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PD173074 {[allProObj[0].p_purity_real_show]}

货号：A150425

PD173074是一种有效的FGFR1抑制剂，IC50为25 nM。它还抑制VEGFR2的活性，IC50为100-200 nM，对FGFR1与PDGFR和c-Src的选择性超过1000倍。

PD173074 化学结构 CAS号：219580-11-7
PD173074 化学结构
CAS号：219580-11-7
PD173074 3D分子结构
CAS号：219580-11-7
PD173074 化学结构 CAS号：219580-11-7
PD173074 3D分子结构 CAS号：219580-11-7
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PD173074 纯度/质量文件 产品仅供科研

货号：A150425 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

全球学术期刊中引用的产品

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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

 		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。
产品名称 VEGFR1 ↓ VEGFR2 ↓ VEGFR3 ↓ 其他靶点 纯度
Motesanib Diphosphate ++++

VEGFR1, IC50: 2 nM

 		++++

VEGFR2/Flk1, IC50: 3 nM

VEGFR2, IC50: 3 nM

 		+++

VEGFR3, IC50: 6 nM

 		PDGFR,RET 97%
Tivozanib ++

VEGFR1, IC50: 30 nM

 		+++

VEGFR2, IC50: 6.5 nM

 		++

VEGFR3, IC50: 15 nM

 		99%+
Brivanib +

VEGFR1, IC50: 380 nM

 		++

Flk1, IC50: 25 nM

VEGFR2, IC50: 25 nM

 		99%+
Regorafenib +++

VEGFR1, IC50: 13 nM

 		+++

VEGFR2, IC50: 4.2 nM

 		+

VEGFR3, IC50: 46 nM

 		RET 98%
Pazopanib +++

VEGFR1, IC50: 10 nM

 		++

VEGFR2, IC50: 30 nM

 		+

VEGFR3, IC50: 47 nM

 		FGFR,PDGFR,c-Kit 99%
Sitravatinib +++

VEGFR1 (FLT1), IC50: 6 nM

 		+++

VEGFR2 (KDR), IC50: 5 nM

 		++++

VEGFR3 (FLT4), IC50: 2 nM

 		99%+
Foretinib +++

VEGFR1/FLT1, IC50: 6.8 nM

 		++++

KDR, IC50: 0.86 nM

 		++++

VEGFR3/FLT4, IC50: 2.8 nM

 		Tie-2 99%+
MGCD-265 analog ++++

VEGFR1, IC50: 3 nM

 		++++

VEGFR2, IC50: 3 nM

 		++++

VEGFR3, IC50: 4 nM

 		Tie-2 99%+
Lactate +++

VEGFR1/FLT1, IC50: 10 nM

 		+++

VEGFR2/Flk1, IC50: 13 nM

 		+++

VEGFR3/FLT4, IC50: 8 nM

 		c-Kit,FLT3 85%
AEE788 +

FLT1, IC50: 59 nM

 		+

KDR, IC50: 77 nM

 		EGFR 98+%
Linifanib ++++

VEGFR1/FLT1, IC50: 3 nM

 		++++

VEGFR2/KDR, IC50: 4 nM

 		+

VEGFR3/FLT4, IC50: 190 nM

 		FLT3 99%+
Vatalanib 2HCl +

VEGFR1/FLT1, IC50: 77 nM

 		++

VEGFR2/Flk1, IC50: 270 nM

VEGFR2/KDR, IC50: 37 nM

 		+

VEGFR3/FLT4, IC50: 660 nM

 		c-Kit,c-Fms/CSF1R 99%+
Axitinib ++++

VEGFR1/FLT1, IC50: 0.1 nM

 		++++

VEGFR2/Flk1, IC50: 0.18 nM

VEGFR2/KDR, IC50: 0.2 nM

 		98%
Dovitinib +++

VEGFR1/FLT1, IC50: 10 nM

 		+++

VEGFR2/Flk1, IC50: 13 nM

 		+++

VEGFR3/FLT4, IC50: 8 nM

 		c-Kit,FLT3 99%+
ZM 306416 +

VEGFR1, IC50: 0.33 μM

 		Src 99%+
KRN-633 +

VEGFR1, IC50: 170 nM

 		+

VEGFR2, IC50: 160 nM

 		+

VEGFR3, IC50: 125 nM

 		BTK,c-Kit 98%
OSI-930 +++

FLT1, IC50: 8 nM

 		+++

KDR, IC50: 9 nM

 		99%+
Lenvatinib ++

VEGFR1/FLT1, IC50: 22 nM

 		++++

VEGFR2/KDR, IC50: 4.0 nM

 		+++

VEGFR3/FLT4, IC50: 5.2 nM

 		98%
NVP-BAW2881 +

hVEGFR1, IC50: 820 nM

 		+++

mVEGF2, IC50: 165 nM

hVEGFR2, IC50: 9 nM

 		+

hVEGFR3, IC50: 420 nM

 		99%
Cediranib +++

VEGFR1/FLT1, IC50: 5 nM

 		++++

VEGFR2/KDR, IC50: 0.5 nM

 		c-Kit 99%+
Nintedanib ++

VEGFR1, IC50: 34 nM

 		+++

VEGFR2, IC50: 13 nM

 		+++

VEGFR3, IC50: 13 nM

 		FLT3 99+%
BMS-794833 ++

VEGFR2, IC50: 15 nM

 		99%+
SKLB1002 ++

VEGFR2, IC50: 32 nM

 		99%
Cabozantinib S-malate ++++

VEGFR2/KDR, IC50: 0.035 nM

 		99+%
Ki8751 ++++

VEGFR2, IC50: 0.9 nM

 		c-Kit 99%
SU 5402 ++

VEGFR2, IC50: 20 nM

 		98%
Apatinib mesylate ++++

VEGFR2, IC50: 1 nM

 		RET 98+%
Ponatinib ++++

VEGFR2, IC50: 1.5 nM

 		98%
LY2874455 +++

VEGFR2, IC50: 7 nM

 		99%+
ZM323881 HCl ++++

VEGFR2, IC50: <2 nM

 		98%
AZD2932 +++

VEGFR-2, IC50: 8 nM

 		c-Kit 99%
Cabozantinib ++++

VEGFR2/KDR, IC50: 0.035 nM

 		98%
Sorafenib ++

VEGFR2/Flk1, IC50: 90 nM

VEGFR2, IC50: 90 nM

 		99%
CYC-116 ++

VEGFR2, Ki: 44 nM

 		FLT3 99%+
Golvatinib ++

VEGFR2, IC50: 16 nM

 		99%+
Sunitinib +

VEGFR2 , IC50: 80 nM

 		FLT3 98%
RAF265 ++

VEGFR2, EC50: 30 nM

 		99%+
PD173074 99%+
BFH772 ++++

VEGFR2, IC50: 3 nM

 		98%
Semaxinib +

VEGFR2/Flk1, IC50: 1.23 μM

 		98%
Vandetanib ++

VEGFR2, IC50: 40 nM

 		+

VEGFR3, IC50: 110 nM

 		EGFR 99%
SAR131675 ++

VEGFR3, IC50: 23 nM

 		99%+
ENMD-2076 +

VEGFR2/KDR, IC50: 58.2 nM

 		++

VEGFR3/FLT4, IC50: 15.9 nM

 		RET,FLT3 98%
Telatinib +++

VEGFR2, IC50: 6 nM

 		++++

VEGFR3, IC50: 4 nM

 		c-Kit 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。

PD173074 生物活性

靶点

  • VEGFR2

    VEGFR2, IC50:100 nM-200 nM

  • FGFR1

    FGFR1, IC50:~25 nM
描述 Angiogenesis, playing a major role in the progression of human diseases such as diabetic retinopathy, atherosclerosis and cancer, involves the concerted action of a number of polypeptide factors such as VEGF, Ang1 and FGF. PD173074 is a selective dual inhibitor of both FGFR1 and VEGFR2 with IC50 value of 21.5nM (measured by kinase activity) and 100-200nM (measured by VEGFR2 auto-phosphorylation in NIH 3T3 cells), respectively. PD173074 inhibited auto-phosphorylation of FGFR1, induced by aFGF and heparin, of NIH-3T3 cells expressing FGFR1 endogenously in a dose-dependent manner with an IC50 in the range 1–5nM, as well as auto-phosphorylation of overexpressed VEGFR2 stimulated with VEGF (100ng/ml) with an IC50 of 100–200nM. Mice treated daily with PD173074 by intraperitoneal injection per day starting 3 days prior to pellet implantation exhibited inhibition of bFGF-induced neovascularization by 86% at a dose of 1mg/kg, as well as inhibition of VEGF induced neovascularization by 81% at a dose of 2mg/kg[1]. PD173704 can specifically and effectively inhibit multiple FGF-2-mediated responses of both oligodendrocyte progenitors, as well as differentiated oligodendrocytes with complete antagonization on two phenotypic alterations, downregulation of myelin proteins, and their re-entry into the cell cycle[2].
作用机制 PD173074 is an ATP-competitive inhibitor of FGFR1.[1]

PD173074 细胞实验

Cell Line
Concentration Treated Time Description References
MGH-U3 cells 500 nM 2 h Inhibition of FGFR3 activity, leading to decreased MYC protein levels EMBO Mol Med. 2018 Apr;10(4):e8163.
RT112 cells 500 nM 2 h Inhibition of FGFR3 activity, leading to decreased MYC protein levels EMBO Mol Med. 2018 Apr;10(4):e8163.
mouse embryonic stem cells 100 ng/ml prevent differentiation of mouse embryonic stem cells Nature. 2009 Apr 9;458(7239):771-5.
T-Rex/K-ras cells 1 μM 24 h PD173074 suppressed K-rasG12V-induced PD-L1 mRNA expression Redox Biol. 2021 Jan;38:101780.
T-Rex/K-ras cells 1 μM 48 h PD173074 decreased the K-ras-induced expression of PD-L1 protein Redox Biol. 2021 Jan;38:101780.
Human embryonic stem cells (H1 ESC) 0.1 μM 8 days To study the role of PD173074 in the differentiation of human embryonic stem cells into trophoblast cells, the results showed that PD173074, in combination with BMP4 and A83-01, successfully induced trophoblast differentiation. J Infect Dis. 2021 Dec 8;224(Suppl 6):S660-S669.
CJ7 embryonic stem cells 0.1 μM Used for the culture of embryonic stem cells, inhibiting FGFR activity Nat Commun. 2017 Jun 1;8:15664.
Pancreatic stellate cells (PS1 cells) 2 µM 48 h Inhibited nuclear localization of FGFR1 and FGF2, significantly reducing cell proliferation EMBO Mol Med. 2014 Apr;6(4):467-81.
Pancreatic cancer cells (COLO-357 cells) 2 µM 48 h No effect on nuclear localization of FGFR1 was observed EMBO Mol Med. 2014 Apr;6(4):467-81.
Human Lung Fibroblasts (HLFs) 0.1 μM 48 h PD173074 inhibited the regulatory effect of FGF2 on the expression of ACTA2, COL1A1, CTGF, LOX, SPRY2, and ETV4 genes. J Pathol. 2018 Sep;246(1):54-66.
Human Lung Fibroblasts (HLFs) 0.1 μM 48 h PD173074 inhibited the inhibitory effect of FGF2 on TGF β1-induced expression of COL1A1, LOX, and ACTA2 genes. J Pathol. 2018 Sep;246(1):54-66.
MCF7 cells 100 nM 24 to 36 h To investigate the effect of PD173074 on FGF2-induced signaling in MCF7 cells. Cancer Res. 2010 Jun 15;70(12):4868-79.

PD173074 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice MMTV-iFGFR1 mouse model Intraperitoneal injection 1 mg/kg Every 3 days To investigate the effect of PD173074 on iFGFR1 signaling and its role in mammary tumorigenesis. Cancer Res. 2010 Jun 15;70(12):4868-79.
Mice Prx1Cre;Fgfr3Y367C/+ mouse model Intraperitoneal injection 10 mg/kg Once daily, starting on the day of fracture and continuing until day 7 and 14 post-fracture PD173074 treatment increased cartilage and hypertrophic cartilage volumes in the fracture callus of mutant mice, but did not stimulate cartilage-to-bone transition and did not affect callus and bone volumes. Stem Cell Reports. 2020 Oct 13;15(4):955-967
C57BL/6 mice Pancreatic cancer model Oral 20 mg/kg Once daily for 2 days PD173074 significantly reduced the levels of phosphorylated Akt and PD-L1 protein expression in vivo Redox Biol. 2021 Jan;38:101780.
Mice Tsc1 −/− mice Intraperitoneal injection 20 mg/kg Daily for four days Inhibited Akt and MAPK activities Gastroenterology. 2013 May;144(5):1055-65
Nude mice MGH-U3 and RT112 xenograft models Oral 25 mg/kg Daily for 9 days Inhibition of FGFR3 activity, delayed tumor growth, and decreased expression of both MYC and FGFR3 EMBO Mol Med. 2018 Apr;10(4):e8163.

PD173074 动物研究

Dose Nude Mice[3]: 12 mg/kg Mice: 1 mg/kg, 2 mg/kg[1] (i.p.), 25 mg/kg - 100 mg/kg[4] (p.o.)
Administration i.p., p.o.

PD173074 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.91mL

0.38mL

0.19mL

9.55mL

1.91mL

0.95mL

19.10mL

3.82mL

1.91mL

PD173074 技术信息

CAS号219580-11-7
分子式C28H41N7O3
分子量 523.67
SMILES Code O=C(NC1=NC2=NC(NCCCCN(CC)CC)=NC=C2C=C1C3=CC(OC)=CC(OC)=C3)NC(C)(C)C
MDL No. MFCD08705327
别名
运输蓝冰
InChI Key DXCUKNQANPLTEJ-UHFFFAOYSA-N
Pubchem ID 1401
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

DMSO: 105 mg/mL(200.51 mM)，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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 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
方案 二
方案 三

Tags: PD173074 | 219580-11-7 | PD 173074 | PD-173074 | FGFR1 Inhibitor | Protein Tyrosine Kinase/RTK | Apoptosis | FGFR | VEGFR | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | PD173074 纯度/质量文件 | PD173074 亚型比较 | PD173074 生物活性 | PD173074 动物研究 | PD173074 实验方案 | PD173074 技术信息

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