Ivaltinostat(Synonyms: CG-200745)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Ivaltinostat (Synonyms: CG-200745)

Ivaltinostat (CG-200745) 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 抑制组蛋白 H3 和微管蛋白的脱乙酰作用。Ivaltinostat 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 可增强 Gemcitabine 耐药细胞对 Gemcitabine (HY-16138) 和 5-Fluorouracil (5-FU; HY-90006) 的敏感性。Ivaltinostat 诱导凋亡并具有抗肿瘤作用。

Ivaltinostat(Synonyms: CG-200745)

Ivaltinostat Chemical Structure

CAS No. : 936221-33-9

规格 价格 是否有货
5 mg ￥9900 询问价格 & 货期
10 mg ￥16000 询问价格 & 货期

* Please select Quantity before adding items.

Ivaltinostat 的其他形式现货产品:

Ivaltinostat formic

生物活性

Ivaltinostat (CG-200745) is an orally active, potent pan-HDAC inhibitor which has the hydroxamic acid moiety to bind zinc at the bottom of catalytic pocket. Ivaltinostat inhibits deacetylation of histone H3 and tubulin. Ivaltinostat induces the accumulation of p53, promotes p53-dependent transactivation, and enhances the expression of MDM2 and p21 (Waf1/Cip1) proteins. Ivaltinostat enhances the sensitivity of Gemcitabine-resistant cells to Gemcitabine (HY-16138) and 5-Fluorouracil (5-FU; HY-90006). Ivaltinostat induces apoptosis and has anti-tumour effects[1][2][3][4].

IC50 & Target[2]

HDAC

 

体外研究
(In Vitro)

Ivaltinostat (CG-200745; 0.01-100 μM; 48 hours) inhibits growth of prostate cancer cells (LNCaP, DU145 and PC3 cells). Ivaltinostat (1, 10 μM; 24, 48 hours) 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) reduces the Calu6 cells proliferation to 40% of untreated cells[4].
Ivaltinostat (3 μM; 1-24 hours) significantly increases Calu6 cells proportion in G2/M phase (69%)[4].
Ivaltinostat (0-10 μM; 1-24 hours) 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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[4]

Cell Line: Calu6 cells
Concentration: 0-10 μM
Incubation Time: 48 hours
Result: Reduced the cell proliferation to 40% of untreated cells.

Cell Cycle Analysis[4]

Cell Line: Calu6 cells
Concentration: 3 μM
Incubation Time: 1, 8, 12, 24 hours
Result: Increased significantly cell proportion in G2/M phase (69%).

Western Blot Analysis[4]

Cell Line: Calu6 cells
Concentration: 0-10 μM
Incubation Time: 1, 4, 8, 12, 24 hours
Result: Increased the acetylation of histone H3 and H4 at various sites in a time-dependent manner.

体内研究
(In Vivo)

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

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male 8-week-old C57BL/6 J mice weighing 20~22 g of unilateral ureteral obstruction (UUO)[5]
Dosage: 30 mg/kg
Administration: PO; daily; for 7 days
Result: Attenuated oxidative stress, inflammatory cytokines and adhesion molecules in UUO kidneys.

Clinical Trial

分子量

427.54

Formula

C24H33N3O4
CAS 号

936221-33-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务