2. MAPK/ERK Pathway Stem Cell/Wnt Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. MEK ERK Apoptosis p38 MAPK CDK PARP
  4. RO5068760

RO5068760 是一种强效、口服有效且选择性的非 ATP 竞争性 MEK1/2 抑制剂，其对 MEK1 的 IC50 值为 0.025 μM。RO5068760 能显著抑制 MAPK 通路活性，从而诱导 G1 期细胞周期阻滞和细胞凋亡 (apoptosis)，进而抑制癌细胞生长。RO5068760 在多种存在 MAPK 通路异常激活的肿瘤中均表现出显著抑制效果，可用于黑色素瘤、结直肠癌、非小细胞肺癌 (NSCLC) 和胰腺癌的相关研究。

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

RO5068760

RO5068760 Chemical Structure

CAS No. : 947182-25-4

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

RO5068760 相关抗体

Top Publications Citing Use of Products

查看 MEK 亚型特异性产品:

查看所有亚型
MEK1 MEK2 MEK5 MEK MAP2K4/MEK4

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

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 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

RO5068760 is a potent, orally active and selective non-ATP-competitive MEK1/2 inhibitor with an IC50 of 0.025 μM for MEK1. RO5068760 significantly inhibits MAPK pathway activity, thereby inducing G1 cell cycle arrest and apoptosis to inhibit cancer cell growth. RO5068760 exhibits significant efficacy in a broad spectrum of tumors with aberrant MAPK pathway activation. RO5068760 can be used for melanoma, colorectal cancer, non-small cell lung cancer (NSCLC), and pancreatic cancer research[1].

IC50 & Target[1]

MEK1

0.025 μM (IC50)

MEK2

 

体外研究
(In Vitro)

RO5068760 能显著抑制 MAPK 通路活性，这体现在多种人类癌细胞系 (例如 LOX、HT-29、H460 和 MIA PaCa-2 细胞) 中 ERK 和 MEK 磷酸化 (p-ERK 和 p-MEK) 的剂量依赖性抑制[1]。
RO5068760 特异性抑制具有激活通路基因突变 (B-Raf 或 KRas) 的癌细胞系的生长，其代表性的 IC50/IC90 值分别为：LOX (B-RafV600E) 细胞为 0.018/0.72 μM，HT-29 (B-RafV600E) 细胞为 0.11/0.56 μM，H460 (KRasG12C) 细胞为 0.30/3.08 μM，MIA PaCa-2 (KRasQ61K) 细胞为 1.25/5.11 μM[1]。
RO5068760 (0-10 μM, 24 小时) 可下调 CDK4/cyclin D1，并上调反应性癌细胞 (HT-29 和 LOX) 中的 p27 和 cleaved PARP，表明其可诱导 G1 细胞周期阻滞，进而导致细胞凋亡[1]。

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

RO5068760 相关抗体:

Western Blot Analysis[1]

Cell Line: HT-29 and LOX cells
Concentration: 0, 2, and 10 μM
Incubation Time: 24 h
Result: Decreased CDK4 and cyclin D1 levels in a dose dependent manner.
Increased p27 and cleaved PARP levels in HT-29 and LOX cells.
体内研究
(In Vivo)

RO5068760 (6.25-500 mg/kg，口服，每日两次或每日一次，或每周一次，持续约 3 至 4 周) 在具有异常 MAPK 通路激活的小鼠的相应人类肿瘤异种移植模型中表现出剂量依赖性的抗肿瘤活性[1]。

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

Animal Model: Female nude mice subcutaneously implanted with human cancer cells (LOX and HT-29 (both B-Raf V600E mutant), MIA PaCa-2 (KRAS G12C mutation) and H460 (KRAS Q61H mutation))[1]
Dosage: 6.25, 12.5, 25, 50, 100, 200 and 500 mg/kg
Administration: p.o., b.i.d. or q.d. or weekly for approximately 3 to 4 weeks
Result: Showed significant tumor growth inhibition (TGI > 65%) in all models when administered once or twice daily.
Exhibited partial (PR) or complete regression (CR) at doses as low as 12.5 mg/kg (b.i.d.) in the LOX melanoma model harboring B-RafV600E mutation.
Resulted in PR or CR in four of four tumor models tested at a dose of 100 mg/kg twice daily.
Exhibited antitumor activity in the LOX melanoma model even at 500 mg/kg once weekly with three PRs and five CRs compared with vehicle controls.
In K-Ras mutant tumors, twice-daily dosing yielded better efficacy than once-daily or weekly regimens at equivalent total doses.
Showed superior in vivo efficacy in B-RafV600E xenografts (LOX and HT-29) compared with K-Ras mutant xenografts (H460 and MIA PaCa-2).
In the MIA PaCa-2 and H460 xenograft models, Cmax levels in plasma reached or exceeded the EC90 of p-ERK suppression, whereas in the LOX and HT-29 models, maximal plasma levels required for a similar degree of efficacy were significantly lower.
分子量

647.43

Formula

C28H27FIN3O6
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

RO5068760 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:

RO5068760947182-25-4RO 5068760RO-5068760MEKERKApoptosisp38 MAPKCDKPARPMitogen-activated protein kinase kinaseMAPKKMAP2KExtracellular signal regulated kinasesCyclin dependent kinasepoly ADP ribose polymerasenon-ATP-competitiveMEK1/2MAPKmelanomacolorectal cancerNSCLCpancreatic cancerLOXHT-29H460MIA PaCa-2Inhibitorinhibitorinhibit

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：
RO5068760
目录号：
HY-111033
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