Futibatinib | TAS-120 | FGFR Inhibitor | AmBeed-信号通路专用抑制剂

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产品名称	FGFR ↓ ↑	FGFR1 ↓ ↑	FGFR2 ↓ ↑	FGFR3 ↓ ↑	FGFR4 ↓ ↑	其他靶点	纯度
Tyrphostin AG1296	+ FGFR (Swiss 3T3), IC50: 12.3 μM					PDGFR	99%+
Pazopanib	+ FGFR, IC50: 140 nM						99%
Erdafitinib	✔					RET	99%+
Gambogenic acid	✔						98+%
Sulfatinib		+++ FGFR1, IC50: 15 nM					99+%
Nintedanib esylate		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM			98%
Zoligratinib		+++ FGFR1, IC50: 9.3 nM	+++ FGFR2, IC50: 7.6 nM	++ FGFR3, IC50: 22 nM	+ FGFR4, IC50: 290 nM		99%+
MK-2461		+ FGFR1, IC50: 65 nM	++ FGFR2, IC50: 39 nM	++ FGFR3, IC50: 50 nM			98%+
SU 5402		++ FGFR1, IC50: 30 nM					98%
Brivanib		+ FGFR1, IC50: 148 nM					99%+
Lucitanib		++ FGFR1, IC50: 17.5 nM	+ FGFR2, IC50: 82.5 nM				99%+
Ponatinib		++++ FGFR1, IC50: 2.2 nM					98%
PD-166866		+ FGFR1, IC50: 52.4 nM					99%
Narazaciclib		++ FGFR1, IC50: 26 nM				RET	99%+
Lactate		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		FLT3,c-Kit	85%
Lenvatinib mesylate		++ FGFR1, IC50: 46 nM				c-RET	99%
LY2874455		++++ FGFR1, IC50: 2.8 nM	++++ FGFR2, IC50: 2.6 nM	+++ FGFR3, IC50: 6.4 nM	+++ FGFR4, IC50: 6 nM		99%+
FIIN-2		+++ FGFR1, IC50: 3.09 nM	+++ FGFR2, IC50: 4.3 nM	++ FGFR3, IC50: 27 nM	++ FGFR4, IC50: 45.3 nM		99%
FIIN-3		+++ FGFR1, IC50: 13.1 nM	++ FGFR2, IC50: 21 nM	++ FGFR3, IC50: 31.4 nM	++ FGFR4, IC50: 35.3 nM		98%
Infigratinib		++++ FGFR1, IC50: 0.9 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.0 nM FGFR3 (K650E), IC50: 4.9 nM	+ FGFR4, IC50: 60 nM		99%+
Danusertib		++ FGFR1, IC50: 47 nM				RET	99%+
R1530		++ FGFR1, IC50: 28 nM					98%
ENMD-2076		+ FGFR1, IC50: 92.7 nM	+ FGFR2, IC50: 70.8 nM			RET,FLT3	98%
Dovitinib		+++ FGFR1, IC50: 8 nM		+++ FGFR3, IC50: 9 nM		FLT3,c-Kit	99%+
Sorafenib		+ FGFR1, IC50: 580 nM					99%
SSR128129E		+ FGFR1, IC50: 1.9 μM					99%+
AZD-4547		++++ FGFR1, IC50: 0.2 nM	++++ FGFR2, IC50: 2.5 nM	++++ FGFR3, IC50: 1.8 nM			98%
Lenvatinib		++ FGFR1, IC50: 46 nM				RET	98%
PD173074		++ FGFR1, IC50: ~25 nM					99%+
S49076		++ FGFR1, IC50: 18 nM	+++ FGFR2, IC50: 17 nM	+++ FGFR3, IC50: 15 nM			98%
Futibatinib		++++ FGFR1, IC50: 1.8 nM	++++ FGFR2, IC50: 1.4 nM	++++ FGFR3, IC50: 1.6 nM	+++ FGFR4, IC50: 3.7 nM		99%+
Ferulic Acid		+ FGFR1, IC50: 3.78 μM	+ FGFR2, IC50: 12.5 μM				98%
Nintedanib		+ FGFR1, IC50: 69 nM	++ FGFR2, IC50: 37 nM	+ FGFR3, IC50: 108 nM	+ FGFR4, IC50: 610 nM		99+%
ASP5878		++++ FGFR1, IC50: 0.47 nM	++++ FGFR2, IC50: 0.6 nM	++++ FGFR3, IC50: 0.74 nM	+++ FGFR4, IC50: 3.5 nM		99%
PRN1371		++++ FGFR1, IC50: 0.6 nM	++++ FGFR2, IC50: 1.3 nM	+++ FGFR3, IC50: 4.1 nM	++ FGFR4, IC50: 19.3 nM		99%
Derazantinib		+++ FGFR1, IC50: 4.5 nM	++++ FGFR2, IC50: 1.8 nM	+++ FGFR3, IC50: 4.5 nM	++ FGFR4, IC50: 34 nM	RET	99%+
ODM-203		+++ FGFR1, IC50: 11 nM	+++ FGFR2, IC50: 16 nM	+++ FGFR3, IC50: 6 nM	++ FGFR4, IC50: 35 nM		99%+
Pemigatinib		++++ FGFR1, IC50: 0.4 nM	++++ FGFR2, IC50: 0.5 nM	++++ FGFR3, IC50: 1.2 nM	++ FGFR4, IC50: 30 nM		99%+
SKLB 610			✔			PDGFR	99%+
Alofanib			✔				99%+
Lirafugratinib			✔				99%
Masitinib mesylate				✔		FAK	99%+
BLU9931				+ FGFR3, IC50: 150 nM	+++ FGFR4, IC50: 3 nM		99%+
BO-264				✔			99%+
Fisogatinib					+++ FGFR4, IC50: 5 nM		99%+
H3B-6527					++++ FGFR4, IC50: <1.2 nM		99%+
Roblitinib					++++ FGFR4, IC50: 1.9 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。

Cell Line MCF10A cells ICC13-7 cells CCLP-1 cells H69-FGFR2-BICC1/BRAF V600E cells H69-FGFR2-BICC1/KRAS G12D cells H69 cells SCMC RH4 RMS559 Ba/F3 TEL-FGFR4	Concentration	Treated Time	Description	References
MCF10A cells	0.2 µM	3 hours 45 minutes	To assess the effect of Futibatinib on FGFR signaling pathways, results showed Futibatinib significantly inhibited phosphorylation of Akt and ERK1/2	Sci Rep. 2023 Nov 18;13(1):20223.
ICC13-7 cells	10 nM	4 hours	Evaluate the signaling inhibition effect of Futibatinib on FGFR2-PHGDH fusion protein	Clin Cancer Res. 2024 Jan 5;30(1):198-208.
CCLP-1 cells	50 nM	4 hours	Evaluate the signaling inhibition effect of Futibatinib on FGFR2-PHGDH fusion protein	Clin Cancer Res. 2024 Jan 5;30(1):198-208.
H69-FGFR2-BICC1/BRAF V600E cells	40 µM	72 hours	To evaluate the impact of BRAF V600E mutation on Futibatinib sensitivity, results showed BRAF V600E mutation significantly reduced the inhibitory effect of Futibatinib.	J Hepatol. 2024 Feb;80(2):322-334.
H69-FGFR2-BICC1/KRAS G12D cells	40 µM	72 hours	To evaluate the impact of KRAS G12D mutation on Futibatinib sensitivity, results showed KRAS G12D mutation significantly reduced the inhibitory effect of Futibatinib.	J Hepatol. 2024 Feb;80(2):322-334.
H69 cells	12.5 nM	72 hours	To evaluate the sensitivity of Futibatinib in FGFR2-BICC1 fusion cells, results showed Futibatinib significantly inhibited the growth of fusion cells.	J Hepatol. 2024 Feb;80(2):322-334.
SCMC	11.7 µM	72 hours	Evaluate the inhibitory effect of Futibatinib on SCMC cells, results show Futibatinib has weaker inhibitory effect on SCMC cells.	Cancers (Basel). 2023 Aug 9;15(16):4034.
RH4	6.64 µM	72 hours	Evaluate the inhibitory effect of Futibatinib on RH4 cells, results show Futibatinib has weaker inhibitory effect on RH4 cells.	Cancers (Basel). 2023 Aug 9;15(16):4034.
RMS559	0.48 µM	72 hours	Evaluate the inhibitory effect of Futibatinib on RMS559 cells, results show Futibatinib significantly inhibits cell growth.	Cancers (Basel). 2023 Aug 9;15(16):4034.
Ba/F3 TEL-FGFR4	1.33 nM	72 hours	Evaluate the inhibitory effect of Futibatinib on Ba/F3 TEL-FGFR4 cells, results show Futibatinib selectively kills cells through FGFR4 inhibition.	Cancers (Basel). 2023 Aug 9;15(16):4034.

Species Rat Female athymic nude mice Nude mice NOD SCID Gamma (NSG) mice NSG mice NOD/SCID gamma mice NSG mice	Animal Model Sprague-Dawley rats Breast cancer PDX models FGFR2-BICC1 and FGFR2-BICC1/KRAS G12D xenograft models RMS559, RH4, and SCMC xenograft models CCLP-1 xenograft model Patient-derived xenograft (PDX) model CCLP-1 xenograft model	Administration	Dosage	Frequency	Description	References
Rat	Sprague-Dawley rats	Oral	10 mg/kg	Single dose	For pharmacokinetic study, to determine the concentration of orelabrutinib in plasma	Front Pharmacol. 2022 Sep 6;13:991281
Female athymic nude mice	Breast cancer PDX models	Oral	15 mg/kg	Daily for 28 days or until tumor diameter reached 1.5 cm3	To evaluate the antitumor activity of Futibatinib in FGFR-altered breast cancer PDX models, results showed significant tumor growth inhibition in FGFR2-amplified and FGFR2 Y375C mutant models	Sci Rep. 2023 Nov 18;13(1):20223.
Nude mice	FGFR2-BICC1 and FGFR2-BICC1/KRAS G12D xenograft models	Oral gavage	5 mg/kg Futibatinib and 6 mg/kg Binimetinib	Once daily for 14 days	To evaluate the antitumor effect of Futibatinib alone or in combination with Binimetinib in FGFR2-BICC1 and FGFR2-BICC1/KRAS G12D xenograft models, results showed combination therapy significantly inhibited tumor growth in FGFR2-BICC1 model but had limited effect in FGFR2-BICC1/KRAS G12D model.	J Hepatol. 2024 Feb;80(2):322-334.
NOD SCID Gamma (NSG) mice	RMS559, RH4, and SCMC xenograft models	Oral gavage	5-25 mg/kg	Once daily for three weeks	Evaluate the efficacy of Futibatinib monotherapy in RMS xenograft models, results show Futibatinib monotherapy had no significant effect on tumor growth or survival.	Cancers (Basel). 2023 Aug 9;15(16):4034.
NSG mice	CCLP-1 xenograft model	Oral gavage	6 mg/kg	Once daily for 10 days	Evaluate the in vivo efficacy of Futibatinib on FGFR2-PHGDH-N550K mutant tumors	Clin Cancer Res. 2024 Jan 5;30(1):198-208.
NOD/SCID gamma mice	Patient-derived xenograft (PDX) model	Not used	6 mg/kg	Once daily for up to 50 days	Evaluate the antitumor activity of Futibatinib against FGFR2 kinase domain mutations in PDX models	Clin Cancer Res. 2024 Nov 1;30(21):4943-4956
NSG mice	CCLP-1 xenograft model	Oral gavage	6 mg/kg	Once daily for 10 days	Evaluate the in vivo efficacy of futibatinib against FGFR2-N550K mutation	Clin Cancer Res. 2024 Jan 5;30(1):198-208.

CAS号	1448169-71-8
分子式	C₂₂H₂₂N₆O₃
分子量	418.45
SMILES Code	C=CC(N1C[C@@H](N2N=C(C#CC3=CC(OC)=CC(OC)=C3)C4=C(N)N=CN=C42)CC1)=O
MDL No.	MFCD29037352

别名	TAS-120
运输	蓝冰
InChI Key	KEIPNCCJPRMIAX-HNNXBMFYSA-N
Pubchem ID	71621331

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FGFR2	FGFR2, IC50:1.4 nM
FGFR3	FGFR3, IC50:1.6 nM
FGFR4	FGFR4, IC50:3.7 nM
FGFR1	FGFR1, IC50:1.8 nM

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