ChemicalBook--->CAS DataBase List--->1637443-98-1

1637443-98-1

1637443-98-1 Structure

1637443-98-1 Structure
IdentificationBack Directory
[Name]

hVEGF-IN-1
[CAS]

1637443-98-1
[Synonyms]

hVEGF-IN-1
hVEGF-IN-1, >98%
hVEGF inhibitor 1
1-Piperazinepropanamide, N-[2-[4-[[4-[2-(diethylamino)ethoxy]phenyl]amino]-2-quinazolinyl]phenyl]-4-methyl-
[Molecular Formula]

C34H43N7O2
[MDL Number]

MFCD31560473
[MOL File]

1637443-98-1.mol
[Molecular Weight]

581.75
Chemical PropertiesBack Directory
[Boiling point ]

710.9±60.0 °C(Predicted)
[density ]

1.188±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[solubility ]

DMSO : 25 mg/mL (42.97 mM);Water : < 0.1 mg/mL (insoluble)
[form ]

Solid
[pka]

14.43±0.70(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Uses]

hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression[1].
[in vivo]

hVEGF-IN-1 (compound 1) (7.5 mg/kg; i.p. once daily for 20 d) inhibits tumor growth in a human breast tumor xenograft[1].

Animal Model:BALB/c female nude mice were implanted MCF-7 cells[1]
Dosage:7.5 mg/kg
Administration:I.p. once daily for 20 days
Result:Reduced the tumor volume to <300 mm3.
Reduced the tumor weight around 60.1% to a final weight of 0.18 g.
Decreased the VEGF-A level in tumor tissue.
[References]

[1] Wang SK, et, al. Discovery of Small Molecules for Repressing Cap-Independent Translation of Human Vascular Endothelial Growth Factor (hVEGF) as Novel Antitumor Agents. J Med Chem. 2017 Jul 13;60(13):5306-5319. DOI:10.1021/acs.jmedchem.6b01444
Spectrum DetailBack Directory
[Spectrum Detail]

hVEGF-IN-1(1637443-98-1)1HNMR
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