Rabusertib (LY2603618)

For research use only. Not for use in humans.

目录号:S2626 别名: IC-83

Rabusertib (LY2603618) Chemical Structure

CAS No. 911222-45-2

Rabusertib (LY2603618, IC-83) 是一种具有高度选择性的Chk1抑制剂,在无细胞试验中具有潜在的抗肿瘤活性,IC50=7 nM,对Chk1的效力比对其他多种检测的蛋白激酶高100倍以上。Rabusertib (LY2603618) 在癌细胞中可诱导细胞周期阻滞、DNA损伤响应和自噬。Rabusertib (LY2603618) 可诱导AML细胞系中bak依赖的凋亡。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 2448.74 现货
RMB 1381.01 现货
RMB 2609.14 现货
RMB 7940.98 现货
RMB 20229.3 现货
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客户使用Selleck生产的Rabusertib (LY2603618)发表文献62篇:

产品安全说明书

Chk抑制剂选择性比较

生物活性

产品描述 Rabusertib (LY2603618, IC-83) 是一种具有高度选择性的Chk1抑制剂,在无细胞试验中具有潜在的抗肿瘤活性,IC50=7 nM,对Chk1的效力比对其他多种检测的蛋白激酶高100倍以上。Rabusertib (LY2603618) 在癌细胞中可诱导细胞周期阻滞、DNA损伤响应和自噬。Rabusertib (LY2603618) 可诱导AML细胞系中bak依赖的凋亡。
靶点
Chk1 [1]
(Cell-free assay)
7 nM
体外研究

Chk 1是一种ATP依赖苏氨酸蛋白激酶和在双链断裂(DSBs)引发的DNA复制检查点系统中的关键蛋白。Chk 1参与所有当前探明的细胞周期检查点,包括G1/S, S期,G 2 /M期,和有丝分裂纺锤体检查点。LY2603618可通过抑制Chk 1活性,干扰由生化试剂造成的DNA损伤的修复,从而增强各种化疗药物的抗肿瘤疗效。不过目前并未见有临床实验报道[1]。抑制Chk 1可提高抗代谢药物的作用,如gemcitabine [2]。LY2603618处理损害DNA合成,增加DNA损伤(通过细胞分裂的缺陷),诱导细胞凋亡,可与pemetrexed协同使用,特别对p53突变的肿瘤细胞作用更强[3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT474 MnvnT4lv[XOnIHHzd4F6 NHS0RmIyKM7:TR?= NGHQeVNFVVOR NFTtS4FqdmirYnn0d{BRNUOKS{GgcIV3\Wy| NXroXFdkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO5NVc{PzhpPkKzPVE4Ozd6PD;hQi=>
MCF7 NFfaPJlMcW6jc3WgZZN{[Xl? M3mzVVEh|ryP M2Ph[mROW09? M2rmdIlvcGmkaYTzJHAuS0iNMTDs[ZZmdHN? MnrjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN7MUezO|goRjJ|OUG3N|c5RC:jPh?=
Hela NV\hcnN3U2mwYYPlJIF{e2G7 MYKzN|AxKG6P NHzlTHVFVVOR M2S1OYlvcGmkaYTzJGNpczFiYXP0bZZqfHl? M3zSfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2MUG0NVI1Lz5{NEGxOFEzPDxxYU6=
Calu6 MojmT4lv[XOnIHHzd4F6 M4\De|M{ODBibl2= NGDUeXZFVVOR NFvudZJqdmirYnn0d{BEcGtzIHHjeIl3cXS7 NUX5RoMyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNVQyOjRpPkK0NVE1OTJ2PD;hQi=>
A549 MXrGeY5kfGmxbjDhd5NigQ>? M1vx[Z4yOCEQvF2= MULEUXNQ MWPpcoR2[2W|IHPlcIwh[3mlbHWgZZJz\XO2 MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl{OEKwOUc,OjR7MkiyNFU9N2F-
H1299 NXjuRZF2TnWwY4Tpc44h[XO|YYm= NYDidGxrhjFyIN88US=> NF;YdWdFVVOR MoPZbY5lfWOnczDj[YxtKGO7Y3zlJIFzemW|dB?= NYmzfGp2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NlgzODVpPkK0PVI5OjB3PD;hQi=>
A549 NWiyW4hOTnWwY4Tpc44h[XO|YYm= MXj+NlAh|ryP NWTqNW5KTE2VTx?= MorSZYN1cX[jdHXzJGRPSSCmYX3h[4Uhe2Wwc3;yJItqdmG|ZYO= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDl{OEKwOUc,OjR7MkiyNFU9N2F-
H1299 MWjGeY5kfGmxbjDhd5NigQ>? MkOzglIxKM7:TR?= NES2cHBFVVOR Ml\SZYN1cX[jdHXzJGRPSSCmYX3h[4Uhe2Wwc3;yJItqdmG|ZYO= NIPTXmU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmyPFIxPSd-MkS5NlgzODV:L3G+
A549 NXTXfIFpSXCxcITvd4l{KGG|c3H5 NUHTbYNYhjJyIN88US=> NUjTNIt1TE2VTx?= M3jlWIlv\HWlZYOgZZBweHSxc3nz M4foW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUK4NlA2Lz5{NEmyPFIxPTxxYU6=
H1299 NYrqTY85SXCxcITvd4l{KGG|c3H5 MmjuglIxKM7:TR?= MVHEUXNQ NUXjeplocW6mdXPld{BieG:ydH;zbZM> M{fvc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUK4NlA2Lz5{NEmyPFIxPTxxYU6=
A549 Ml\lR5l1d3irY3n0fUBie3OjeR?= MUf+NlAh|ryP NXq4Z4J3TE2VTx?= MWLpcoR2[2W|IHH1eI9xcGGpeR?= NY[1W5NvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NlgzODVpPkK0PVI5OjB3PD;hQi=>
H1299 NGLie2pEgXSxeHnjbZR6KGG|c3H5 NHjTbWp,OjBizszN NILz[FFFVVOR NH6yfHBqdmS3Y3XzJIF2fG:yaHHnfS=> M2H1R|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUK4NlA2Lz5{NEmyPFIxPTxxYU6=
A549 NVrCRXVETnWwY4Tpc44h[XO|YYm= MWr+NlAh|ryP NWD6ZXJPTE2VTx?= NI\kVWlqdmO{ZXHz[ZMhUk6NIHHu[EBxOzhiTVHQT{BxcG:|cHjvdplt[XSrb36= M2XENlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUK4NlA2Lz5{NEmyPFIxPTxxYU6=
H1299 NWC0bmVtTnWwY4Tpc44h[XO|YYm= MkPkglIxKM7:TR?= MV7EUXNQ NF:4TXVqdmO{ZXHz[ZMhUk6NIHHu[EBxOzhiTVHQT{BxcG:|cHjvdplt[XSrb36= MlrUQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR7MkiyNFUoRjJ2OUK4NlA2RC:jPh?=
OHS-50 MWTxTHRUKGG|c3H5 MWPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MnnmQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 MoHldWhVWyCjc4PhfS=> Moj1dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= M172PFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MV\xTHRUKGG|c3H5 NUXIcokxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uVUNiY3XscJM> MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 MmfpdWhVWyCjc4PhfS=> MUPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NX\4dWFWRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 MkezdWhVWyCjc4PhfS=> MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NVG5XYVpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Chk1 / Chk1 / CDC25A ; 

PubMed: 29326282     


CHK1 inhibition was monitored by measuring levels of CHK1 p-S345 and CDC25A by western blots. Cells were treated with various concentrations of LY2603618 for 8 h. 

PARP / CF-PARP / p-CDC25C / p-CDK1 / p-CDK2 ; 

PubMed: 25458954     


BxPC-3 cells were treated with vehicle control, MK-1775 (MK), LY2603618 (LY) or MK-1775 plus LY2603618 for 48 h. Protein extracts were subjected to Western blotting and probed with anti-PARP, -p-CHK1, -CHK1, -p-CDC25C, -p-CDK1, -CDK1, -p-CDK2, -CDK2, -γH2AX, or -β-actin antibody. 

29326282 25458954
Growth inhibition assay
Cell viability; 

PubMed: 29326282     


MTT assay following CHK1 inhibition by LY2603618 in BC cells with higher RNF126 expression vs. BC cells with lower RNF126 expression. Cells were treated with various concentrations of LY2603618 for 72 h. n=3. (Two-way ANOVA, P(BT474 VS. MDA-MB-231)<0.001; P(BT474 VS. MDA-MB-468)<0.001; P(ZR751 VS. MDA-MB-231)<0.001; P(ZR751 VS. MDA-MB-468)<0.001).

29326282
体内研究 在异种移植模型中,LY2603618可与pemetrexed联合使用抑制肿瘤生长[3]

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)

细胞实验:

[4]

- 合并
  • Cell lines: A549 and H1299 cell
  • Concentrations: 5 or 10 μM
  • Incubation Time: 24 h
  • Method:

    Cells were treated with LY2603618 and DMSO as a control. After trypsinization, cells were fixed in 70 % ethanol at 4 C overnight. The cells were washed twice with PBS and incubated for 30 min in the dark in PBS containing propidium iodide (PI) and RNase A. Stained cells were analyzed by a FACScan flow cytometry and CellQuest analysis software.


    (Only for Reference)

溶解度 (25°C)

体外 DMSO 13 mg/mL (29.79 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):
5% DMSO+ 40% PEG 300+5% Tween 80 +50% ddH2O
1mg/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 436.3
化学式

C18H22BrN5O3

CAS号 911222-45-2
储存条件 粉状
溶于溶剂
别名 IC-83

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

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01341457 Completed Drug: LY2603618|Drug: Gemcitabine Solid Tumors Eli Lilly and Company May 2011 Phase 1
NCT01296568 Completed Drug: LY2603618|Drug: Pemetrexed|Drug: Gemcitabine Advanced Cancer Eli Lilly and Company February 2011 Phase 1
NCT01139775 Completed Drug: Pemetrexed|Drug: Cisplatin|Drug: LY2603618 Non Small Cell Lung Cancer Eli Lilly and Company February 2011 Phase 1|Phase 2
NCT00988858 Completed Drug: LY2603618|Drug: Pemetrexed Non Small Cell Lung Cancer Eli Lilly and Company November 2009 Phase 2
NCT00839332 Completed Drug: LY2603618|Drug: Gemcitabine Pancreatic Neoplasms Eli Lilly and Company February 2009 Phase 1|Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID