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AB141368

SU-5402, VEGFR and FGFR inhibitor

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(2 Publications)

MW 296.32 Da, Purity >97%. Potent, selective VEGFR and FGFR inhibitor (IC50 values are 0.02 (VEGFR2), 0.03 (FGFR1), 0.51 (PDGFRβ) and >100 μM (EGFR)). Attenuates integrin β4-induced differentiation of neural stem cells. Shows antitumor effects in vivo. .

View Alternative Names

7TM receptor, ACM2_HUMAN, AChR, ASV, AW259666, Acetylcholine receptor, muscarinic, 2, Avian sarcoma virus, BFGFR, Basic fibroblast growth factor receptor 1, C SRC, CA 2, CA-II, CAC, CAH2_HUMAN, CANN6, CB-R, CB1, CB1A, CB1K5, CB1R, CD 140B, CD140A, CD140a antigen, CD140b antigen, CD309, CD309 antigen, CD331, CDNA FLJ14219 fis clone NT2RP3003800 highly similar to Rattus norvegicus tyrosine protein kinase pp60 c src mRNA, CEK, CHRM 2, CM2, CNR, CNR1_HUMAN, Cannabinoid receptor 1, Car 2, Carbonate dehydratase II, Carbonic anhydrase 2, Carbonic anhydrase B, Carbonic anhydrase C, Carbonic anhydrase C, formerly, Carbonic anhydrase II, Carbonic dehydratase, Central cannabinoid receptor, Cholinergic receptor muscarinic 2, Cholinergic receptor, muscarinic 2, cardiac, Cholinergic receptor, muscarinic 2, isoform a, Cholinergic receptor, muscarinic 2a, D(2) dopamine receptor, D2 dopamine receptor, D2DR, D2R, DRD2_HUMAN, Dopamine D2 receptor, Dopamine receptor D2, EC 2.7.10.1, EC 2.7.10.2, Epididymis secretory protein Li 282, FGFBR, FGFR1/PLAG1 fusion, FGFR1_HUMAN, FLG, FLJ43243, FLK-1, FLK1, mouse, homolog of, FLT, FLT-2, FRT, Fetal liver kinase 1, Flt-1, Fms related tyrosine kinase 1, Fms related tyrosine kinase 1 (vascular endothelial growth factor/vascular permeability factor receptor), Fms related tyrosine kinase 1 vascular endothelial growth factor/vascular permeability factor receptor, Fms-like gene, Fms-like tyrosine kinase 1, Fms-like tyrosine kinase 2, HBGFR, HEL-76, HEL-S-282, HH2, HM 2, HRTFDS, KAL2, KRD1, Kdr, Kinase insert domain receptor, Kinase insert domain receptor (a type III receptor tyrosine kinase), Ly73, M2 muscarinic receptor, M2-mAChR, MGC120006, MGC120007, Muscarinic M2 receptor, Muscarinic acetylcholine receptor M2, N-SAM, Neuronal CSRC tyrosine specific protein kinase, Neuronal SRC, Neuronal proto-oncogene tyrosine-protein kinase Src, OGD, OTTHUMP00000016838, OTTHUMP00000174476, OTTHUMP00000174477, OTTHUMP00000214579, Oncogene SRC, PDGF Receptor alpha + beta, PDGF-R-alpha, PDGF-R-beta, PDGFR 2, PDGFRA, PDGFRB, Platelet derived growth factor receptor alpha, Platelet derived growth factor receptor beta, Protein-tyrosine kinase receptor flk-1, Proto-oncogene c-Fgr, Proto-oncogene c-Src, Proto-oncogene tyrosine-protein kinase Src, Protooncogene SRC, Protooncogene SRC Rous sarcoma, SRC Oncogene, SRC proto oncogene non receptor tyrosine kinase, SRC_HUMAN, Soluble VEGF receptor 1 14, Soluble VEGFR1 variant 2, Soluble VEGFR1 variant 21, Tyrosine kinase growth factor receptor, Tyrosine kinase pp60c src, Tyrosine protein kinase SRC 1, Tyrosine-protein kinase FRT, Tyrosine-protein kinase receptor FLT, V src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog (avian), VEGFR, VEGFR-1, VEGFR-2, VGFR1_HUMAN, VGFR2_HUMAN, Vascular endothelial growth factor receptor 1, Vascular endothelial growth factor receptor 2, Vascular endothelial growth factor vascular permeability factor receptor, Vascular permeability factor receptor, Vascular permeability factor receptor 1, bFGF-R-1, chrm2a, epididymis luminal protein 76, fibroblast growth factor receptor 1, fms-related tyrosine kinase 2, heparin-binding growth factor receptor, hydroxyaryl-protein kinase, p60-Src, p60c-src, pp60c-src, soluble VEGFR2, v src avian sarcoma (Schmidt Ruppin A2) viral oncogene homolog, v src sarcoma (Schmidt Ruppin A 2) viral oncogene homolog avian

1 Images
Chemical Structure - SU-5402, VEGFR and FGFR inhibitor (AB141368)
  • Chemical Structure

Lab

Chemical Structure - SU-5402, VEGFR and FGFR inhibitor (AB141368)

2D chemical structure image of ab141368, SU-5402, VEGFR and FGFR inhibitor

Key facts

CAS number

215543-92-3

Purity

>97%

Form

Solid

form

Molecular weight

296.32 Da

Molecular formula

C<sub>1</sub><sub>7</sub>H<sub>1</sub><sub>6</sub>N<sub>2</sub>O<sub>3</sub>

PubChem

5289418

Nature

Synthetic

Biochemical name

3-[(3-(2-Carboxyethyl)-4-methylpyrrol-2-YL)methylene]-2-indolinone

Biological description

Potent, selective VEGFR and FGFR inhibitor (IC50 values are 0.02 (VEGFR2), 0.03 (FGFR1), 0.51 (PDGFRβ) and >100 μM (EGFR)). Attenuates integrin β4-induced differentiation of neural stem cells. Shows antitumor effects in vivo.

Canonical smiles

CC1=CNC(=C1CCC(=O)O)C=C2C3=CC=CC=C3NC2=O

Isomeric smiles

CC1=CNC(=C1CCC(=O)O)/C=C\2/C3=CC=CC=C3NC2=O

InChi

InChI=1S/C17H16N2O3/c1-10-9-18-15(11(10)6-7-16(20)21)8-13-12-4-2-3-5-14(12)19-17(13)22/h2-5,8-9,18H,6-7H2,1H3,(H,19,22)(H,20,21)/b13-8-

InChiKey

JNDVEAXZWJIOKB-JYRVWZFOSA-N

IUPAC Name

3-[4-methyl-2-[(Z)-(2-oxo-1H-indol-3-ylidene)methyl]-1H-pyrrol-3-yl]propanoic acid

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

Supplementary information

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

Src VEGF Receptor 2 VEGF Receptor 1 PDGFR alpha + beta and FGFR1 are protein tyrosine kinases that are important in cell signaling. The Src protein with a molecular mass of around 60 kDa functions as a non-receptor tyrosine kinase. It is expressed in various tissues and is also known as pp60src. The VEGF Receptor 2 also known as KDR or Flk-1 and VEGF Receptor 1 known as Flt-1 are expressed mainly in endothelial cells. PDGFR alpha and beta are receptor tyrosine kinases expressed in mesenchymal cells. FGFR1 or fibroblast growth factor receptor 1 with a mass of around 97 kDa is commonly found in a wide range of cell types including fibroblasts.
Biological function summary

Src being a tyrosine kinase influences cell growth motility and differentiation. Src alongside other kinases forms part of complex signaling networks. VEGF Receptors 1 and 2 play major roles in vasculogenesis and angiogenesis essential for new blood vessel formation. PDGFR alpha and beta participate in developmental processes and cellular differentiation. FGFR1 is involved in cell growth embryonic development and tissue repair. These proteins oftentimes interact through complexes that have cascading effects on cell behavior.

Pathways

Src interacts significantly in the MAPK/ERK and PI3K/AKT pathways both vital for cell cycle and survival. VEGF Receptors 1 and 2 are active in the VEGF signaling pathway important for vascular endothelial cell function. PDGFRs and FGFR1 participate in the same pathways affecting cell growth and angiogenesis. Src also phosphorylates downstream proteins that link it indirectly through such pathways including PLCγ and STATs influencing gene expression.

Src and the discussed receptors contribute to oncogenesis and cardiovascular diseases. Dysregulation and overactivity of Src can lead to cancer cell proliferation in breast and colon cancers. VEGF Receptors have a direct link to tumor angiogenesis found in various cancers. PDGFRs and FGFR1 relate to disorders like chronic myelomonocytic leukemia and skeletal dysplasias. Interaction with related proteins like SHP2 and Ras highlights the relevance of these kinases in disease pathways providing potential therapeutic targets for drug development.

Product protocols

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Publications (2)

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

eLife 12: PubMed37947350

2023

scMultiome analysis identifies embryonic hindbrain progenitors with mixed rhombomere identities.

Applications

Unspecified application

Species

Unspecified reactive species

Yong-Il Kim,Rebecca O'Rourke,Charles G Sagerström

Scientific reports 7:12574 PubMed28974764

2017

Cancer-associated fibroblasts support vascular growth through mechanical force.

Applications

Unspecified application

Species

Unspecified reactive species

Mary Kathryn Sewell-Loftin,Samantha Van Hove Bayer,Elizabeth Crist,Taylor Hughes,Sofia M Joison,Gregory D Longmore,Steven C George
View all publications

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