Prexasertib HCl (LY2606368)

For research use only. Not for use in humans.

目录号:S7178

Prexasertib HCl (LY2606368) Chemical Structure

CAS No. 1234015-54-3

Prexasertib (LY2606368)是CHK1的ATP竞争性抑制剂,Ki值为0.9 nM。在cell-free实验中,LY2606368对CHK2RSK的IC50值分别为8 nM和9 nM。

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客户使用Selleck生产的Prexasertib HCl (LY2606368)发表文献13篇:

客户使用该产品的1个实验数据:

  • EW8 and TC71 cells were treated with increasing doses of prexasertib for 6 hours. Cell lysates were then collected and blotted for p-CHK1-345.

    Mol Cancer Ther, 2018, 17(12):2676-2688. Prexasertib HCl (LY2606368) purchased from Selleck.

产品安全说明书

Chk抑制剂选择性比较

生物活性

产品描述 Prexasertib (LY2606368)是CHK1的ATP竞争性抑制剂,Ki值为0.9 nM。在cell-free实验中,LY2606368对CHK2RSK的IC50值分别为8 nM和9 nM。
靶点
Chk1 [1]
(Cell-free assay)
Chk2 [1]
(Cell-free assay)
RSK [1]
(Cell-free assay)
0.9 nM(Ki) 8 nM 9 nM
体外研究

在临床前研究中发现,LY2606368可诱导DNA损伤[1]。对细胞予以LY2606368的处理将导致处于S期的细胞很快出现TUNEL和pH2AXy阳性的双链DNA断裂。在含p53缺陷的HeLa细胞中,LY2606368可有效取消doxorubicin激活的G2-M检查点,EC50为9 nM。LY2606368可广泛地在多种细胞中发挥抗增殖作用,在多数敏感细胞系中,IC50s < 50 nM;仅有少数细胞系对LY2606368具有抗性,IC50s > 1000 nM。LY2606368造成DNA损伤需要CDC25A和CDK2[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HeLa cells Mlu4SpVv[3Srb36gZZN{[Xl? NUfxbllFOzNib4KgNVAxKG6vb3yvUC=> NFPxN4k4KGixdYLz Mk\3ZpkhPyCqb4Xyd{wh[SC|dXLwc5B2dGG2aX;uJI9nKGOnbHzzJJN1[WmwZXSgd5Rzd26pbImg[o9zKESVQjDifUBjd3SqIGTVUmVNKGGwZDDwTFJCYA>? MlWxNlYyPDF7NEi=
U-2 OS cells NWm0dmVPTnWwY4Tpc44h[XO|YYm= M3\uTFQhdm2xbD;M NGDkS3AzPCCq NEjN[nhiKGyjcnflJJNpcW[2IHnuJINmdGxvY4njcIUheG:ydXzheIlwdnNiZoLvcUBIOSCjbnSgS|LjiJOPIITvJHMueGijc3Wge4l1cCCjbjDhZ4NwdXCjbnnl[EBqdmS3Y4Tpc44hd2ZiSELBXEBxcG:|cHjvdplt[XSrb36u NVvseVhCOjZzNEG5OFg>
CCRF-CEM parental cells NFvMT5BHfW6ldHnvckBie3OjeR?= M3fjS|ExKG6P M2X0blQhcA>? NUPqRZpNcW6mdXPl[EBUVE[QMUGgZolv\GmwZzD0c{BkcHKxbXH0bY4h[W6mIHnuZ5Jm[XOnZDD0bIUh[2i{b33heIlvKGKrbnTpcochd2ZiQ1TDOFU> Mnq1Nlk{QTVyNkG=
SLFN11-del cells M{fLUmZ2dmO2aX;uJIF{e2G7 MWqxNEBvVQ>? MUi0JIg> M{DiU4lv\HWlZXSgV2xHVjFzIHLpcoRqdmdidH:gZ4hzd22jdHnuJIFv\CCrbnPy[YF{\WRidHjlJINpem:vYYTpckBjcW6maX7nJI9nKEOGQ{S1 MknYNlk{QTVyNkG=
K562-WT Ml7sSpVv[3Srb36gZZN{[Xl? NE\T[GwyODBibl2= M3T4XVIhcA>? MXfTUGZPOTFuIFPER|Q2KGGwZDDQR25CKHencnWg[Y5zcWOqZXSgc44hdmG|Y3XueEBFVkF? NUnEbYdoOjl|OUWwOlE>
K562-E669Q Mn\XSpVv[3Srb36gZZN{[Xl? NWjDeFdoOTByIH7N NHP0[4ozKGh? NYDWVYJMW0yITkGxMEBETEN2NTDhcoQhWEOQQTD3[ZJmKGWwcnnjbIVlKG:wIH7hd4NmdnRiRF7B NYKzXow5Ojl|OUWwOlE>
CCRF-CEM parental cells MmTqSpVv[3Srb36gZZN{[Xl? NVzXbVBUOTByIH7N M4O2OVIhcA>? MmfNV2xHVjFzLDDDSGM1PSCjbnSgVGNPSSC5ZYLlJIVvemmlaHXkJI9vKG6jc3PlcpQhTE6D MXGyPVM6PTB4MR?=
HCT-116 cells MmGzSpVv[3Srb36gZZN{[Xl? MojUNVDjiK:mYYnz MVfpcohq[mm2ZXSgZo91cCCIQV7DSFIhfWKrcYXpeIlv[XSrb36gZY5lKGmwY4LlZZNm\CCUYXS1NUBt\X[nbIOsJJNq\26rZnnjZY51dHliaX7jdoVie2WmIIPlcpNqfGm4aYT5JI9nKEiFVD2xNVYh[2WubIOgeI8hTjFy NIPUdYQ{ODR|OUW2Oy=>
U937 cells M{HXOWZ2dmO2aX;uJIF{e2G7 NEHoUpo{6oDLbl2= MYTlcohidmOnZDD0bIUh[3m2b4TvfIlkcXS7IH;mJGNRYC1|NUGgZZQhdG:5IH7hco9ud2yjcjDjc45k\W62cnH0bY9vew>? MXuzNFg{PzZ2Mx?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CHK1 / p-CHK1(Ser345) / γH2AX / Cleaved caspase3 ; 

PubMed: 28401005     


E, F. Western blot analyses of AGS and MKN1 cells treated with LY2606368 for 24 hours. Endogenous Chk1, γ-H2AX, cleaved caspase3, and p-Chk1 (Ser345) were detected using their respective antibodies as shown left to each panel.

pS6 (S235/236) / pS6 (S240/244); 

PubMed: 28490518     


Immunoblot analysis of H69 and H69/CR cells before and after treatment with LY2606368 (24 hours; 100 nmol/L). The basal expression level of pS6 S240/244 and pS6 S235/236 was lower in nontreated H69 cells than in nontreated H69/CR cells, and this was further abrogated by treatment with LY2606368. Actin was used as a loading control.

28401005 28490518
Immunofluorescence
SLFN11 / CDC45 / EdU; 

PubMed: 29395061     


Immunofluorescence analysis for DNA replication (EdU) (purple), chromatin-bound SLFN11 (green), CDC45 (red) and DAPI (blue). CCRF-CEM parental and SLFN11-del cells were treated for 4 hours with CHK1 inhibitor (CHK1i, LY2606368, 10 nM]. EdU was added 30 min before cell collection.

29395061
Growth inhibition assay
Cell viability; 

PubMed: 28401005     


Graphical presentation of % cell viability of AGS and MKN1 cells measured 3 days after treatment with LY2606368.

IC50; 

PubMed: 28490518     


Cell viability in response to treatment with LY2606368 in a panel of human SCLC (hSCLC) cell lines (blue bars), GEMM-derived SCLC cell lines (green bars), a PDX-derived cell line (yellow bar), a large-cell neuroendocrine carcinoma (LCNEC) cell line (black bar), and NSCLC cell lines (red bars). 

28401005 28490518
体内研究 在肿瘤异种移植模型中,LY2606368无论是单独给药还是与其他药物组合给药,都能有效地抑制肿瘤生长,发挥抗肿瘤活性[1]。在SKOV3卵巢癌模型中,LY2606368可抑制原发肿瘤的生长并显著地减少转移率和腹水积累。在SW1990原位胰脏癌模型中,LY2606368可抑制92%的原发肿瘤生长,阻止其向淋巴结结核、脾脏和肠道的转移[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:

[2]

- 合并
  • Cell lines: HeLa细胞
  • Concentrations: 33 或 100 nmol/L
  • Incubation Time: 12 h
  • Method:

    将HeLa细胞铺于T25培养瓶中,使其生长24小时。然后将LY2606368加入其中,使其终浓度为33或100 nM。然后用小分子抑制剂处理细胞12小时,在处理过程中的最后2小时,加入1 μg/mL colchicine。收集细胞并进行固定,检测核中期分裂相和染色体。将15μL 溶于3:1 methanol/acetic acid fixative的细胞悬浮液从离载玻片高3 cm处滴落至其上。然后在43℃金属浴下加热载玻片45秒,静置待其温度降至室温。封片,然后进行观察。


    (Only for Reference)
动物实验:

[2]

- 合并
  • Animal Models: 雌性 CD-1 nu-/nu- 小鼠
  • Dosages: 15 mg/kg
  • Administration: s.c.
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 2 mg/mL (4.56 mM)
Water Insoluble
Ethanol Insoluble

* 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 438.31
化学式

C18H19N7O2.2HCl

CAS号 1234015-54-3
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、MSDS / 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、MSDS / 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
NCT04095221 Recruiting Drug: Prexasertib|Drug: Irinotecan Desmoplastic Small Round Cell Tumor|Rhabdomyosarcoma Memorial Sloan Kettering Cancer Center September 17 2019 Phase 1|Phase 2
NCT03495323 Active not recruiting Drug: LY3300054|Drug: Prexasertib Cancer Dana-Farber Cancer Institute|Eli Lilly and Company May 16 2018 Phase 1
NCT03414047 Active not recruiting Drug: Prexasertib Ovarian Cancer Eli Lilly and Company April 10 2018 Phase 2
NCT03057145 Active not recruiting Drug: Prexasertib|Drug: Olaparib Solid Tumor Khanh Do|Eli Lilly and Company|AstraZeneca|Dana-Farber Cancer Institute March 10 2017 Phase 1

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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:

    Would you please suggest a suitable vehicle to dissolve Prexasertib HCl (LY2606368) for in vivo use?

  • 回答:

    You can dissolve S7178 in a vehicle: 5% DMSO+40%PEG 300+5%Tween80+ddH2O for in vivo use in mice (i.p.). This stock concentration reahces 10mg/ml, and can be prepared for work solution as 0.5mg/ml, stable for no longer than 30min.

  • 问题 2:

    What is the solubility of LY2606368 in 20% Captisol?

  • 回答:

    S7178 in 20% Captisol is a suspension, which is fine for oral gavage. You can dissolve it in this vehicle to the concentration you need as long as the suspension is homogeneous.

Chk Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID