CAS |
112522-64-2 |
Chinese Name |
他地那兰 |
English Name |
Tacedinaline |
Synonyms |
N-acetyldinaline;Duvoglustat;PD-123654 |
Molecular Formula |
C15H15N3O2 |
Molecular Weight |
269.3 |
Solubility |
Soluble in DMSO ≥5mg/mL(Need ultrasonic) |
Purity |
≥98% |
Appearance |
White to off-white Solid |
Storage |
Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC |
EINECS 200-256-5 |
MDL |
MFCD00866266 |
SMILES |
O=C(NC1=C(N)C=CC=C1)C2=CC=C(NC(C)=O)C=C2 |
InChIKey |
VAZAPHZUAVEOMC-UHFFFAOYSA-N |
InChI |
InChI=1S/C15H15N3O2/c1-10(19)17-12-8-6-11(7-9-12)15(20)18-14-5-3-2-4-13(14)16/h2-9H,16H2,1H3,(H,17,19)(H,18,20) |
PubChem CID |
2746 |
Target Point |
HDAC |
Passage |
DNA Damage/DNA Repair;Epigenetics;NF-κB |
Background |
Tacedinaline is a selective type I HDAC inhibitor. |
Biological Activity |
CI-994 (Tacedinaline)是组蛋白脱乙酰酶(HDAC)的抑制剂,抑制重组HDAC 1, 2 and 3的 IC50 值分别为0.9, 0.9, 1.2 μM.[1-4] |
In Vitro |
CI-994(N-乙酰基二氢萘)是一种新型口服化合物,在临床前模型中具有广谱的抗肿瘤活性。作用机制可能涉及抑制组蛋白去乙酰化和细胞周期停滞。 CI-994与常用于非小细胞肺癌细胞系管理的抗肿瘤药联合应用,在CI-994(40μM)和吉西他滨(0.01μM)之间观察到明显的作用协同作用(R = 1.8,R = 1.5))治疗48和72小时[2] .CI-994抑制丝裂原刺激的血液淋巴细胞增殖,IC50值为3μM[4]。 |
In Vivo |
CI-994具有针对8/8实体瘤的活性:胰腺导管腺癌#02(4.7);胰腺癌#03(3.0; 1/6治愈);结肠腺癌#38(1.6);结肠腺癌#51 / A(1.1);乳腺癌#25(1.7);乳腺癌#17 / ADR(0.5);催促成骨肉瘤(4.0);和人前列腺癌LNCaP(1.2)。 CI-994是地那林的乙酰化代谢产物,在体内具有与地那林相同的活性谱。它在时间表比较/毒性试验中也表现相似[3]。 CI-994可以在单次口服给药后1天内对大鼠的淋巴组织产生影响,这种作用通常在7天内可逆[4]。 |
Animal Experiment |
大鼠:为了表征CI-994对淋巴组织的作用,在0(载体对照),10,23和45mg / kg下给予雄性大鼠单次口服剂量并在给药后7天内杀死以评估白血细胞分化,骨髓分化,淋巴组织重量和选择的淋巴组织组织病理学[4]。 |
Data Literature Source |
[1]. Moradei OM,et al. Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. J Med Chem. 2007 Nov 15;50(23):5543-6. [2]. Loprevite M,etal. In vitro study of CI-994,a histone deacetylase inhibitor,in non-small cell lung cancer cell lines. Oncol Res. 2005;15(1):39-48. [3]. LoRusso PM,et al. Preclinical antitumor activity of CI-994. Invest New Drugs. 1996;14(4):349-56. [4]. Graziano MJ,et al. Immunotoxicity of the anticancer drug CI-994 in rats: effects on lymphoid tissue. Arch Toxicol. 1999 Apr-May;73(3):168-74 |
Unit |
Bottle |
Specification |
10mg 50mg |