Avutometinib | CH5126766 | MEK/RAF Inhibitor | AmBeed-信号通路专用抑制剂

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Avutometinib 98%

货号：A245684 同义名： CH5126766;Ro 5126766

Avutometinib（Ro 5126766）是一种双重MEK/RAF抑制剂，具有抗肿瘤活性。它对BRAFV600E、CRAF、MEK和BRAF的IC50值分别为8.2 nM、56 nM、160 nM和190 nM。

Avutometinib 化学结构
CAS号：946128-88-7

Avutometinib 3D分子结构
CAS号：946128-88-7

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Avutometinib 纯度/质量文件产品仅供科研

货号：A245684 标准纯度： 98% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

MEK 亚型比较
Raf 亚型比较

产品名称	MEK ↓ ↑	MEK1 ↓ ↑	MEK1/2 ↓ ↑	MEK2 ↓ ↑	MEK5 ↓ ↑	其他靶点	纯度
Honokiol	✔						98%
Mirdametinib	++++ MEK, IC50: 0.33 nM						99%+
Binimetinib	+++ MEK, IC50: 12 nM						99%+
BI-847325		++ MEK1, IC50: 25 nM		+++ MEK2, IC50: 4 nM			99%+
U0126-EtOH		+ MEK1, IC50: 0.07 μM		++ MEK2, IC50: 0.06 μM			98%
GDC-0623		++++ MEK1, IC50: 0.13 nM					99%+
TAK-733		++++ MEK1, IC50: 3.2 nM					99%+
Trametinib		++++ MEK1, IC50: 0.92 nM		++++ MEK2, IC50: 1.8 nM			99%+
Selumetinib		+++ MEK1, IC50: 14 nM MEK1, Kd: 99 nM		+ MEK2, Kd: 530 nM			99%+
CI-1040		++ MEK1, IC50: 17 nM		++ MEK2, IC50: 17 nM			99%+
Myricetin		✔					98%
Refametinib		++ MEK1, IC50: 19 nM		++ MEK2, IC50: 47 nM			99%+
Cobimetinib		+++ MEK1, IC50: 4.2 nM					99%+
PD98059		+ MEK1, IC50: 2 μM					99%+
SL327		+ MEK1, IC50: 0.18 μM		+ MEK2, IC50: 0.22 μM		AP-1	98+%
PD318088			✔				98%
AZD8330			+++ MEK1/2, IC50: 7 nM				99%+
Pimasertib							98%
(E/Z)-BIX02189					++++ MEK5, IC50: 1.5 nM		99%+
(E/Z)-BIX02188					+++ MEK5, IC50: 4.3 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	A-raf ↓ ↑	B-Raf ↓ ↑	C-Raf/Raf-1 ↓ ↑	Raf ↓ ↑	其他靶点	纯度
Encorafenib		✔				99%+
GDC-0879		++++ B-Raf, IC50: 0.13 nM				99%+
SB-590885		++++ B-Raf, Ki: 0.16 nM				99%+
RAF265						99%+
Dabrafenib		++++ B-Raf, IC50: 5.2 nM B-Raf (V600E), IC50: 0.7 nM	+++ C-Raf, IC50: 6.3 nM			98%
Lifirafenib	++++ WT A-RAF, IC50: 1 nM	++ BRAF(V600E), IC50: 23 nM BRAF WT, IC50: 32 nM	+++ C-RAF (Y340/341D), IC50: 7 nM		EGFR	96%
ZM 336372			+ C-Raf, IC50: 70 nM			99%+
NVP-BHG 712			+ C-Raf, IC50: 0.395 μM			99%+
CCT196969		+ BRAF, IC50: 0.1 μM	++ CRAF, IC50: 0.01 μM		Src	98%
Vemurafenib		++ B-Raf, IC50: 100 nM B-Raf (V600E), IC50: 31 nM	+ C-Raf, IC50: 48 nM			98+%
PLX4720		++ B-Raf, IC50: 160 nM B-Raf (V600E), IC50: 13 nM	+++ C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM		BRK	99+%
GW 5074			+++ C-Raf, IC50: 9 nM			99%+
Avutometinib		+++ BRAF, IC50: 19 nM BRAF V600E, IC50: 8.2 nM	+ CRAF, IC50: 56 nM			98%
LY3009120		++++ BRAF(V600E), IC50: 5.8 nM BRAF WT, IC50: 15 nM	++++ C-Raf, IC50: 4.3 nM			99%+
Agerafenib		++ B-Raf (V600E), Kd: 14 nM B-Raf, Kd: 36 nM	+ C-Raf, Kd: 39 nM		RET	99%+
TAK-632		+++ B-Raf, IC50: 8.3 nM	++++ C-Raf, IC50: 1.4 nM			99%+
AZ 628		+ B-Raf, IC50: 105 nM B-Raf (V600E), IC50: 34 nM	++ C-Raf-1, IC50: 29 nM			99%
PLX7904				✔		98+%
Sorafenib		++ B-Raf, IC50: 22 nM B-Raf (V599E), IC50: 38 nM	++++ Raf-1, IC50: 6 nM	++++ Raf-1, IC50: 6 nM		99%
Tovorafenib				✔		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Avutometinib 生物活性

靶点	B-Raf BRAF, IC50:19 nM BRAF V600E, IC50:8.2 nM C-Raf/Raf-1 CRAF, IC50:56 nM
描述	The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. Among them, B-RAF is the most frequently mutated protein kinase in human cancers. Ro 5126766 is a unique and allosteric MEK/RAF signaling inhibitor with IC50 values of 8.2, 19, 56 and 160nM for BRAF^V600E mutant, BRAF, CRAF and MEK1 (measured by cell-free kinase assays), respectively. Treatment with Ro 5126766 at dose ranging in 0.01-10μM for 2h can reduce levels of both p-MEK and p-ERK dose-dependently till to undetectable levels in HCT116 KRAS-mutant colorectal cancer cells, whereas other MEK inhibitors PD0325901/GSK1120212 only inhibited ERK phosphorylation and either GDC-0879 or PLX-4720, the RAF inhibitor, induced p-MEK and p-ERK in response to paradoxical activation of RAF kinase as previous report. Consistent with the in vitro study, Ro 5126766 showed more effective inhibition on ERK signaling output than PD0325901 in chronically treated tumors with RAS mutations in the Calu-6 (NSCLC, KRAS Q61K) xenograft models. Oral administration of Ro 5126766 at dose of 1.5mg/kg, every day for 11 days showed more anti-tumor effect than PD0325901. Also Ro 5126766 at dose of 2mg/kg can cease the tumor growth on the PD0325901-refractory tumors in the HCT116 xenograft tumor model. Both of these more prolonged growth inhibition with Ro 5126766 was accompanied with suppression on both ERK signaling, p-MEK and p-ERK^[1].
作用机制	The binding of Ro 5126766 caused MEK to adopt a conformation in which it cannot be phosphorylated by and released from RAF, thus resulting in formation of a stable MEK/RAF complex and inhibition of RAF kinase.^[1]

Avutometinib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HCT116 cell		Function assay	96 h	Inhibition of human HCT116 cell growth after 96 hrs by counting kit-8 analysis, IC50=0.04 μM	24900832
human A549 cells	10 μM	Function assay	1 h	Inhibition of MEK1 in human A549 cells assessed as reduction in pErk1/2 level at 10 uM after 1 hr by Western blotting analysis	25766633
human C32 cells		Growth inhibition assay		Growth inhibition of human C32 cells harboring R-Raf V600E mutant, IC50=0.047 μM	24900832
human PANC1 cells	10 μM	Function assay	1 h	Inhibition of MEK1 in human PANC1 cells assessed as reduction in pErk1/2 level at 10 uM after 1 hr by Western blotting analysis	25766633

Avutometinib 动物研究

Dose	Mice: 0.1 mg/kg - 1 mg/kg^[2] (p.o.)
Administration	p.o.

Avutometinib 参考文献

[1]Souers AJ, Leverson JD, et al. ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets. Nat Med. 2013 Feb;19(2):202-8.

Avutometinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.12mL

0.42mL

0.21mL

10.61mL

2.12mL

1.06mL

21.21mL

4.24mL

2.12mL

Avutometinib 技术信息

CAS号	946128-88-7
分子式	C₂₁H₁₈FN₅O₅S
分子量	471.462

别名	CH5126766;Ro 5126766
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 120 mg/mL(254.53 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

Avutometinib 98%

Avutometinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Avutometinib 质控信息

Avutometinib 生物活性

Avutometinib 细胞研究

Avutometinib 动物研究

Avutometinib 参考文献

Avutometinib 实验方案

Avutometinib 技术信息

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B-Raf	BRAF, IC50:19 nM BRAF V600E, IC50:8.2 nM
C-Raf/Raf-1	CRAF, IC50:56 nM

Avutometinib 98%

Avutometinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Avutometinib 质控信息

Avutometinib 生物活性

Avutometinib 细胞研究

Avutometinib 动物研究

Avutometinib 参考文献

Avutometinib 实验方案

Avutometinib 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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Avutometinib 纯度/质量文件产品仅供科研