RAF265 | CHIR-265 | RAF/VEGFR2 Inhibitor | AmBeed-信号通路专用抑制剂

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RAF265 99%+

货号：A342718 同义名： CHIR-265 产品仅供科研

RAF265 is a pan-inhibitor that inhibits C-Raf, B-Raf and B-Raf V600E with IC50 of 3 nM-60 nM. It also shows inhibition on phosphorylation of VEGFR2 with EC50 of 30 nM.

RAF265 化学结构
CAS号：927880-90-8

RAF265 3D分子结构
CAS号：927880-90-8

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RAF265 纯度/质量文件

货号：A342718 标准纯度：99%+ 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: • Mar. Drugs, 2024, 22(5): 194. Ambeed. [ A104599 ]; • Pharmaceuticals, 2024, 17(5): 570. Ambeed. [ A224421 ]; 更多 >

VEGFR 亚型比较
Raf 亚型比较

产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2, IC50: 3 nM VEGFR2/Flk1, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	99%+
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ VEGFR2, IC50: 25 nM Flk1, IC50: 25 nM			99%+
Regorafenib	+++ VEGFR1, IC50: 13 nM	+++ VEGFR2, IC50: 4.2 nM	+ VEGFR3, IC50: 46 nM	RET	98%
Pazopanib	+++ VEGFR1, IC50: 10 nM	++ VEGFR2, IC50: 30 nM	+ VEGFR3, IC50: 47 nM	PDGFR,FGFR,c-Kit	99%
Sitravatinib	+++ VEGFR1 (FLT1), IC50: 6 nM	+++ VEGFR2 (KDR), IC50: 5 nM	++++ VEGFR3 (FLT4), IC50: 2 nM		99%+
Foretinib	+++ VEGFR1/FLT1, IC50: 6.8 nM	++++ KDR, IC50: 0.86 nM	++++ VEGFR3/FLT4, IC50: 2.8 nM	Tie-2	99%+
MGCD-265 analog	++++ VEGFR1, IC50: 3 nM	++++ VEGFR2, IC50: 3 nM	++++ VEGFR3, IC50: 4 nM	Tie-2	99%+
Lactate	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	85%
AEE788	+ FLT1, IC50: 59 nM	+ KDR, IC50: 77 nM		EGFR	98+%
Linifanib	++++ VEGFR1/FLT1, IC50: 3 nM	++++ VEGFR2/KDR, IC50: 4 nM	+ VEGFR3/FLT4, IC50: 190 nM	FLT3	99%+
Vatalanib 2HCl	+ VEGFR1/FLT1, IC50: 77 nM	++ VEGFR2/KDR, IC50: 37 nM VEGFR2/Flk1, IC50: 270 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Fms,c-Kit	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/KDR, IC50: 0.2 nM VEGFR2/Flk1, IC50: 0.18 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	FLT3,c-Kit	99%+
ZM 306416	+ VEGFR1, IC50: 0.33 μM			Src	99%+
KRN-633	+ VEGFR1, IC50: 170 nM	+ VEGFR2, IC50: 160 nM	+ VEGFR3, IC50: 125 nM	BTK,c-Kit	99%+
OSI-930	+++ FLT1, IC50: 8 nM	+++ KDR, IC50: 9 nM			99%+
Lenvatinib	++ VEGFR1/FLT1, IC50: 22 nM	++++ VEGFR2/KDR, IC50: 4.0 nM	+++ VEGFR3/FLT4, IC50: 5.2 nM		98%
NVP-BAW2881	+ hVEGFR1, IC50: 820 nM	+++ mVEGF2, IC50: 165 nM hVEGFR2, IC50: 9 nM	+ hVEGFR3, IC50: 420 nM		98%
Cediranib	+++ VEGFR1/FLT1, IC50: 5 nM	++++ VEGFR2/KDR, IC50: 0.5 nM		c-Kit	99%+
Nintedanib	++ VEGFR1, IC50: 34 nM	+++ VEGFR2, IC50: 13 nM	+++ VEGFR3, IC50: 13 nM	FLT3	99+%
BMS-794833		++ VEGFR2, IC50: 15 nM			99%+
SKLB1002		++ VEGFR2, IC50: 32 nM			98%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	98+%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Rivoceranib Mesylate		++++ VEGFR2, IC50: 1 nM		RET	98+%
Ponatinib		++++ VEGFR2, IC50: 1.5 nM			98%
LY2874455		+++ VEGFR2, IC50: 7 nM			99%+
ZM323881 HCl		++++ VEGFR2, IC50: <2 nM			98%
AZD2932		+++ VEGFR-2, IC50: 8 nM		c-Kit	98%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2, IC50: 90 nM VEGFR2/Flk1, IC50: 90 nM			99%
CYC-116		++ VEGFR2, Ki: 44 nM		FLT3	99%+
Golvatinib		++ VEGFR2, IC50: 16 nM			99%+
Sunitinib		+ VEGFR2 , IC50: 80 nM		FLT3	98%
RAF265		++ VEGFR2, EC50: 30 nM			99%+
PD173074					99%+
BFH772		++++ VEGFR2, IC50: 3 nM			99%+
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	98%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	FLT3,RET	98%
Telatinib		+++ VEGFR2, IC50: 6 nM	++++ VEGFR3, IC50: 4 nM	c-Kit	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 (V600E), IC50: 0.7 nM B-Raf, IC50: 5.2 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 (V600E), IC50: 31 nM B-Raf, IC50: 100 nM	+ C-Raf, IC50: 48 nM			98%
PLX4720		++ B-Raf (V600E), IC50: 13 nM B-Raf, IC50: 160 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, 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 (V600E), IC50: 34 nM B-Raf, IC50: 105 nM	++ C-Raf-1, IC50: 29 nM			99%
PLX7904				✔		99%+
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。

RAF265 生物活性

靶点

VEGFR2

VEGFR2, EC50:30 nM
VEGFR2

VEGFR2, EC50:30 nM
B-Raf

B-Raf, IC50:3 nM-60 nM

描述

B-Raf protein is a key mediator in the MAPK signaling pathway that involved in the pathogenesis of multiple cancers. An important V600E mutation has been shown to cause constitutive B-Raf activation. RAF265 is an oral molecule inhibitor of both mutant BRAF^V600E and VEGFR2 with EC₅₀ values of 0.14 μM and 0.19 μM, respectively^[5]. The IC₅₀ values of RAF265 against of BRAF^V600E, wild-type BRAF, VEGFR, and C-RAF were 0.5, 70, 20 and 19μM, respectively^[6]. In HT29 and MDAMB231 cells, RAF265 inhibited cell viability with IC₂₀ values of 1-3μM and IC₅₀ values of 5-10μM. In A549 and HCT116 cells, the IC20₂₀ values of RAF265 were 1μM for both cell lines, but the IC₅₀ values were more than 10μM. Additionally, treatment with RAF265 at the concentrations of 1-10μM decreased MEK phosphorylation in BRAF-mutated cell lines. In HCT116, HT29, and MDAMB231 cell lines, increasing doses of RAF265 also decreased the phosphorylation of S6 ribosomal protein. In mice inoculated with HCT116 cancer cells, the time to achieve a relative 10 times of the initial tumor volume was 25 days in the RAF265 group (12 mg/kg, once per day), compared to 20 days in the control group. The combination of RAF265 and RAD001 at a dose of 12 mg/kg/d delayed the tumor growth for 5 days ^[7].

RAF265 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
A375 cells		Proliferation assay		Antiproliferative activity against human A375 cells harboring B-RAF V600E mutant, IC50=0.04 μM	26396681
human Malme-3M cells		Function assay		Inhibition of B-RAF V600E mutant in human Malme-3M cells assessed as phosphorylation of ERK, IC50=0.04 μM	26396681
SK-MEL-28 cells		Function assay		Inhibition of B-RAF V600E mutant in human SK-MEL-28 cells assessed as phosphorylation of ERK, IC50=0.14 μM	26396681
WM1799 cells		Proliferation assay		Antiproliferative activity against human WM1799 cells harboring B-RAF V600E mutant, IC50=0.04 μM	26396681

RAF265 动物研究

Dose

Mice: 10 mg/kg - 100 mg/kg^[3] (p.o., q2d); 0.2 mg/kg, 10 mg/kg - 20 mg/kg^[4] (i.p.)

Administration

p.o., i.p.

Pharmacokinetics

Animal	Mice^[3]	Rats^[3]	Dogs^[3]	Monkeys^[3]
Dose	5 mg/kg (i.v.) 30 mg/kg (p.o.)	5 mg/kg (i.v.) 20 mg/kg (p.o.)	1.25 mg/kg (i.v.) 5 mg/kg (p.o.)	1 mg/kg (i.v.) 5 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.	i.v. p.o.	i.v. p.o.
F	0.51	>95%	0.35	0.28
T_1/2	41 h	46 h	27 h	27 h
AUC_∞	4300 μM·h (p.o.)	450 μM·h (p.o.)	35 μM·h (p.o.)	48 μM·h (p.o.)
CL	0.1 ml/min/kg	0.9 ml/min/kg	0.8 ml/min/kg	1.5 ml/min/kg
Vss	0.5 L/kg	3.3 L/kg	1.9 L/kg	2.9 L/kg

RAF265 参考文献

[1]Mordant P, Loriot Y, et al. Dependence on phosphoinositide 3-kinase and RAS-RAF pathways drive the activity of RAF265, a novel RAF/VEGFR2 inhibitor, and RAD001 (Everolimus) in combination. Mol Cancer Ther. 2010 Feb;9(2):358-68.

[2]Zitzmann K, de Toni E, et al. The novel Raf inhibitor Raf265 decreases Bcl-2 levels and confers TRAIL-sensitivity to neuroendocrine tumour cells. Endocr Relat Cancer. 2011 Mar 21;18(2):277-85.

[3]Williams TE, Subramanian S, et al. Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma. ACS Med Chem Lett. 2015 Aug 3;6(9):961-5.

[4]Chow AK, Cheng NS, et al. Preclinical analysis of the anti-tumor and anti-metastatic effects of Raf265 on colon cancer cells and CD26(+) cancer stem cells in colorectal carcinoma. Mol Cancer. 2015 Apr 11;14:80.

[5]Huang T, Karsy M, Zhuge J, Zhong M, Liu D. B-Raf and the inhibitors: from bench to bedside. J Hematol Oncol. 2013 Apr 25;6:30. doi: 10.1186/1756-8722-6-30. PMID: 23617957; PMCID: PMC3646677.

[6]Williams TE, Subramanian S, Verhagen J, McBride CM, Costales A, Sung L, Antonios-McCrea W, McKenna M, Louie AK, Ramurthy S, Levine B, Shafer CM, Machajewski T, Renhowe PA, Appleton BA, Amiri P, Chou J, Stuart D, Aardalen K, Poon D. Discovery of RAF265: A Potent mut-B-RAF Inhibitor for the Treatment of Metastatic Melanoma. ACS Med Chem Lett. 2015 Aug 3;6(9):961-5. doi: 10.1021/ml500526p. PMID: 26396681; PMCID: PMC4569875.

[7]Mordant P, Loriot Y, Leteur C, Calderaro J, Bourhis J, Wislez M, Soria JC, Deutsch E. Dependence on phosphoinositide 3-kinase and RAS-RAF pathways drive the activity of RAF265, a novel RAF/VEGFR2 inhibitor, and RAD001 (Everolimus) in combination. Mol Cancer Ther. 2010 Feb;9(2):358-68. doi: 10.1158/1535-7163.MCT-09-1014. Epub 2010 Feb 2. PMID: 20124452.

RAF265 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.93mL

0.39mL

0.19mL

9.64mL

1.93mL

0.96mL

19.29mL

3.86mL

1.93mL

RAF265 技术信息

CAS号	927880-90-8
分子式	C₂₄H₁₆F₆N₆O
分子量	518.414

别名	CHIR-265
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 25 mg/mL(48.22 mM)，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

无水乙醇: 8 mg/mL(15.43 mM)，配合低频超声助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 3 mg/mL clear

PO 0.5% CMC-Na 40 mg/mL suspension

RAF265 99%+

RAF265 纯度/质量文件

全球学术期刊中引用的产品

RAF265 生物活性

RAF265 细胞研究

RAF265 动物研究

RAF265 参考文献

RAF265 实验方案

RAF265 技术信息

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VEGFR2	VEGFR2, EC50:30 nM
VEGFR2	VEGFR2, EC50:30 nM
B-Raf	B-Raf, IC50:3 nM-60 nM

RAF265 99%+

RAF265 纯度/质量文件

全球学术期刊中引用的产品

RAF265 生物活性

RAF265 细胞研究

RAF265 动物研究

RAF265 参考文献

RAF265 实验方案

RAF265 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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