乙酰地那林作用機制 - Medchemexpress - MCE中國

1、Product Data SheetTacedinalineCat. No.: HY-50934CAS No.: 112522-64-2分式: CHNO分量: 269.3作靶點: HDAC; Apoptosis作通路: Cell Cycle/DNA Damage; Epigenetics; Apoptosis儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 58 mg/mL (215.37 mM)* means soluble, but saturation unknow

2、n.SolventMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 3.7133 mL 18.5667 mL 37.1333 mL5 mM 0.7427 mL 3.7133 mL 7.4267 mL10 mM 0.3713 mL 1.8567 mL 3.7133 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲存時，請在 6 個內(nèi)使，-20C 儲存時，請在 1 個內(nèi)使。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式

3、選擇適當?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實驗結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天 使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.28 mM); Clear solution此案可獲得 2.5 mg/mL (9.28 mM，飽和度未知) 的澄清溶

4、液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。Page 1 of 2 www.MedChemEBIOLOGICAL ACTIVITY物活性 Tacedinaline (N-acetyldinaline) 0.9，0.9，1.2 M。組蛋脫酰酶(HDAC)的抑制劑，抑制重 組 HDAC 1, 2 和 3 的 IC50 值分別為IC & Target HD1 HD2 HD30.9 M (IC50) 0.9 M (IC

5、50) 1.2 M (IC50)體外研究 Tacedinaline (N-acetyldinaline) is a novel oral compound with a wide spectrum of antitumor activity in preclinicalmodels. The mechanism of action may involve inhibition of histone deacetylation and cell cycle arrest. Tacedinaline(N-acetyldinaline) is combined with antineoplastic

6、 agents commonly used in non-small cell lung cancer cell linemanagement, a marked synergism of action (R=1.8, R=1.5) is observed between Tacedinaline (N-acetyldinaline) (40 M) and gemcitabine (0.01 M) at 48 and 72 h of treatment2. Tacedinaline (N-acetyldinaline) inhibits mitogen-stimulated blood lym

7、phocyte proliferation with an IC50 value of 3 M4.體內(nèi)研究 Tacedinaline (CI-994) has activity against 8/8 solid tumors tested: pancreatic ductal adenocarcinoma #02 (4.7);pancreatic adenocarcinoma #03 (3.0; 1/6 cures); colon adenocarcinoma #38 (1.6); colon adenocarcinoma #51/A (1.1);mammary adenocarcinoma

8、 #25 (1.7); mammary adenocarcinoma #17/ADR (0.5); Dunning osteogenic sarcoma (4.0);and the human prostate carcinoma LNCaP (1.2). CI-994 is the acetylated metabolite of dinaline and has the samespectrum of activity in vivo as dinaline. It also behaves similarly in schedule comparison/toxicity trials3

9、. Tacedinaline(CI-994) can effect lymphoid tissue in rats within 1 day of a single oral dose, that effects are generally reversible within7 days4.PROTOCOLAnimal Rats: To characterize the effects of Tacedinaline (CI-994) on lymphoid tissue, male rats are administered single oralAdministration 4 doses

10、 at 0 (vehicle control), 10, 23, and 45 mg/kg and killed up to 7 days after dosing for evaluation of white bloodcell differentials, bone marrow differentials, lymphoid tissue weights, and selected histopathology of lymphoid tissue4.MCE has not independently confirmed the accuracy of these methods. T

11、hey are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 J Mol Med (Berl). 2019 Aug;97(8):1183-1193.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Moradei OM, et al. Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. J Med Chem. 200

12、7 Nov15;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.McePdfHeightPage 2 of 3 www.MedChemECaution: Product has no