Lirafugratinib | RLY-4008 | EGFR | AmBeed-信号通路专用抑制剂

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Lirafugratinib {[allProObj[0].p_purity_real_show]}

货号：A1678566 同义名： RLY-4008

Lirafugratinib是一种针对 FGFR2 的抑制剂，具有口服活性。它通过抑制 FGFR2 的活性，抑制肿瘤细胞生长，对 FGFR2 突变或扩增的肿瘤具有治疗潜力。

Lirafugratinib 化学结构
CAS号：2549174-42-5

Lirafugratinib 3D分子结构
CAS号：2549174-42-5

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Lirafugratinib 纯度/质量文件产品仅供科研

货号：A1678566 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: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

EGFR 亚型比较

产品名称	EGFR/ErbB1 ↓ ↑	ErbB3 ↓ ↑	ErbB4 ↓ ↑	HER2/ErbB2 ↓ ↑	mutant EGFR ↓ ↑	其他靶点	纯度
WZ-3146	++++ EGFR (E746_A750/T790M), IC50: 14 nM EGFR (E746_A750), IC50: 2 nM						99%+
Daphnetin	+ EGFR, IC50: 7.67 μM					PKA,PKC	95%
Lifirafenib	++ EGFR, IC50: 29 nM				+ EGFR(T790M/L858R), IC50: 495 nM		98%
PD168393	++++ EGFR, IC50: 0.70 nM						99%+
Nazartinib	++ mutant EGFR, Ki: 0.031 μM				++ mutant EGFR, Ki: 0.031 μM		98%
Norcantharidin	✔						98%
CL-387785	++++ EGFR, IC50: 370 pM						98%
WHI-P154	+++ EGFR, IC50: 4 nM					Src,VEGFR	98%
Tyrphostin A9	+ EGFR, IC50: 460 μM					PDGFR	98%
AG 555	+ EGFR, IC50: 0.7 μM						98%
AG 494	+ EGFR, IC50: 1.2 μM						99%+
AG-556	+ EGFR, IC50: 5 μM						98%
RG13022	+ EGFR, IC50: 4 μM						99%+
Tyrphostin RG 14620	✔						99%+
Vandetanib	+ EGFR, IC50: 500 nM						98%
CNX-2006	++ mutant EGFR, IC50: <20 nM				++ mutant EGFR, IC50: <20 nM		98%
AZD3759	++++ EGFR (WT), IC50: 0.3 nM EGFR (L858R), IC50: 0.2 nM						98%
Erlotinib	++++ EGFR, IC50: 2 nM						95%
Saracatinib	+++ EGFR, IC50: 5 nM EGFR (L861Q), IC50: 4 nM						99%+
AG1557	✔						98%
Rociletinib	++ EGFR (wt), Ki: 303.3 nM EGFR (L858R/T790M), Ki: 21.5 nM						98%
AG490	+ EGFR, IC50: 0.1 μM						98%
Cetuximab	++++ EGFR, Kd: 0.39 nM						98%
Osimertinib	++ L858R/T790M EGFR, IC50: 11.44 nM WT EGFR, IC50: 12.92 nM						99%
Osimertinib mesylate	✔						98% (Content MsOH 15.2-18.2%)
Chrysophanol	✔					mTOR	98%
PD153035	++++ EGFR, Ki: 5.2 pM						99%+
Olmutinib	✔					BTK	99%+
WZ4002	++++ EGFR (L858R/T790M), IC50: 8 nM EGFR (L858R), IC50: 2 nM						99%+
Icotinib	+++ EGFR, IC50: 5 nM						98+%
Desmethyl Erlotinib HCl	++++ EGFR, IC50: 2 nM						98%
Cyasterone	✔						99%+
PP 3	+ EGFR tyrosine kinase, IC50: 2.7 μM						98%
WZ8040	✔						99%+
(-)-Epigallocatechin Gallate	✔						99%
AG 18	+ EGFR, IC50: 35 μM						99%+
O-Desmethyl gefitinib	++ EGFR, IC50: 36 nM						98%
Falnidamol	✔						99%+
AZ-5104	++++ EGFR (L861Q) , IC50: <1 nM EGFR (L858R), IC50: 6 nM		+++ ErbB4, IC50: 7 nM			BRK	99%+
Butein	✔						95%
Genistein	✔						98%
SU5214	+ EGFR, IC50: 36.7 μM						99%+
Naquotinib	✔						99%+
Gefitinib	++ EGFR, IC50: 15.5 nM				+ EGFR (858R/T790M), IC50: 823.3 nM		98%
Theliatinib	+++ WT EGFR, IC50: 3 nM				++ EGFR T790M/L858R, IC50: 22 nM		98+%
Lazertinib	++++ L858R/T790M EGFR, IC50: 2 nM WT EGFR, IC50: 76 nM				++++ Del19/T790M, IC50: 1.7 nM		99%+
Gefitinib-based PROTAC 3	++ EGFR, DC50: 22.3 nM						99%+
MTX-211	✔					PI3K	98%
(E)-AG 99	✔						99%+
Licochalcone D	✔					Caspase,PARP	97%
Zipalertinib	+++ EGFR WT, IC50: 8 nM EGFR (L861Q), IC50: 4.1 nM		+++ HER4, IC50: 4 nM		++++ EGFR(d746-750), IC50: 1.4 nM EGFR L858R, IC50: 2 nM		97%
JND3229	+++ EGFR WT, IC50: 6.8 nM				++ EGFR L858R/T790M, IC50: 30.5 nM		99%+
Firmonertinib mesylate	✔						99%+
Tyrphostin AG30	✔						99%+
EGFR-IN-12	++ EGFR, IC50: 21 nM						99%+
Mobocertinib	✔						98%
(Rac)-JBJ-04-125-02	✔						99%
(S)-Sunvozertinib	✔						98%
BLU-945	✔						95%
Poziotinib	+++ HER1, IC50: 3.2 nM		++ HER4, IC50: 23.5 nM	+++ HER2, IC50: 5.3 nM			98%
TAK-285	++ EGFR/HER1, IC50: 23 nM		+ HER4, IC50: 260 nM	++ HER2, IC50: 17 nM			99%+
ARRY-380 analog				✔			98%
Canertinib	++++ EGFR, IC50: 1.5 nM			+++ ErbB2, IC50: 9.0 nM			99%+
Dacomitinib	+++ EGFR, IC50: 6.0 nM		+ ErbB4, IC50: 73.7 nM	+ ErbB2, IC50: 45.7 nM			98%
EGFR/ErbB-2/ErbB-4 inhibitor-2			+ ErbB4, IC50: 1.91 μM	+ ErbB2, IC50: 0.08 μM			99%+
(E/Z)-CP-724714				++ HER2/ErbB2, IC50: 10 nM			98+%
Lapatinib	++ EGFR, IC50: 10.8 nM		+ ErbB4, IC50: 367 nM	+++ ErbB2, IC50: 9.2 nM			98%
AEE788	++++ EGFR, IC50: 2 nM		+ HER4/ErbB4, IC50: 160 nM	+++ HER2/ErbB2, IC50: 6 nM		c-Fms	98+%
AV-412 free base	++++ EGFR, IC50: 0.75 nM			++ ErbB2, IC50: 19 nM	++++ EGFR^T790M, IC50: 0.79 nM EGFR^L858R/T790M, IC50: 0.51 nM		98+%
Neratinib	+ EGFR, IC50: 92 nM			+ HER2, IC50: 59 nM		Src	98%
BMS-599626	++ HER1, IC50: 20 nM		+ HER4, IC50: 190 nM	++ HER2, IC50: 30 nM			99+%
Tucatinib				+++ ErbB2, IC50: 8 nM			98%
Allitinib	++++ EGFR, IC50: 0.5 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Pelitinib	+ EGFR, IC50: 38.5 nM			+ ErbB2, IC50: 1.255 μM		Src,Raf	99%+
Sapitinib	+++ EGFR, IC50: 4 nM	+++ ErbB3, IC50: 4 nM		+++ ErbB2, IC50: 3 nM			99%+
CUDC-101	+++ EGFR, IC50: 2.4 nM			++ HER2, IC50: 15.7 nM		HDAC	99%+
Varlitinib	+++ ErbB1, IC50: 7 nM			++++ ErbB2, IC50: 2 nM			99%+
Afatinib dimaleate	++++ EGFR (L858R/T790M), IC50: 0.4 nM EGFR (wt), IC50: 0.5 nM			++ HER2, IC50: 14 nM			98%
Canertinib dihydrochloride	+++ EGFR, IC50: 7.4 nM			+++ ErbB2, IC50: 9 nM			98%
Allitinib tosylate	++++ EGFR, IC50: 0.5 nM EGFR (T790M/L858R), IC50: 12 nM		++++ ErbB4, IC50: 0.8 nM	+++ ErbB2, IC50: 3.0 nM			99%
Tyrphostin AG 528	+ EGFR, IC50: 4.9 μM			+ HER2, IC50: 2.1 μM			98%
Afatinib	++++ EGFR (wt), IC50: 0.5 nM EGFR (L858R), IC50: 10 nM		++++ ErbB4, IC50: 1 nM	++ HER2, IC50: 14 nM			99%
Pyrotinib dimaleate	++ EGFR, IC50: 0.013 μM			++ HER2, IC50: 0.038 μM			98%
Epertinib HCl	++++ EGFR, IC50: 1.48 nM		+++ HER4, IC50: 2.49 nM	+++ HER2, IC50: 7.15 nM			98%
Tuxobertinib	++++ EGFR, Kd: 0.2 nM			++++ HER2, Kd: 0.76 nM			98%
ALK-IN-1					++ EGFR(del19), IC50: 36.8 nM EGFR(C797S/del19), IC50: 138.6 nM	ALK	98+%
Brigatinib					+ EGFR(C797S/T790M/del19), IC50: 67.2 nM EGFR(del19), IC50: 39.9 nM	FLT3,ALK	98%
Avitinib					++++ EGFR L858R/T790M, IC50: 0.18 nM	BTK	99%+
EAI045					✔		97%
Almonertinib					✔		98%
BI-4020					++++ EGFR^{del19 T790M C797S}, IC50: 0.2 nM		99%+
EGFR-IN-7					++++ EGFR^{d746-750/T790M/C797S}, IC50: 0.26 nM EGFR^L858R/T790M, IC50: 0.19 nM		98%
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。

Lirafugratinib 生物活性

靶点	FGFR2
描述	Lirafugratinib (RLY-4008) 是一种高度选择性且不可逆的FGFR2抑制剂，专门设计用于靶向FGFR2的激酶结构域。它通过共价结合在FGFR2的一个关键位点处发挥作用，从而阻断FGFR2信号传导途径。
体内研究	雌性BALB/c小鼠分别口服1、5和10 mg/kg，每日2次，Lirafugratinib血浆暴露量随剂量线性增加，但在给药间隔内迅速下降。同时，Lirafugratinib表现出对磷酸化FGFR2 (pFGFR2)的依赖性调节，包括在5和10 mg/kg组中，pFGFR2在给药后2小时完全抑制，10 mg/kg每日2次可观察到肿瘤停滞。
体外研究	Lirafugratinib对FGFR2具有优越的选择性，其对FGFR1/2/3/4的IC50分别为0.77 µM，0.003 µM，0.26 µM和15 µM。Lirafugratinib抑制SNU16细胞系增殖的IC50为0.002 µM，抑制JMSU细胞系增殖的IC50为0.66 µM。

Lirafugratinib 参考文献

[1]Schönherr H, et al. Discovery of lirafugratinib (RLY-4008), a highly selective irreversible small-molecule inhibitor of FGFR2.

Lirafugratinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.81mL

1.96mL

0.98mL

19.63mL

3.93mL

1.96mL

Lirafugratinib 技术信息

CAS号	2549174-42-5
分子式	C₂₈H₂₄FN₇O₂
分子量	509.534

别名	RLY-4008
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

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

溶解度

DMSO: 60 mg/mL(117.75 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

动物实验配方

Lirafugratinib {[allProObj[0].p_purity_real_show]}

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