdX7v[ox2d3Knc3PlcoNmNWKjc3XkJIF{e2G7IDjk[ZRm[3SrbnegeIhmKH[rcnHsJG5RKHC{b4TlbY4hcW5idHjlJI52[2yndYOgc4YhfGinIG\ldo8hTTZiY3XscJMqNCCLQ{WwQVAvOTV2OElOwG0v NUfEW25SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{KzOVM5PTlpPkOyN|U{QDV7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AXL / c-Myc / p-Mnk1 / Mnk1 / p-eIF4E / eIF4E ; 

PubMed: 31431614     


Immunoblots of A549 and A549R cells treated with onalespib for the indicated time. 

EGFR / p-EGFR / AKT / p-AKT / ERK / p-ERK / S6 / p-S6 ; 

PubMed: 28679777     


LN229, U251HF and A172 cells were exposed to 0.1, 0.2 and 0.4 μM onalespib for 48 h before being evaluated for the expression of EGFR, pEGFR, AKT, pAKT, ERK1/2, p-ERK1/2, S6, p-S6 by immunoblotting. GAPDH was assayed as a loading control.

HSP90 / HSP70 ; 

PubMed: 28679777     


HSP90 and HSP70 protein expression (upper panel) were evaluated by immunoblotting after treatment with onalespib 0.1, 0.2 and 0.4 μM for 48h on LN229, U251HF and A172 cell lines; GAPDH was used as loading control (lower panel). Immunoblots are representative of three independent experiments and DMSO was used as vehicle control.

31431614 28679777
Growth inhibition assay
Cell viability; 

PubMed: 28679777     


MES (GSC2 and GSC20) and PN (GSC11 and GSC23) GSC lines were exposed to increasing concentrations and times of onalespib before being assayed for viability using the WST-1 assay in all four GSC lines *p<0.05. Data represents the mean ± SEM of triplicate values from two independent experiments. 

28679777
体内研究 AT13387按70 mg/kg剂量每周处理两次,或者按90 mg/kg剂量每周处理一次。鼠体重降低不超过20%。非治疗期延长,及抗癌活性,与AT13387作用于突变EGFR和其他生物标签的长期药效,及AT13387对肿瘤的记忆有关。[2]

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)

激酶实验:[2]
- 合并

HSP90竞争等温热量测定:

竞争等温热量测定(ITC)格式测定AT13387与HSP90结合的Kd值。ITC 实验在Micro Cal VP-ITC上 25oC下进行,实验buffer含 25 mM Tris, 100 mM NaCl, 1 mM MgCl2 和 1 mM Tris(2-羧乙基) 磷化氢,pH 为7.4,为了获得高亲和力。
细胞实验:[2]
- 合并
  • Cell lines: A375, 22RV1, T474
  • Concentrations: 1 μM
  • Incubation Time: 4小时
  • Method: A375, 22RV1, T474, DU1 45, LNCa P, MCF-7, DA-MB-468 细胞系接种在96孔板上,然后加入溶于0.1% (v/v)DMSO的AT13387。使用10孔剂量反应曲线,测定GI50值,重复2次。然后加入Alamar blueis,细胞再温育4小时,然后读取荧光值。
    (Only for Reference)
动物实验:[2]
- 合并
  • Animal Models: 无胸腺BALB /c鼠
  • Dosages: 80 mg/kg
  • Administration: 腹腔注射
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 25 mg/mL (61.04 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
2% DMSO+30% PEG 300+ddH2O (prepare before use)
10mg/mL

* 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

分子量 409.52
化学式

C24H31N3O3

CAS号 912999-49-6
储存条件 粉状
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
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

计算器

摩尔浓度计算器

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

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

  • 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

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

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

技术支持

在订购、运输、储存和使用我们的产品的任何阶段,您遇到的任何问题,均可以通过拨打我们的热线电话400-668-6834,或者技术支持邮箱tech@selleck.cn,直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题,请给我们留言。

  • * 必填项

常见问题及建议解决方法

  • 问题 1:

    How to prepare the compound for in vivo studies?

  • 回答:

    S1163 AT13387 can be dissolved in 2% DMSO/30% PEG 300/ddH2O at 10 mg/ml as a clear solution. But after stayed for about 1 hour, the precipitation will goes out. So it is recommended to be prepared before use.

HSP (HSP90) Signaling Pathway Map

HSP (HSP90) Inhibitors with Unique Features

相关HSP (HSP90)产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID