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Ivaltinostat formic
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Ivaltinostat formic图片
包装与价格：
包装价格(元)
5mg电议
10mg电议

产品介绍
Ivaltinostat (CG-200745) formic 是一种口服有效的泛 HDAC 抑制剂，具有异羟肟酸部分，可在催化袋底部结合锌。Ivaltinostat formic 抑制组蛋白 H3 和微管蛋白的脱乙酰作用。Ivaltinostat formic 诱导 p53 的积累，促进 p53 依赖性反式激活，并增强 MDM2 和 p21 (Waf1/Cip1) 蛋白的表达。Ivaltinostat formic 可增强 Gemcitabine 耐药细胞对 Gemcitabine 和 5-Fluorouracil (5-FU; ) 的敏感性。Ivaltinostat formic 诱导凋亡并具有抗肿瘤作用。$
别名CG-200745 formic
分子式C25H35N3O6
分子量473.56
溶解度Water : 50 mg/mL (105.58 mM; Need ultrasonic)|DMSO : 50 mg/mL (105.58 mM; Need ultrasonic)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Ivaltinostat (CG-200745) formic is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat formic inhibits deacetylation of histone H3 and tubulin. Ivaltinostat formic induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat formic enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine and 5-Fluorouracil (5-FU; ). Ivaltinostat formic induces apoptosis and has anti-tumour effects[1][2][3].

Ivaltinostat (CG-200745; 0.01-100 μM; 48 hours) formic inhibits growth of prostate cancer cells (LNCaP, DU145 and PC3 cells). Ivaltinostat (1, 10 μM; 24, 48 hours) formic increases sub-G1 population, and activates caspase-9, -3 and -8[2].Ivaltinostat (0.001-100 μM; for 72 hours) inhibits proliferation of cholangiocarcinoma cells (IC50s of 0.63, 0.93, and 1.80 μM for SNU-1196, SNU-1196/GR, SNU-308 cells, respectively)[3].Ivaltinostat (0-10 μM; 48 hours) formic reduces the Calu6 cells proliferation to 40% of untreated cells[4].Ivaltinostat (3 μM; 1-24 hours) formic significantly increases Calu6 cells proportion in G2/M phase (69%)[4]. Ivaltinostat (0-10 μM; 1-24 hours) formic treatment with low concentration significantly increases the acetylation of histone H3 and H4 in Calu6 cells at various sites in a time-dependent manner up to 24 hours after treatment[4].

Ivaltinostat (CG-200745; p.o.; 30 mg/kg/day; for 7 days) formic attenuates oxidative stress, inflammatory cytokines, and adhesion molecules in UUO kidneys[5].

[1]. Oh ET, et al. Novel histone deacetylase inhibitor CG200745 induces clonogenic cell death by modulating acetylation of p53 in cancer cells. Invest New Drugs. 2012 Apr;30(2):435-42.
[2]. Hwang JJ, et al. A novel histone deacetylase inhibitor, CG200745, potentiates anticancer effect of docetaxel in prostate cancer via decreasing Mcl-1 and Bcl-XL. Invest New Drugs. 2012 Aug;30(4):1434-42.
[3]. Dawoon E Jung, et al. CG200745, an HDAC inhibitor, induces anti-tumour effects in cholangiocarcinoma cell lines via miRNAs targeting the Hippo pathway. Sci Rep. 2017 Sep 7;7(1):10921.
[4]. Chun SM, et al. Epigenetic modulation with HDAC inhibitor CG200745 induces anti-proliferation in non-small cell lung cancer cells. PLoS One. 2015 Mar 17;10(3):e0119379.
[5]. Choi HS, et al. Histone deacetylase inhibitor, CG200745 attenuates renal fibrosis in obstructive kidney disease. Sci Rep. 2018 Aug 1;8(1):11546.

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