Infigratinib phosphate | BGJ-398 phosphate | FGFR Inhibitor

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Infigratinib phosphate {[allProObj[0].p_purity_real_show]}

货号：A980301 同义名： BGJ-398 phosphate; NVP-BGJ398 phosphate

BGJ398 Phosphate is a selective and potent inhibitor of FGFRs with IC50 values of 1nM for FGFR11-3 and 60nM for FGFR4, as well as 4.9nM for FGFR3-K650E mutant.

Infigratinib phosphate 化学结构
CAS号：1310746-10-1

Infigratinib phosphate 3D分子结构
CAS号：1310746-10-1

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Infigratinib phosphate 纯度/质量文件产品仅供科研

货号：A980301 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

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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		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			FLT3,RET	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。

Infigratinib phosphate 生物活性

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 1nM for FGFR11-3 and 60nM for FGFR4, as well as 4.9nM 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 5nM. Consistent with the in vitro study, BGJ398 inhibited the proliferation of the FGFR1-, FGFR2-, and FGFR3-dependent BaF3 cells with IC50 values ranged from 0.7-52.2nM depended by different FGFR isoforms. Daily oral treatment with BGJ398 at dose of 10 or 30mg/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 15mg/kg in RT112 human bladder cancer xenografted rats.^[1]

作用机制

BGJ398 Phosphate binds with ATP-binding pocket of FGFR3.^[1]

Infigratinib phosphate 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.

Infigratinib phosphate 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.52mL

0.30mL

0.15mL

7.59mL

1.52mL

0.76mL

15.19mL

3.04mL

1.52mL

Infigratinib phosphate 技术信息

CAS号	1310746-10-1
分子式	C₂₆H₃₄Cl₂N₇O₇P
分子量	658.47
SMILES Code	O=P(O)(O)O.ClC1=C(C(Cl)=C(C=C1OC)OC)NC(N(C2=CC(NC3=CC=C(C=C3)N4CCN(CC4)CC)=NC=N2)C)=O
MDL No.	MFCD26960938

别名	BGJ-398 phosphate; NVP-BGJ398 phosphate
运输	蓝冰

存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, 2-8°C

溶解方案

动物实验：配制的工作液建议现用现配，短期内尽快用完。以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

方案一

Infigratinib phosphate {[allProObj[0].p_purity_real_show]}

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Infigratinib phosphate 参考文献

Infigratinib phosphate 实验方案

Infigratinib phosphate 技术信息

最近浏览的产品

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