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AB141117

PD 173074, FGFR1 and FGFR3 inhibitor

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(2 Publications)

MW 523.7 Da, Purity >99%. Potent, ATP-competitive fibroblast growth factor receptor 1 (FGFR1) and FGFR3 inhibitor (IC50 values are 21.5 and 5 nM respectively). Shows little activity at EGFR, InsR, MEK and cPKC. Effectively inhibits angiogenesis in vivo. Also impairs tumor growth and inhibits self-renewal of stem cells.
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Functional Studies - PD 173074, FGFR1 and FGFR3 inhibitor (AB141117)
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Functional Studies - PD 173074, FGFR1 and FGFR3 inhibitor (AB141117)

BT549 cells were incubated at 37°C for 1 hour with vehicle control (0 μM) and different concentrations of PD 173074 (ab141117) in DMSO. Decreased expression of RSK1 p90 (phospho T359 + S363) ab32413 correlates with an increase in PD 173074 concentration, as described in literature.

Whole cell lysates were prepared with RIPA buffer (containing protease inhibitors and sodium orthovanadate), 10 μg of each were loaded on the gel and the WB was run under reducing conditions. After transfer the membrane was blocked for an hour using 5% BSA before being incubated with ab32413 at 1/5000 dilution and ab8227 at 1 μg/ml overnight at 4°C. Antibody binding was detected using an anti-rabbit antibody conjugated to HRP ab97051 at 1/10000 dilution and visualised using ECL development solution.

Chemical Structure - PD 173074, FGFR1 and FGFR3 inhibitor (AB141117)
  • Chemical Structure

Lab

Chemical Structure - PD 173074, FGFR1 and FGFR3 inhibitor (AB141117)

2D chemical structure image of ab141117, PD 173074, FGFR1 and FGFR3 inhibitor

Key facts

CAS number

219580-11-7

Purity

>99%

Form

Solid

form

Molecular weight

523.7 Da

Molecular formula

C<sub>2</sub><sub>8</sub>H<sub>4</sub><sub>1</sub>N<sub>7</sub>O<sub>3</sub>

PubChem

1401

Nature

Synthetic

Solubility

Soluble in DMSO to 100 mM

Soluble in ethanol to 100 mM

Biochemical name

1-(tert-Butyl)-3-(2-((4-(diethylamino)butyl)amino)-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)urea

Biological description

Potent, ATP-competitive fibroblast growth factor receptor 1 (FGFR1) and FGFR3 inhibitor (IC50 values are 21.5 and 5 nM respectively). Shows little activity at EGFR, InsR, MEK and cPKC. Effectively inhibits angiogenesis in vivo. Also impairs tumor growth and inhibits self-renewal of stem cells.

Canonical smiles

CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C

InChi

InChI=1S/C28H41N7O3/c1-8-35(9-2)13-11-10-12-29-26-30-18-20-16-23(19-14-21(37-6)17-22(15-19)38-7)25(31-24(20)32-26)33-27(36)34-28(3,4)5/h14-18H,8-13H2,1-7H3,(H3,29,30,31,32,33,34,36)

InChiKey

DXCUKNQANPLTEJ-UHFFFAOYSA-N

IUPAC Name

1-tert-butyl-3-[2-[4-(diethylamino)butylamino]-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]urea

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Complementary Products

Secondary Antibodies

AB150077

Goat Anti-Rabbit IgG H&L (Alexa Fluor® 488)

Immunocytochemistry/ Immunofluorescence - Goat Anti-Rabbit IgG H&L (Alexa Fluor® 488) (AB150077)

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Biochemicals

AB120892

Anacardic acid, Histone acetyltransferase (HAT) inhibitor

Chemical Structure - Anacardic acid, Histone acetyltransferase (HAT) inhibitor (AB120892)

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Primary Antibodies

AB133273

Anti-Androgen Receptor antibody [EPR1535(2)]

BOND RX™ Validated|RabMAb|Recombinant|Lab Essentials

Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded sections) - Anti-Androgen Receptor antibody [EPR1535(2)] (AB133273)

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Primary Antibodies

AB283818

Anti-IL-1 beta antibody [RM1009]

BOND RX™ Validated|KO Validated|RabMAb|Recombinant|Lab Essentials|20ul selling size

Immunocytochemistry - Anti-IL-1 beta antibody [RM1009] (AB283818)

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
The product can be stored for up to 12 months
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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

Interferon beta Src Glucocorticoid Receptor CSK Estrogen Receptor VEGF Receptor 2 VEGF Receptor 1 Gli3 Androgen Receptor FGFR1 FGFR2 FGFR4 FGFR3 Yes1 and IDH1 represent proteins and receptors playing different mechanical roles. For instance FGFR1 known as Fibroblast Growth Factor Receptor 1 involves signaling pathways controlling cell division and differentiation; it possesses a mass of approximately 115 kDa. FGFR3 another receptor with similar functions is known for its variants like FGFR3 inhibitors impacting certain pathways. These proteins usually express across various tissues playing roles in development and maintenance.
Biological function summary

These targets and proteins serve roles in signal transduction and cellular response. They are part of complexes that help the body react to external signals. For example VEGF Receptors 1 and 2 contribute to angiogenesis and vascular maintenance. FGFR3 interacts with inhibitors influencing bone development and maintenance. Androgen and Estrogen Receptors modulate gene expression in response to hormonal signals affecting diverse physiological processes.

Pathways

Many of these proteins like Src and Yes1 integrate into significant signaling pathways. The MAPK and PI3K/AKT pathways involve multiple targets such as FGFR1 and Glucocorticoid Receptor contributing to cell growth and survival regulation. These pathways often interact with other proteins for coordinated cellular responses allowing complex regulation of different cellular functions.

These proteins connect to certain pathologies through their involvement in critical pathways. For instance FGFR3 and its inhibitors relate to skeletal disorders like achondroplasia. Estrogen Receptor's interaction can link to breast cancer development often alongside Androgen Receptors influencing hormone-driven tumorous growths. Understanding their roles helps in developing targeted therapies for these conditions.
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Product protocols

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Publications (2)

Recent publications for all applications. Explore the full list and refine your search

International journal of molecular sciences 22: PubMed33396256

2020

Global Genome Conformational Programming during Neuronal Development Is Associated with CTCF and Nuclear FGFR1-The Genome Archipelago Model.

Applications

Unspecified application

Species

Unspecified reactive species

Brandon Decker,Michal Liput,Hussam Abdellatif,Donald Yergeau,Yongho Bae,Josep M Jornet,Ewa K Stachowiak,Michal K Stachowiak

Frontiers in immunology 8:1852 PubMed29312335

2017

The G-Protein-Coupled Chemoattractant Receptor Fpr2 Exacerbates High Glucose-Mediated Proinflammatory Responses of Müller Glial Cells.

Applications

Unspecified application

Species

Unspecified reactive species

Ying Yu,Zhiyao Bao,Xiaofei Wang,Wanghua Gong,Hui Chen,Huaijin Guan,Yingying Le,Shaobo Su,Keqiang Chen,Ji Ming Wang
View all publications
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