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MW 264.32 Da, Purity >98%. Potent, selective VEGFR and PDGFR tyrosine kinases inhibitor (IC50 values are 0.8 and 19.4 μM respectively). Shows anti-angiogenic effects. Active in vivo.

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Images

Chemical Structure - SU4312, VEGFR and PDGFR receptor tyrosine kinase inhibitor (AB141577), expandable thumbnail

Publications

Key facts

CAS number

5812-07-7

Purity

> 98%

Form

Solid

Molecular weight

264.32 Da

Molecular formula

C17H16N2O

PubChem identifier

6450842

Nature

Synthetic

Alternative names

Recommended products

MW 264.32 Da, Purity >98%. Potent, selective VEGFR and PDGFR tyrosine kinases inhibitor (IC50 values are 0.8 and 19.4 μM respectively). Shows anti-angiogenic effects. Active in vivo.

Key facts

Purity

> 98%

PubChem identifier

6450842

Solubility

Soluble in DMSO to 75 mM.

Biochemical name

3-(4-(Dimethylamino)benzylidene)-1,3-dihydro-2H-indol-2-one

Biological description

Potent, selective VEGFR and PDGFR tyrosine kinases inhibitor (IC50 values are 0.8 and 19.4 μM respectively). Shows anti-angiogenic effects. Active in vivo.

Canonical SMILES

CN(C)C1=CC=C(C=C1)C=C2C3=CC=CC=C3NC2=O

Isomeric SMILES

CN(C)C1=CC=C(C=C1)/C=C\2/C3=CC=CC=C3NC2=O

InChI

InChI=1S/C17H16N2O/c1-19(2)13-9-7-12(8-10-13)11-15-14-5-3-4-6-16(14)18-17(15)20/h3-11H,1-2H3,(H,18,20)/b15-11-

InChIKey

UAKWLVYMKBWHMX-PTNGSMBKSA-N

IUPAC name

(3Z)-3-[[4-(dimethylamino)phenyl]methylidene]-1H-indol-2-one

Storage

Shipped at conditions

Ambient - Can Ship with Ice

Appropriate short-term storage conditions

-20°C

Appropriate long-term storage conditions

-20°C

Storage information

Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary info

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

Activity summary

Amyloid Precursor Protein (APP) Tau and Alpha-synuclein are proteins with significant roles in neurological diseases. APP is a membrane protein that is cleaved to create amyloid-beta linked with Alzheimer's disease. Its mass is around 100-140 kDa depending on isoform. APP is mainly expressed in the brain in neurons. Tau protein another key player helps stabilize microtubules and has a mass of about 50-65 kDa. It is found widely in the central nervous system. Alpha-synuclein also prevalent in the brain especially in presynaptic terminals is involved in numerous synaptic functions. The VEGF Receptor 1 also known as FLT1 mainly modulates angiogenesis expressed in vascular endothelial cells. The NPR-A or guanylyl cyclase-A receptor binds natriuretic peptides and facilitates vascular and renal homeostasis. Niemann-Pick C1 protein (NPC1) is found in late endosomes and lysosomes and it regulates cholesterol trafficking in cells.

Biological function summary

APP processes give rise to amyloid-beta impacting neural network activities and contributing to plaque formation in Alzheimer’s disease. Tau protein often binding with tubulin assists in microtubule assembly but also shows aggregation in neurodegenerative conditions. Alpha-synuclein's role in synaptic vesicle regulation hints at neurotransmitter release involvement. VEGF Receptor 1 supports blood vessel growth and maintenance forming complexes with other kinases linked receptors like PDGF receptors. NPR-A mediates natriuresis and blood pressure regulation while cooperatively functioning with complex signaling pathways. NPC1 maintains cellular lipid sorting and cholesterol homeostasis contributing to the prevention of lipid build-up in lysosomes.

Pathways

APP and its generated amyloid-beta partake in synaptic functions and APP processing pathways interacting with proteins like presenilin and BACE1 in Alzheimer's disease pathways. Tau participates in the MAPK/ERK pathway important for neuronal health where hyperphosphorylation affects its role in cell stability. Alpha-synuclein is integral in dopaminergic pathways often associating with PARK7 in Parkinson's disease. VEGF Receptor 1 is actively involved in angiogenesis pathways together with kinases linked receptors influencing cellular responses to PDGFR activators. NPR-A regulates the cGMP pathway impacting natriuretic peptide signaling. NPC1 plays a role in lipid transport pathways engaging with proteins regulating cholesterol storage and efflux.

Associated diseases and disorders

Beta-amyloid and Tau are strongly linked to Alzheimer's disease. These proteins through abnormal aggregation contribute significantly to neurodegeneration and cognitive decline. Alpha-synuclein through its misfolded forms remains a central figure in Parkinson's disease pathogenesis promoting dopaminergic neuron loss. VEGF Receptor 1 through endothelial dysfunction associates with cancer progression due to its influence on tumor angiogenesis. NPR-A dysfunctions connect with cardiovascular diseases through disrupted natriuretic peptide signaling. Niemann-Pick C1 malfunction results in Niemann-Pick disease type C where it causes severe lipid accumulation in lysosomes showcasing connections to cholesterol management disorders.

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1 product image

  • Chemical Structure - SU4312, VEGFR and PDGFR receptor tyrosine kinase inhibitor (ab141577), expandable thumbnail

    Chemical Structure - SU4312, VEGFR and PDGFR receptor tyrosine kinase inhibitor (ab141577)

    2D chemical structure image of ab141577, SU4312, VEGFR and PDGFR receptor tyrosine kinase inhibitor

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