Infigratinib | NVP-BGJ398 | FGFR Inhibitor | AmBeed-信号通路专用抑制剂

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Infigratinib 99%+

货号：A107926 同义名： NVP-BGJ398;BGJ398

Infigratinib（BGJ-398；NVP-BGJ398）对FGFR家族具有强效抑制作用，对FGFR1、FGFR2、FGFR3和FGFR4的IC50值分别为0.9 nM、1.4 nM、1 nM和60 nM。

Infigratinib 化学结构
CAS号：872511-34-7

Infigratinib 3D分子结构
CAS号：872511-34-7

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Infigratinib 纯度/质量文件产品仅供科研

货号：A107926 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: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]; • JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

MAO 亚型比较
FGFR 亚型比较

产品名称	MAO ↓ ↑	MAO-A ↓ ↑	MAO-B ↓ ↑	纯度
Sennoside A	++ MAO, IC50: 17 μM			98%+
Glycyrrhizic acid	++++ MAO, IC50: 0.16 μM			80% HPLC
Rasagiline		++++ MAO-A, IC50: 412 nM	++++ MAO-B, IC50: 4.43 nM	99+%
Isatin	++ MAO, IC50: 15 μM	+ MAO-A, IC50: 58 μM	++ MAO-B, IC50: 14 μM	98%
Paeonol		+ MAO-A, IC50: 54.6 μM	+ MAO-B, IC50: 42.5 μM	98%
Tranylcypromine hydrochloride		+++ MAO-A, IC50: 11.5 μM	+++ MAO-B, IC50: 7 μM	97%
Moclobemide		+++ MAO-A (5-HT), IC50: 6.1 μM		99%+
Pargyline HCl		++ MAO-A, Ki: 13 μM	+++ MAO-B, Ki: 0.5 μM	99%+
Safinamide			++++ MAO-B, IC50: 98 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。

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					98%
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		98%
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		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		98%
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			✔				98%
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。

Infigratinib 生物活性

靶点	FGFR2 FGFR2, IC50:1.4 nM FGFR3 FGFR3, IC50:1.0 nM FGFR3 (K650E), IC50:4.9 nM FGFR4 FGFR4, IC50:60 nM FGFR1 FGFR1, IC50:0.9 nM
描述	The FGFR (fibroblast growth factor receptor) family, comprising four members, FGFR1, FGFR2, FGFR3 and FGFR4, belongs to the RTKs which serve as high affinity receptors for FGFs controlling cell proliferation, migration, apoptosis and differentiation. BGJ398 is a selective and potent inhibitor of FGFRs with IC50 values of 1 nM for FGFR11-3 and 60 nM for FGFR4, as well as 4.9 nM for FGFR3-K650E mutant (measured by purified recombinant enzymes). Treatment with BGJ398 in cell lysate from HEK293 cells transfected with FGFRs resulted in inhibition on autophosphorylation on specific tyrosine residues of FGFR 1 - 3 with IC50 values below 5 nM. Consistent with the in vitro study, BGJ398 inhibited the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values ranged from 0.7 - 52.2 nM depended by different FGFR isoforms. Daily oral treatment with BGJ398 at dose of 10 or 30 mg/kg for 12 consecutive days induced tumor growth inhibition in the orthotopic xenograft bladder cancer model. Similarly, nearly complete tumor stasis was achieved by oral treatment of BGJ398 at dose of 5, 10 and 15 mg/kg in RT112 human bladder cancer xenografted rats^[1].
作用机制	BGJ398 binds with ATP-binding pocket of FGFR3^[1].

Infigratinib 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
AN3CA		Growth Inhibition Assay		IC50=1.00 ± 0.20 μM	23443805
ECC1		Growth Inhibition Assay		IC50=6.74 ± 0.59 μM	23443805
EFE184		Growth Inhibition Assay		IC50=8.04 ± 0.69 μM	23443805
EN		Growth Inhibition Assay		IC50=6.03 ± 0.31 μM	23443805

Infigratinib 动物研究

Dose

Rat^[1] (p.o.): 4.25 mg/kg, 8.51 mg/kg; Mice: 5 mg/kg^[1] (i.v.), 20 mg/kg^[1] (p.o.), 50 mg/kg^[2] (p.o.)

Administration

i.v., p.o.

Pharmacokinetics

Animal	Nude mice^[1]	Rats^[1]
Dose	5 mg/kg (i.v.) 20 mg/kg (p.o.)	5 mg/kg (i.v.) 10 mg/kg (p.o.)
Administration	i.v. p.o.	i.v. p.o.
C_max	0.86 μM (i.v.) 0.42 μM (p.o.)	0.97 μM (i.v.) 0.26 μM (p.o.)
T_1/2	9.3 h (i.v.) 4.3 h (p.o.)	4.5 h (i.v.) 4.8 h (p.o.)
F	32% (p.o.)	51% (p.o.)
T_max	1 h (p.o.)	4 h (p.o.)
V_ss	26 L/kg (i.v.)
Vss		9.6 L/kg (i.v.)
CL	3.3 L/h/kg (i.v.)	3.6 L/h/kg (i.v.)
AUC_{(normalized to 1 mg/kg)}	0.6 μM·h (i.v.) 0.18 μM·h (p.o.)	0.49 μM·h (i.v.) 0.25 μM·h (p.o.)

Infigratinib 参考文献

[1]Guagnano V, Furet P, et al. Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem. 2011 Oct 27;54(20):7066-83.

[2]Xiao L, Du E, et al. Inhibition of FGFR Signaling Partially Rescues Hypophosphatemic Rickets in HMWFGF2 Tg Male Mice. Endocrinology. 2017 Oct 1;158(10):3629-3646.

Infigratinib 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.78mL

0.36mL

0.18mL

8.92mL

1.78mL

0.89mL

17.84mL

3.57mL

1.78mL

Infigratinib 技术信息

CAS号	872511-34-7
分子式	C₂₆H₃₁Cl₂N₇O₃
分子量	560.475

别名	NVP-BGJ398;BGJ398;NVP-BGJ398
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 12 mg/mL(21.41 mM)，配合低频超声助溶，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

1%CMC-Na+water 30 mg/mL suspension

AN3CA		Growth Inhibition Assay		IC50=1.00 ± 0.20 μM	23443805
ECC1		Growth Inhibition Assay		IC50=6.74 ± 0.59 μM	23443805
EFE184		Growth Inhibition Assay		IC50=8.04 ± 0.69 μM	23443805
EN		Growth Inhibition Assay		IC50=6.03 ± 0.31 μM	23443805
EN1		Growth Inhibition Assay		IC50=4.75 ± 0.62 μM	23443805
HCC	1-2500 nM	Growth Inhibition Assay	48 h	IC50= 2359 nm	25688743
HCC	1-2500 nM	Growth Inhibition Assay	48 h	IC50=1124 nm	25688743
HCD9	0.5-5 μM	Growth Inhibition Assay	48/72 h	decreases cell viability	24135816
HCT116		Growth Inhibition Assay	48 h	IC50=3 μM	24503538
HCT116	0.5-5 μM	Growth Inhibition Assay	48/72 h	decreases cell viability	24135816
HEC155		Growth Inhibition Assay		IC50=4.74 ± 1.09 μM	23443805
HEC1A		Growth Inhibition Assay		IC50=10.00 ± 1.00 μM	23443805
HEC1B		Growth Inhibition Assay		IC50=6.45 ± 0.67 μM	23443805
HKH2		Growth Inhibition Assay	48 h	IC50=4 μM	24503538
ISHIKAWA		Growth Inhibition Assay		IC50=5.48 ± 0.03 μM	23443805
KLE		Growth Inhibition Assay		IC50=3.03 ± 0.11 μM	23443805
LS174T		Growth Inhibition Assay	48 h	IC50=4 μM	24503538
MFE280		Growth Inhibition Assay		IC50=2.63 ± 0.82 μM	23443805
MFE296		Growth Inhibition Assay		IC50=2.86 ± 0.20 μM	23443805
MFE319		Growth Inhibition Assay		IC50=5.37 ± 0.03 μM	23443805
RKO		Growth Inhibition Assay	48 h	IC50=1.2 μM	24503538
RL952		Growth Inhibition Assay		IC50=3.41 ± 0.23 μM	23443805
SNGII		Growth Inhibition Assay		IC50=4.29 ± 0.58 μM	23443805
SNGM		Growth Inhibition Assay		IC50=5.00 ± 0.41 μM	23443805
SNU-C1	0.5-5 μM	Growth Inhibition Assay	48/72 h	no effect	24135816
SPAC1L		Growth Inhibition Assay		IC50=4.92 ± 0.50 μM	23443805
SPAC1S		Growth Inhibition Assay		IC50=3.19 ± 0.93 μM	23443805
USPC1		Growth Inhibition Assay		IC50=5.75 ± 0.50 μM	23443805
USPC2		Growth Inhibition Assay		IC50=7.00 ± 0.21 μM	23443805

Infigratinib 99%+

Infigratinib 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Infigratinib 质控信息

Infigratinib 生物活性

Infigratinib 细胞研究

Infigratinib 动物研究

Infigratinib 参考文献

Infigratinib 实验方案

Infigratinib 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

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FGFR2	FGFR2, IC50:1.4 nM
FGFR3	FGFR3, IC50:1.0 nM FGFR3 (K650E), IC50:4.9 nM
FGFR4	FGFR4, IC50:60 nM
FGFR1	FGFR1, IC50:0.9 nM

Infigratinib 99%+

Infigratinib 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Infigratinib 质控信息

Infigratinib 生物活性

Infigratinib 细胞研究

Infigratinib 动物研究

Infigratinib 参考文献

Infigratinib 实验方案

Infigratinib 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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热门区域

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Infigratinib 纯度/质量文件产品仅供科研