Roblitinib | FGF-401 | FGFR4 Inhibitor | AmBeed-信号通路专用抑制剂

Roblitinib {[allProObj[0].p_purity_real_show]}

货号：A303280 同义名： FGF-401

Roblitinib是一种人类成纤维生长因子受体4（FGFR4）抑制剂，IC50为1.1 nM，具有潜在的抗肿瘤活性。

Roblitinib 化学结构
CAS号：1708971-55-4

Roblitinib 3D分子结构
CAS号：1708971-55-4

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FGFR 亚型比较

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		c-Kit,FLT3	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 (K650E), IC50: 4.9 nM FGFR3, IC50: 1.0 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		c-Kit,FLT3	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。

Roblitinib 生物活性

靶点

FGFR4

FGFR4, IC50:1.9 nM

描述

Roblitinib, also known as FGF-401, is an orally active, highly selective inhibitor of FGFR4, with an IC50 of 1.9 nM. Roblitinib shows no activity against FGFR1, FGFR2, FGFR3, rat FGFR4, and C552A FGFR4 (all IC50s >10 µM). It inhibits HUH7 (IC50=12 nM), Hep3B (IC50=9 nM), JHH7 (IC50=9 nM), while showing no inhibitory activity in HEPG2 and JHH (both IC50s >10 µM)^[1].

Roblitinib 细胞实验

Cell Line HCC09-0913 cells MDA-MB-361 MDA-MB-453 AU565 BT474 SKBR3 MKN45 cells	Concentration	Treated Time	Description	References
HCC09-0913 cells	1 µM	24 hours	To evaluate the inhibitory effect of FGF401 on the FGF19/FGFR-4 signaling pathway, results showed FGF401 inhibited phosphorylation of FRS-2α and Erk1/2	Exp Mol Med. 2020 Nov;52(11):1857-1868.
MDA-MB-361	0.5 μM		Evaluate the anti-tumor effect of Roblitinib on MDA-MB-361 cells, results showed Roblitinib significantly inhibited cell proliferation	Nat Commun. 2022 May 13;13(1):2672.
MDA-MB-453	0.5 μM		Evaluate the anti-tumor effect of Roblitinib on MDA-MB-453 cells, results showed Roblitinib significantly inhibited cell proliferation	Nat Commun. 2022 May 13;13(1):2672.
AU565	0.5 μM		Evaluate the anti-tumor effect of Roblitinib on AU565 cells, results showed Roblitinib significantly inhibited cell proliferation	Nat Commun. 2022 May 13;13(1):2672.
BT474	0.5 μM		Evaluate the anti-tumor effect of Roblitinib on BT474 cells, results showed Roblitinib significantly inhibited cell proliferation	Nat Commun. 2022 May 13;13(1):2672.
SKBR3	0.5 μM		Evaluate the anti-tumor effect of Roblitinib on SKBR3 cells, results showed Roblitinib significantly inhibited cell proliferation	Nat Commun. 2022 May 13;13(1):2672.
MKN45 cells	20 μM	24 hours	Roblitinib inhibits FGFR4 kinase activity and reverses the pro-oncogenic effects of FGF19 and LIF on MKN45 cells.	Cell Oncol (Dordr). 2024 Apr;47(2):695-710.

Cell Line

HCC09-0913 cells MDA-MB-361 MDA-MB-453 AU565 BT474 SKBR3 MKN45 cells

Concentration

Treated Time

Description

References

HCC09-0913 cells

1 µM

24 hours

To evaluate the inhibitory effect of FGF401 on the FGF19/FGFR-4 signaling pathway, results showed FGF401 inhibited phosphorylation of FRS-2α and Erk1/2

Exp Mol Med. 2020 Nov;52(11):1857-1868.

MDA-MB-361

0.5 μM

Evaluate the anti-tumor effect of Roblitinib on MDA-MB-361 cells, results showed Roblitinib significantly inhibited cell proliferation

Nat Commun. 2022 May 13;13(1):2672.

MDA-MB-453

0.5 μM

Evaluate the anti-tumor effect of Roblitinib on MDA-MB-453 cells, results showed Roblitinib significantly inhibited cell proliferation

Nat Commun. 2022 May 13;13(1):2672.

AU565

0.5 μM

Evaluate the anti-tumor effect of Roblitinib on AU565 cells, results showed Roblitinib significantly inhibited cell proliferation

Nat Commun. 2022 May 13;13(1):2672.

BT474

0.5 μM

Evaluate the anti-tumor effect of Roblitinib on BT474 cells, results showed Roblitinib significantly inhibited cell proliferation

Nat Commun. 2022 May 13;13(1):2672.

SKBR3

0.5 μM

Evaluate the anti-tumor effect of Roblitinib on SKBR3 cells, results showed Roblitinib significantly inhibited cell proliferation

Nat Commun. 2022 May 13;13(1):2672.

MKN45 cells

20 μM

24 hours

Roblitinib inhibits FGFR4 kinase activity and reverses the pro-oncogenic effects of FGF19 and LIF on MKN45 cells.

Cell Oncol (Dordr). 2024 Apr;47(2):695-710.

Roblitinib 动物实验

Species BALB/c nude mice Mice	Animal Model RSKBR3 and MDA-MB-361 tumor models HCC25-0705A xenograft model	Administration	Dosage	Frequency	Description	References
BALB/c nude mice	RSKBR3 and MDA-MB-361 tumor models	Oral	30 mg/kg		Evaluate the anti-tumor effect of Roblitinib in vivo, results showed Roblitinib significantly inhibited tumor growth	Nat Commun. 2022 May 13;13(1):2672.
Mice	HCC25-0705A xenograft model	Oral	20, 30, and 40 mg/kg	Twice daily for indicated days	To evaluate the dose-response of FGF401, results showed 30 mg/kg FGF401 significantly inhibited tumor growth	Exp Mol Med. 2020 Nov;52(11):1857-1868.

Species

BALB/c nude mice Mice

Animal Model

RSKBR3 and MDA-MB-361 tumor models HCC25-0705A xenograft model

Administration

Dosage

Frequency

Description

References

BALB/c nude mice

RSKBR3 and MDA-MB-361 tumor models

Oral

30 mg/kg

Evaluate the anti-tumor effect of Roblitinib in vivo, results showed Roblitinib significantly inhibited tumor growth

Nat Commun. 2022 May 13;13(1):2672.

Mice

HCC25-0705A xenograft model

Oral

20, 30, and 40 mg/kg

Twice daily for indicated days

To evaluate the dose-response of FGF401, results showed 30 mg/kg FGF401 significantly inhibited tumor growth

Exp Mol Med. 2020 Nov;52(11):1857-1868.

Roblitinib 动物研究

Animal study

Roblitinib reduces plasma concentration to below the IC90 threshold within 8 hours and maintains tumor growth at a standstill with the lowest dose of 10 mg/kg for 6 days. Administering Roblitinib to animals, via oral gavage at doses of 10-100 mg/kg twice daily for 10 days, achieves maximal suppression of FGFR4-dependent tumor growth in the Hep3B xenograft model. Roblitinib has a half-life (T1/2) of 1.4 hours, a clearance (CL) of 28 mL/min•kg, and a steady-state volume of distribution (Vss) of 2.3 L/kg in male mice (C57BL/6)^[1].

Roblitinib 参考文献

Roblitinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL

Roblitinib 技术信息

CAS号	1708971-55-4
分子式	C₂₅H₃₀N₈O₄
分子量	506.56
SMILES Code	O=C(N1CCCC2=C1N=C(C=O)C(CN3C(CN(C)CC3)=O)=C2)NC4=NC=C(C#N)C(NCCOC)=C4
MDL No.	MFCD31381923

别名	FGF-401
运输	蓝冰
InChI Key	BHKDKKZMPODMIQ-UHFFFAOYSA-N
Pubchem ID	118036971

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, 2-8°C

溶解方案

细胞实验：

DMSO: 4 mg/mL(7.9 mM)，配合低频超声，并水浴加热至45℃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

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