abemaciclib mesylate (LY2835219)

For research use only. Not for use in humans.

目录号:S7158

abemaciclib mesylate (LY2835219) Chemical Structure

Molecular Weight(MW): 602.7

abemaciclib (LY2835219)是一种有效的,选择性CDK4CDK6抑制剂,无细胞试验中IC50分别为2 nM和10 nM。Phase 3。

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客户使用Selleck生产的abemaciclib mesylate (LY2835219)发表文献23篇:

产品安全说明书

CDK抑制剂选择性比较

生物活性

产品描述 abemaciclib (LY2835219)是一种有效的,选择性CDK4CDK6抑制剂,无细胞试验中IC50分别为2 nM和10 nM。Phase 3。
靶点
CDK4 [1]
(Cell-free assay)
CDK6 [1]
(Cell-free assay)
2 nM 10 nM
体外研究

LY2835219是一种口服有效的细胞周期蛋白依赖性激酶(CDK)抑制剂,靶向作用于CDK4(cyclin D1)和CDK6(cyclin D3)细胞周期通路,具有潜在的抗肿瘤活性。LY2835219特异性抑制CDK4和6,从而在早G1期抑制视网膜母细胞瘤(Rb)蛋白磷酸化。抑制Rb磷酸化,防止CDK-介导的G1-S期转换,从而使细胞周期停滞在G1期,抑制DNA合成,且抑制癌细胞生长。某些类型的癌症中丝/苏氨酸激酶CDK4/6的过表达,导致细胞周期调节失控。[1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
insect cells  Ml7DSpVv[3Srb36gZZN{[Xl? Ml3FOVAhdWmwcx?= M1O0VmNwdXCndHn0bZZmKGmwaHnibZRqd25ib3[gbJVu[W5iQ1TLOE9kgWOuaX6gSFEh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{Bie3Onc4Pl[EBieyCyaH;zdIhwenmuYYTpc44hd2ZiQ2TSSkBi\nSncjC1NEBucW6|IHL5JG1q[2ijZXzpd{1O\W62ZX6gdIxwfCCjbnHsfZNqeyCrbjDwdoV{\W6lZTDv[kBCXFBuIFvpQVAvPiCwTR?= M3LXRlI3OTF3NUex
insect cells  M{P5bmZ2dmO2aX;uJIF{e2G7 MYW1NEBucW6| NH:0[ldKdmirYnn0bY9vKG:oIHj1cYFvKEOGS{SvZ5lkdGmwIFSxJIV5eHKnc4Pl[EBqdiCrboPlZ5Qh[2WubIOgZZN{\XO|ZXSgZZMheGixc4Doc5J6dGG2aX;uJI9nKEOWUl[gZYZ1\XJiNUCgcYlveyCkeTDtbYNzd3CuYYTlJJNkcW62aXzsZZRqd25iY3;1cpRmeixiSVO1NF0zKG6P MWWyOlEyPTV5MR?=
human COLO205 cells NVHjd3RUTnWwY4Tpc44h[XO|YYm= NV\q[GtwOjRiaB?= M2G1T2lvcGmkaYTpc44hd2ZiQ1TLOE83KGmwIHj1cYFvKEORTF:yNFUh[2WubIOgZZN{\XO|ZXSgZZMhcW6qaXLpeIlwdiCxZjDSZkBxcG:|cHjvdplt[XSrb36gZYZ1\XJiMkSgbJJ{KGK7IIDyc5Bq\Gm3bTDpc4Rq\GVic4ThbY5qdmdvYnHz[YQhdGG|ZYKtd4Nidm6rbneg[ox2d3Knc3PlcoNmKG2rY4LvdIxifGViY4n0c41mfHKrYzDhcoFtgXOrcx?= M1vJVlI3OTF3NUex
human COLO205 cells NUnYNHdGTnWwY4Tpc44h[XO|YYm= M3nC[VI1KGh? NUDveJk3UW6qaXLpeIlwdiCxZjDDSGs1NzZiaX6gbJVu[W5iQ1;MU|IxPSClZXzsd{Bie3Onc4Pl[EBieyCvYYjpcZVuKGOnbHygZ5lkdGViYYLy[ZN1KGG2IFexJJBp[XOnIHHmeIVzKDJ2IHjyd{BjgSCycn;wbYRqfW1iaX;kbYRmKHO2YXnubY5oNWKjc3XkJIZtd3diY4n0c41mfHKrYzDhcoFtgXOrcx?= MXKyOlEyPTV5MR?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Rb(S780) / Rb / p21; 

PubMed: 26909611     


Effects of LY2835219 on RB phosphorylation and p21 expression were evaluated by immunoblotting at indicated concentrations (A)

p-ERK / ERK / p-Akt / Akt / p-mTOR(S2448) / mTOR; 

PubMed: 26909611     


Effects of LY2835219 on RB phosphorylation and p21 expression were evaluated by immunoblotting at indicated time points (B).

pRb(S795) / E2F1 / Cyclin A2 / Cyclin E2; 

PubMed: 27748766     


(c) MCF-7 and MR cells were treated with 100 nm LY2835219 and collected at indicated times. Immunoblots were performed with the indicated antibodies. (d) MCF-7 and MR cells were treated with increasing concentrations of LY2835219 and harvested after 24 h; lysates were then subjected to immunoblotting.

26909611 27748766
Growth inhibition assay
Cell viability; 

PubMed: 26909611     


Cell viability of OSC-19, FaDu, and YD-10B cells treated with LY2835219 at indicated concentrations. Data are representative of three independent experiments: mean ± SEM.

26909611
体内研究 LY2835219-MsOH处理脑的剂量百分比为0.5–3.9%。LY2835219-MsOH处理皮下和颅内胶质瘤模型(U87MG),抑制肿瘤生长,这种作用存在剂量依赖性,不管是单独处理,还是与Temozolomide联用。[1]

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)

溶解度 (25°C)

体外 Water 100 mg/mL (165.92 mM)
DMSO 83 mg/mL (137.71 mM)
Ethanol 24 mg/mL (39.82 mM)
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):
water
100mg/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 602.7
化学式

C27H32F2N8.CH4O3S

CAS号 1231930-82-7
储存条件 粉状
溶于溶剂
别名 N/A

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
NCT02327143 Completed Drug: LY2835219|Drug: ¹³C₈-LY2835219 Healthy Volunteers Eli Lilly and Company January 2015 Phase 1
NCT02256267 Completed Drug: LY2835219|Drug: Rifampin Healthy Volunteers Eli Lilly and Company October 2014 Phase 1
NCT02059148 Completed Drug: LY2835219 Healthy Volunteers Eli Lilly and Company February 2014 Phase 1
NCT02014129 Completed Drug: LY2835219 Neoplasm Metastasis|Lymphoma Eli Lilly and Company December 18 2013 Phase 1
NCT01913314 Completed Drug: [^14C]-LY2835219 Healthy Volunteers Eli Lilly and Company August 2013 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:

    Is your product S7158 LY2835219 “mesylate salt form”?

  • 回答:

    Our S7158 LY2835219 is mesylate salt form.

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

相关CDK产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID