2. Cell Cycle/DNA Damage Epigenetics
  3. CDK Aurora Kinase
  4. LCI133

LCI133 是一款首创、具有纳摩尔级效力、选择性的多靶点激酶抑制剂，靶向 CDK4/6/9 和 AURKA/B (IC50值分别为 4.7/10.2/4.1 nM 和 2.8/10.6 nM)。LCI133 可在 MYCN 扩增的神经母细胞瘤 BE(2)-C 细胞中诱导 S/G2 期阻滞并触发显著细胞凋亡 (apoptosis)。在 BE(2)-C 神经母细胞瘤异种移植模型中，LCI133 显示出显著的抗肿瘤疗效。

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

LCI133

LCI133 Chemical Structure

CAS No. : 3065284-87-6

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 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

LCI133 相关抗体

Top Publications Citing Use of Products

查看 CDK 亚型特异性产品:

查看所有亚型
CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

查看 Aurora Kinase 亚型特异性产品:

查看所有亚型
Aurora Kinase Aurora A Aurora B Aurora C

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LCI133 is afirst-in-class,nanomolar-potent, selective multikinase inhibitor targeting CDK4/6/9 and AURKA/B (IC50 = 4.7/10.2/4.1 nM and 2.8/10.6 nM). LCI133 induces S/G2 cell-cycle arrest and robust apoptosis in MYCN-amplified neuroblastoma BE(2)-C cells. LCI133 demonstrates significant antitumor efficacy in a BE(2)-C neuroblastoma xenograft model[1].

IC50 & Target[1]

CDK4

4.7 nM (IC50)

CDK6

10.2 nM (IC50)

CDK9

4.1 nM (IC50)

Aurora A

2.8 nM (IC50)

Aurora B

10.6 nM (IC50)

体外研究
(In Vitro)

LCI133 (72 h) 在 BE(2)-C、NGP、Kelly、SK-N-AS 与 SHEP 神经母细胞瘤细胞中降低细胞活性 (IC50 = 0.17-0.55 μM)[1]。
LCI133 (0.5-1 μM；24 h) 在 BE(2)-C 细胞中诱导细胞周期阻滞 (S 期增加，并出现明显的 G2 期阻滞)[1]。
LCI133 (0.5-1 μM；24 h) 在 BE(2)-C 细胞中增加细胞凋亡 (Annexin V/7-AAD)[1]。
LCI133 (0.5-1 μM；24 h) 在 BE(2)-C 与 NGP 细胞中抑制 RNAP II Ser2 磷酸化并降低 MCL-1 蛋白水平[1]。
LCI133 (0.5-1 μM；24 h) 在 BE(2)-C 细胞中增加 cleaved PARP[1]。
LCI133 (0.5 μM；3 h) 在 BE(2)-C 细胞中降低 MYCN 与 MCL1 的 mRNA 表达水平[1]。

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

LCI133 相关抗体:

Cell Cycle Analysis[1]

Cell Line: BE(2)-C
Concentration: 0.5 μM; 1 μM
Incubation Time: 24 h
Result: Increased the proportion of cells in S phase at 1 μM.
Induced a pronounced G2-phase blockade at 0.5 μM and 1 μM.

Apoptosis Analysis[1]

Cell Line: BE(2)-C
Concentration: 0.5 μM ; 1 μM
Incubation Time: 24 h
Result: Increased apoptosis, as indicated by an increased proportion of Annexin V/7-AAD–positive cells.

Western Blot Analysis[1]

Cell Line: BE(2)-C ; NGP
Concentration: 0.5 μM; 1 μM
Incubation Time: 24 h
Result: Inhibited RNAP II Ser2 phosphorylation and decreased MCL-1 protein levels in BE(2)-C and NGP cells.
Increased cleaved PARP in BE(2)-C cells.

RT-PCR[1]

Cell Line: BE(2)-C
Concentration: 0.5 μM
Incubation Time: 3 h
Result: Decreased MYCN (p = 0.006) and MCL1 (p < 0.0003) mRNA expression versus DMSO control.
体内研究
(In Vivo)

LCI133-HCl (40 mg/kg/day ; 腹腔注射 i.p. ;每日一次 QD ; 给药 28 天) 可显著抑制雌性 NSG 小鼠皮下 BE(2)-C 异种移植瘤生长并提高总体生存率，且未见明显毒性[1]。

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

Animal Model: Adult female NSG mice bearing subcutaneous BE(2)-C xenografts (1 × 10^6 cells injected s.c. into the right flank; 2-3 weeks engraftment)[1].
Dosage: 40 mg/kg/d
Administration: Intraperitoneal injection (i.p.), once daily (QD), for 28 days.
Result: Significantly reduced BE(2)-C xenograft tumor growth and improved overall survival without obvious changes in mouse behavior or body weight.
分子量

578.66

Formula

C33H34N6O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

LCI133 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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)
× = ×
C1   V1   C2   V2
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:

LCI1333065284-87-6LCI 133LCI-133CDKAurora KinaseCyclin dependent kinaseCDK4CDK6CDK9Aurora AAurora Bmultikinase inhibitorneuroblastomaMYCNMCL-1BE(2)-C xenograftInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   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：

Bulk Inquiry

Inquiry Information

产品名称：
LCI133
目录号：
HY-179375
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   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：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z