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NAV-2729

品牌
Sigma-Aldrich
CAS
419547-11-8
货号
SML2238
规格纯度
≥98% (HPLC)
参考价格
1023.96 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
-+
产品名称:
419547-11-8
NAV-2729
NAV 2729
3-(4-Chlorophenyl)-5-(4-nitrophenyl)-2-(phenylmethyl)-pyrazolo[1,5-a]pyrimidin-7(4H)-one
NAV2729
产品介绍:

产品说明

生化/生理作用

Originally characterized as a non-nucleotide-competitive and reversible ARF6-selective inhibitor (IC50 = 1.4 μM without GEF and 2.4 μM with 100 nM ARNO or BRAG2/GEP100) that targets ARF6 GEF-binding region, NAV-2729 prevents GEF-dependent ARF1 & ARF6 activity (% inhibition of BRAG2Sec7PH-stimulated GTPase activity/[NAV-2729] = 50% Δ17Arf1/10 μM and 15% Δ13Arf6/25 μM) with higher potency against BRAG2- than ARNO-dependent ARF1 activity (64% vs. 20% Δ17Arf1 inhibition at 25 μM in the presence of respective GEF sec7 domain). NAV-2729 treatment effectively inhibits G-alpha-q downstream signaling pathways and anchorage-independent colony growth of Mel92.1 & Mel202 melanoma cells in vitro (10 μM) as well as uveal melanoma tumor establishment in Mel202 xenograft mice in vivo (30 mg/kg/day i.p.).
NAV-2729 (IC50 of 1.5 μM) has a therapeutic benefit in reducing the adverse effect of diabetic retinopathy in animal models.

基本信息

经验(实验)分子式C25H17ClN4O3
分子量456.88
MDL编号MFCD01455625
NACRESNA.77

产品性质

测定≥98% (HPLC)
形式powder
颜色 white to beige
溶解性DMSO: 2 mg/mL, clear
储存温度2-8℃
SMILES stringO=C1C=C(C2=CC=C([N+]([O-])=O)C=C2)NC3=C(C4=CC=C(Cl)C=C4)C(CC5=CC=CC=C5)=NN31

安全信息

储存分类代码13 - Non Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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