LY3009120 | DP-4978 | Pan RAF Inhibitor | AmBeed-信号通路专用抑制剂

首页 / 抑制剂/激动剂 / MAPK/ERK Pathway / Raf / LY3009120

LY3009120 {[allProObj[0].p_purity_real_show]}

货号：A417155 同义名： DP-4978

LY3009120 is a small molecule that has been shown to be a pan-RAF inhibitor of all isoforms, inhibiting BRAFV600E, BRAFWT and CRAFWT with IC50 values of 5.8, 9.1 and 15 nM and blocking proliferation in both BRAF and RAS mutant cells.

LY3009120 化学结构
CAS号：1454682-72-4

LY3009120 3D分子结构
CAS号：1454682-72-4

规格	价格	会员价	库存	数量
{[ item.pr_size ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_tag_price) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_tag_price) ]}	{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_tag_price) ]}	{[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]}	现货	1周咨询	- +

购物车0 收藏询单

sales@ambeed.cn tech@ambeed.cn 400-920-2911 产品手册产品订购技术咨询
快速发货顺丰冷链运输，1-2 天到达

品质保证

技术支持

免费溶解

LY3009120 纯度/质量文件产品仅供科研

货号：A417155 标准纯度： {[allProObj[0].p_purity_real_show]} 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: 更多 >

Raf 亚型比较

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	98%
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 V600E, IC50: 8.2 nM BRAF, IC50: 19 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, Kd: 36 nM B-Raf (V600E), Kd: 14 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。

LY3009120 生物活性

靶点	C-Raf/Raf-1 C-Raf, IC50:4.3 nM B-Raf BRAF(V600E), IC50:5.8 nM BRAF WT, IC50:15 nM
描述	The RAS/RAF signaling pathway is an important mediator of tumor cell proliferation and angiogenesis. LY3009120 is a pan RAF inhibitor with IC50 values for 15nM, 5.8nM and 9.1nM for C-Raf, B-Raf^V600E and BRAF-WT (measured by a whole cell-based KiNativ assay), respectively, which can be used to avoid the paradoxical activation of RAF induced by B-Raf^V600E selective inhibitor, like Vemurafenib and Dabrafenib. Treatment with LY3009120 at dose >41nM can dramatically decrease the level of p-ERK in the BRAF WT cell line HCT116, whereas Vemurafenib produces significant paradoxical activation with elevated p-ERK level as doses increase^[1]. Potent inhibition of phosphorylation of both MEK1/2 and ERK1/2 was observed with 1 μM LY3009120 treatment in RKO and HCT 116 cell lines with high basal levels of pMEK1/2 and pERK1/2 at time point 0.5h and 2h, but not in HCT-15 and SW620 cell lines with relative low basal levels of pMEK1/2 and pERK1/2^[2]. Oral administration of LY3009120 at dose of 15 or 30mg/kg b.i.d. caused a dose-dependent tumor growth inhibition in rats bearing BRAF V600E ST019VR PDX tumors^[1].
作用机制	LY3009120 binds to inactive form of B-Raf (DFG-D_out).^[1]^[3]

LY3009120 细胞研究

细胞系	浓度	检测类型	检测时间	活性说明	数据源
human A375 cells		Proliferation assay	72 h	Antiproliferative activity against human A375 cells after 72 hrs by resazurin assay, IC50=9.2 nM	25965804
human A375 cells		Function assay	15 mins	Competitive binding affinity to EphA2 in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.02 μM	25965804
human A375 cells		Function assay	15 mins	Competitive binding affinity to BRAF in human A375 cells after 15 mins in presence of ATP analogue, IC50=0.031 μM	25965804
human A375 cells		Function assay	72 h	Inhibition of BRAF V600E mutant in human A375 cells assessed as inhibition of ERK phosphorylation measured after 72 hrs by ELISA assay, IC50=0.037 μM	25965804

LY3009120 动物研究

Dose	Rat: 3 mg/kg - 50 mg/kg^[4] (p.o.)
Administration	p..o.

LY3009120 参考文献

[1]Henry JR, Kaufman MD, et al. Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d] pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. J Med Chem. 2015 May 28;58(10):4165-79.

[2]Vakana E, Pratt S, et al. LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer. Oncotarget. 2017 Feb 7;8(6):9251-9266.

[3]Roskoski R Jr, et al. Targeting oncogenic Raf protein-serine/threonine kinases in human cancers. Pharmacol Res. 2018 Sep;135:239-258.

LY3009120 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.78mL

2.36mL

1.18mL

23.56mL

4.71mL

2.36mL

LY3009120 技术信息

CAS号	1454682-72-4
分子式	C₂₃H₂₉FN₆O
分子量	424.51
SMILES Code	O=C(NC1=CC(C2=CC3=CN=C(NC)N=C3N=C2C)=C(C)C=C1F)NCCC(C)(C)C
MDL No.	MFCD28411374

别名	DP-4978
运输	蓝冰
InChI Key	HHCBMISMPSAZBF-UHFFFAOYSA-N
Pubchem ID	71721540

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C

溶解方案

动物实验：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 0.2 mg/mL clear

PO 0.5% CMC-Na 31 mg/mL suspension

LY3009120 {[allProObj[0].p_purity_real_show]}

LY3009120 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

LY3009120 质控信息

LY3009120 生物活性

LY3009120 细胞研究

LY3009120 动物研究

LY3009120 参考文献

LY3009120 实验方案

LY3009120 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

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

C-Raf/Raf-1	C-Raf, IC50:4.3 nM
B-Raf	BRAF(V600E), IC50:5.8 nM BRAF WT, IC50:15 nM

LY3009120 {[allProObj[0].p_purity_real_show]}

LY3009120 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

LY3009120 质控信息

LY3009120 生物活性

LY3009120 细胞研究

LY3009120 动物研究

LY3009120 参考文献

LY3009120 实验方案

LY3009120 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

请登录您的专属账户

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

LY3009120 纯度/质量文件产品仅供科研