ChemicalBook > CAS DataBase List > MAZ51

MAZ51

Product Name
MAZ51
CAS No.
163655-37-6
Chemical Name
MAZ51
Synonyms
MAZ51;CS-2885;MAZ51;MAZ-51;MAZ 51;VEGFR3 Kinase Inhibitor, MAZ;3-((4-(Dimethylamino)naphthalen-1-yl)methylene)indolin-2-one;3-(4-DIMETHYLAMINO-NAPHTHALEN-1-YLMETHYLENE)-1,3-DIHYDRO-INDOL-2-ONE;(3E)-3-[[4-(dimethylamino)naphthalen-1-yl]methylidene]-1H-indol-2-one;(3E)-3-{[4-(Dimethylamino)-1-naphthyl]methylene}-1,3-dihydro-2H-indol-2-one;2H-Indol-2-one, 3-[[4-(dimethylamino)-1-naphthalenyl]methylene]-1,3-dihydro-;EGFR,Apoptosis,growth,phosphorylation,Inhibitor,inhibit,PDGFRβ,MAZ51,MAZ 51,tumor,VEGF-D,indolinone,VEGFR,IGF-1R,VEGF-C,Vascular endothelial growth factor receptor,ligand-induced,MAZ-51,proliferation
CBNumber
CB5393484
Molecular Formula
C21H18N2O
Formula Weight
314.38
MOL File
163655-37-6.mol
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MAZ51 Property

storage temp. 
2-8°C
solubility 
DMSO: 11 mg/mL
form 
solid
color 
orange
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Safety

Hazard Codes 
Xn,N
Risk Statements 
22-37/38-41-51/53
Safety Statements 
26-39-61
RIDADR 
UN 3077 9/PG 3
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
676492
Product name
VEGFR3 Kinase Inhibitor, MAZ51 - CAS 163655-37-6 - Calbiochem
Packaging
10MG
Price
$201
Updated
2024/03/01
Cayman Chemical
Product number
16168
Product name
MAZ51
Purity
≥95%
Packaging
1mg
Price
$49
Updated
2024/03/01
Cayman Chemical
Product number
16168
Product name
MAZ51
Purity
≥95%
Packaging
5mg
Price
$120
Updated
2024/03/01
Cayman Chemical
Product number
16168
Product name
MAZ51
Purity
≥95%
Packaging
10mg
Price
$190
Updated
2024/03/01
Cayman Chemical
Product number
16168
Product name
MAZ51
Purity
≥95%
Packaging
25mg
Price
$416
Updated
2024/03/01
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MAZ51 Chemical Properties,Usage,Production

Description

The VEGF receptors (VEGFRs) mediate signaling leading to angiogenesis, with VEGFR3 (FLT4), activated by VEGF isoforms VEGFC and VEGFD, primarily expressed on lymphatic endothelial cells and directing lymphangiogenesis. MAZ51 is an indolinone that selectively antagonizes the activation of VEGFR3 by VEGFC (IC50 = 1 μM) without blocking VEGFC-mediated stimulation of VEGFR2. It does not inhibit ligand-induced autophosphorylation of EGFR, IGF-1R, or PDGFRβ. By preventing VEGFR3 activation, MAZ51 interferes with an autocrine loop involving the induced expression of the ligand VEGFC as well as VEGFA. It reduces proliferation and induces apoptosis in a variety of cancer cells in vitro and suppresses tumor growth in vivo. MAZ51 is used to study the role of VEGFR3 in endothelial and cancer cell function and survival.

Uses

MAZ51 is an indolinone compound that selectively antagonizes the activation of VEGFR-3 by VEGF-C without blocking VEGF-C mediated stumulation of VEGFR-2. This reduces proliferation and induces apoptosis in various cancer cells and suppresses tumor growth.

in vitro

maz51 caused dramatic shape changes, including the retraction of cellular protrusions and cell rounding in the rat c6 and human u251mg glioma cell lines. maz51 also inhibited cellular proliferation by inducing g2/m phase cell cycle arrest without triggering significant cell death in dose- and time-dependent patterns. treatment of glioma cells with maz51 increased phosphorylated gsk3β levels by activating akt and increasing levels of active rhoa. treatment with maz51 in vegfr-3-silenced cells caused the alterations of cell shape and cytoskeletal arrangements [1]. maz51 surprisingly blocked proliferation of human dermal microvascular endothelial cells (hdmec) with an ic50 of < 1 μm [2].

in vivo

in the rats subcutaneously injected with mt450 rat mammary carcinoma cells, treatment daily with maz51 (8 mg/kg, i.p.) significantly suppressed the growth of mt450 tumors when compared with the solvent-treated animals [2]. in the mammary fat pad of balb/c mice injected with the metastatic mammary tumor cell line cl66, maz51 treatment (i.p.) significantly inhibited tumor growth in a dose-dependent manner [3].

References

[1]. park j h, shin y j, riew t r, et al. the indolinone maz51 induces cell rounding and g2/m cell cycle arrest in glioma cells without the inhibition of vegfr-3 phosphorylation: involvement of the rhoa and akt/gsk3β signaling pathways[j]. plos one, 2014, 9(9): e109055.
[2]. kirkin v, thiele w, baumann p, et al. maz51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo[j]. international journal of cancer, 2004, 112(6): 986-993.
[3]. michelle l. varney, anguraj sadanandam, joyce c. solheim, james e. talmadge and rakesh k. singh experimental and molecular therapeutics 28: antibodies and therapeutic targets vegfr3 antagonist (maz51) directly and indirectly inhibits murine mammary tumor growth and metastasis.

MAZ51 Preparation Products And Raw materials

Raw materials

Preparation Products

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MAZ51 Suppliers

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163655-37-6, MAZ51Related Search:

VEGF Receptor 3 Kinase Inhibitor, MAZ51 MAZ51 1-STYRYLNAPHTHALENE SU 4312

  • (3E)-3-{[4-(Dimethylamino)-1-naphthyl]methylene}-1,3-dihydro-2H-indol-2-one
  • (3E)-3-[[4-(dimethylamino)naphthalen-1-yl]methylidene]-1H-indol-2-one
  • MAZ51
  • 3-(4-DIMETHYLAMINO-NAPHTHALEN-1-YLMETHYLENE)-1,3-DIHYDRO-INDOL-2-ONE
  • CS-2885
  • MAZ51;MAZ-51;MAZ 51
  • 2H-Indol-2-one, 3-[[4-(dimethylamino)-1-naphthalenyl]methylene]-1,3-dihydro-
  • VEGFR3 Kinase Inhibitor, MAZ
  • 3-((4-(Dimethylamino)naphthalen-1-yl)methylene)indolin-2-one
  • EGFR,Apoptosis,growth,phosphorylation,Inhibitor,inhibit,PDGFRβ,MAZ51,MAZ 51,tumor,VEGF-D,indolinone,VEGFR,IGF-1R,VEGF-C,Vascular endothelial growth factor receptor,ligand-induced,MAZ-51,proliferation
  • 163655-37-6
  • C21H18N2O
  • BioChemical
  • Cell Signaling and Neuroscience
  • Cell Biology
  • Vascular Endothelial Growth Factor (VEGF)
  • Receptor Tyrosine Kinase Inhibitors
  • Kinase/Phosphatase Biology