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NAV-2729

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Purity:98.83%

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COA HNMR HPLC

NAV-2729

Catalog No. T5142Cas No. 419547-11-8

NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6.

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Pack Size	Price	Availability
2 mg	$38	In Stock
5 mg	$61	In Stock
10 mg	$97	In Stock
25 mg	$215	In Stock
50 mg	$318	In Stock
100 mg	$477	In Stock
500 mg	$987	In Stock
1 mL x 10 mM (in DMSO)	$68	In Stock

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Product Introduction

Bioactivity

Description	NAV-2729 inhibits six ArfGEFs (human ARNO, EFA6, BIG1, and BRAG2 and Legionella and Rickettsia RalF), the strongest effects being against BRAG2, Arf1 and Arf6.
In vitro	NAV-2729(25 μM) inhibits spontaneous nucleotide exchange of Δ13Arf6 by ~15%. NAV-2729 inhibits the activation of Δ13Arf6 by BRAG2Sec7PH by 25%. Δ17Arf1 has no measurable spontaneous nucleotide exchange. Activation of Δ17Arf1 by BRAG2Sec7PH is inhibited by NAV-2729, and the efficiency is markedly higher than that for Arf6 (50%). In a dose-response experiment, nucleotide exchange rates are reduced by 50% by 10 μM NAV-2729 for Δ17Arf1 while 50% inhibition is not achieved even at 25 μM NAV-2729 for Δ13Arf6[1]. NAV-2729 blocks ARNO- and GEP100-mediated guanine nucleotide exchange on Arf6 and spontaneous activation of Arf6 and its activation by cytohesins and BRAG. The treatment of uveal melanoma cells with NAV-2729 interferes with anchorage-independent growth of the cell[1]. NAV-2729 is more effective toward Arf1 than Arf6[1].
In vivo	In orthotopic xenograft mouse model of uveal melanoma, systemic treatment of NAV-2729 interfere with tumorigenesis and tumor growth[2].

Chemical Properties

Molecular Weight	456.88
Formula	C25H17ClN4O3
Cas No.	419547-11-8

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 6.88 mg/mL (15.05 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1888 mL	10.9438 mL	21.8876 mL	109.4379 mL
5 mM	0.4378 mL	2.1888 mL	4.3775 mL	21.8876 mL
10 mM	0.2189 mL	1.0944 mL	2.1888 mL	10.9438 mL

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