| Identification | Back 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 Properties | Back 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 Information | Back 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.
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| [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 |
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