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

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产品名称	VEGFR1 ↓ ↑	VEGFR2 ↓ ↑	VEGFR3 ↓ ↑	其他靶点	纯度
Motesanib Diphosphate	++++ VEGFR1, IC50: 2 nM	++++ VEGFR2/Flk1, IC50: 3 nM VEGFR2, IC50: 3 nM	+++ VEGFR3, IC50: 6 nM	PDGFR,RET	97%
Tivozanib	++ VEGFR1, IC50: 30 nM	+++ VEGFR2, IC50: 6.5 nM	++ VEGFR3, IC50: 15 nM		99%+
Brivanib	+ VEGFR1, IC50: 380 nM	++ Flk1, IC50: 25 nM VEGFR2, 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	FGFR,PDGFR,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	c-Kit,FLT3	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/Flk1, IC50: 270 nM VEGFR2/KDR, IC50: 37 nM	+ VEGFR3/FLT4, IC50: 660 nM	c-Kit,c-Fms/CSF1R	99%+
Axitinib	++++ VEGFR1/FLT1, IC50: 0.1 nM	++++ VEGFR2/Flk1, IC50: 0.18 nM VEGFR2/KDR, IC50: 0.2 nM			98%
Dovitinib	+++ VEGFR1/FLT1, IC50: 10 nM	+++ VEGFR2/Flk1, IC50: 13 nM	+++ VEGFR3/FLT4, IC50: 8 nM	c-Kit,FLT3	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	98%
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		99%
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			99%
Cabozantinib S-malate		++++ VEGFR2/KDR, IC50: 0.035 nM			99+%
Ki8751		++++ VEGFR2, IC50: 0.9 nM		c-Kit	99%
SU 5402		++ VEGFR2, IC50: 20 nM			98%
Apatinib 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	99%
Cabozantinib		++++ VEGFR2/KDR, IC50: 0.035 nM			98%
Sorafenib		++ VEGFR2/Flk1, IC50: 90 nM VEGFR2, 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			98%
Semaxinib		+ VEGFR2/Flk1, IC50: 1.23 μM			98%
Vandetanib		++ VEGFR2, IC50: 40 nM	+ VEGFR3, IC50: 110 nM	EGFR	99%
SAR131675			++ VEGFR3, IC50: 23 nM		99%+
ENMD-2076		+ VEGFR2/KDR, IC50: 58.2 nM	++ VEGFR3/FLT4, IC50: 15.9 nM	RET,FLT3	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, 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 WT, IC50: 32 nM BRAF(V600E), IC50: 23 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 WT, IC50: 15 nM BRAF(V600E), IC50: 5.8 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			98%
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。

Cell Line MV4;11 cells MV4;11 cells A375M cells A375M cells A549 MiaPaCa2 B-CPAP TT CAL62	Concentration	Treated Time	Description	References
MV4;11 cells	1.0 µM	24 hours	To evaluate the inhibitory effect of RAF265 on FDG accumulation in MV4;11 cells, results showed that RAF265 did not significantly inhibit FDG accumulation at 24 hours.	Neoplasia. 2011 Mar;13(3):266-75.
MV4;11 cells	0.1 µM	24 hours	To evaluate the inhibitory effect of RAF265 on FDG accumulation in MV4;11 cells, results showed that RAF265 did not significantly inhibit FDG accumulation at 24 hours.	Neoplasia. 2011 Mar;13(3):266-75.
A375M cells	1.0 µM	28 hours	To evaluate the inhibitory effect of RAF265 on FDG accumulation in A375M cells, results showed that RAF265 significantly inhibited FDG accumulation at 28 hours with an inhibition rate of 75.5%.	Neoplasia. 2011 Mar;13(3):266-75.
A375M cells	0.1 µM	28 hours	To evaluate the inhibitory effect of RAF265 on FDG accumulation in A375M cells, results showed that RAF265 significantly inhibited FDG accumulation at 28 hours with an inhibition rate of 38.2%.	Neoplasia. 2011 Mar;13(3):266-75.
A549	0.1 to 2.5 µM	4 hours	RAF265 induced paradoxical ERK activation at low/intermediate concentrations (0.1 to 2.5 μM), with relatively little changes occurring at the level of MEK and p90RSK phosphorylation	J Exp Clin Cancer Res. 2018 Jul 9;37(1):140.
MiaPaCa2	0.1 to 2.5 µM	4 hours	RAF265 induced paradoxical ERK activation at low/intermediate concentrations (0.1 to 2.5 μM), with relatively little changes occurring at the level of MEK and p90RSK phosphorylation	J Exp Clin Cancer Res. 2018 Jul 9;37(1):140.
B-CPAP	200 nM	5 days	RAF265 significantly inhibited the proliferation of B-CPAP cells and showed synergistic effects when combined with BEZ-235.	Clin Cancer Res. 2011 Oct 15;17(20):6482-9.
TT	200 nM	5 days	RAF265 significantly inhibited the proliferation of TT cells and showed synergistic effects when combined with BEZ-235.	Clin Cancer Res. 2011 Oct 15;17(20):6482-9.
CAL62	200 nM	5 days	RAF265 significantly inhibited the proliferation of CAL62 cells and showed synergistic effects when combined with BEZ-235.	Clin Cancer Res. 2011 Oct 15;17(20):6482-9.

Species Nude mice Nude mice Nude mice	Animal Model CAL62 and TT xenograft models A375M tumor xenograft model Human metastatic melanoma tumor model	Administration	Dosage	Frequency	Description	References
Nude mice	CAL62 and TT xenograft models	Oral	10 mg/kg	Thrice weekly, throughout the experiment	RAF265 significantly inhibited tumor growth in CAL62 and TT xenograft models and showed enhanced inhibition when combined with BEZ-235.	Clin Cancer Res. 2011 Oct 15;17(20):6482-9.
Nude mice	A375M tumor xenograft model	Oral	100 mg/kg	Every 3 days for 15 days	To evaluate the inhibitory effect of RAF265 on FDG accumulation in the A375M tumor xenograft model, results showed that RAF265 significantly inhibited FDG accumulation as early as 1 day after treatment, and the inhibitory effect persisted until the end of treatment.	Neoplasia. 2011 Mar;13(3):266-75.
Nude mice	Human metastatic melanoma tumor model	Oral	40 mg/kg	Once daily for 30 days	To evaluate the effect of RAF265 on the growth of human metastatic melanoma tumors, results showed that 7/17 tumors responded to RAF265 treatment with more than 50% reduction in tumor volume	Clin Cancer Res. 2012 Apr 15;18(8):2184-98

CAS号	927880-90-8
分子式	C₂₄H₁₆F₆N₆O
分子量	518.41
SMILES Code	FC(C1=CC=C(NC2=NC3=CC(OC4=CC(C5=NC=C(C(F)(F)F)N5)=NC=C4)=CC=C3N2C)C=C1)(F)F
MDL No.	MFCD16659061

别名	CHIR-265
运输	蓝冰
InChI Key	YABJJWZLRMPFSI-UHFFFAOYSA-N
Pubchem ID	11656518

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

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