详情描述
MAZ51 is a selective inhibitor of VEGFR-3 (Flt-4) tyrosine kinase. MAZ51 inhibits VEGF-C-induced activation of VEGFR-3 without blocking VEGF-C-mediated stimulation of VEGFR2. MAZ51 had no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ. MAZ51 blocks proliferation and induces apoptosis in a wide variety of tumor cells. Antitumor activity.
Product information
CAS Number: 163655-37-6
Molecular Weight: 314.38
Formula: C21H18N2O
Chemical Name: (3E)-3-{[4-(dimethylamino)naphthalen-1-yl]methylidene}-2, 3-dihydro-1H-indol-2-one
Smiles: CN(C)C1=CC=C(/C=C2/C(=O)NC3=CC=CC=C/23)C2=CC=CC=C12
InChiKey: VFCXONOPGCDDBQ-QGOAFFKASA-N
InChi: InChI=1S/C21H18N2O/c1-23(2)20-12-11-14(15-7-3-4-9-17(15)20)13-18-16-8-5-6-10-19(16)22-21(18)24/h3-13H,1-2H3,(H,22,24)/b18-13+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 7.69 mg/mL (24.46 mM; Need ultrasonic)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
MAZ51 (2.5-10 μM; 24 hours) blocks proliferation and induces apoptosis in a wide variety of tumor cells. MAZ51 (0.5-50 μM; 25 minutes) has no effect on ligand-induced autophosphorylation of EGFR, IGF-1R and PDGFRβ in A431 cells, HEK-293 cells, and PAE cells, respectively.
In Vivo:
MAZ51 (8 mg/kg; i.p.; daily for 15 day) significantly suppresses the growth of MT450 tumors.
References:
- Kirkin V, et al. Characterization of indolinones which preferentially inhibit VEGF-C- and VEGF-D-induced activation of VEGFR-3 rather than VEGFR-2. Eur J Biochem. 2001 Nov;268(21):5530-40.
- Kirkin V, et al. MAZ51, an indolinone that inhibits endothelial cell and tumor cell growth in vitro, suppresses tumor growth in vivo. Int J Cancer. 2004 Dec 20;112(6):986-93.
Products are for research use only. Not for human use.