Product Data?SheetRomidepsinCat. No.:CAS No.:分?式:分?量:作?靶点:作?通路:储存?式:HY-15149128517-07-7C??H??N?O?S?540.7HDAC; ApoptosisCell Cycle/DNA Damage; Epigenetics; ApoptosisPowder-20°C3 yearsInhibitors?Agonists?Screening Libraries* 该产品在溶液状态不稳定，建议您现?现配，即刻使?。溶解性数据体外实验DMSO : 50 mg/mL (92.47 mM; Need ultrasonic)Mass1 mg5 mg10 mgSolventConcentration制备储备液1 mM5 mM10 mM1.8495 mL0.3699 mL0.1849 mL9.2473 mL1.8495 mL0.9247 mL18.4945 mL3.6989 mL1.8495 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现?现配， 即刻使?.体内实验请根据您的实验动物和给药?式选择适当的溶解?案。以下溶解?案都请先按照 In Vitro ?式配制澄清的储备液，再依次添加助溶剂： 为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的?作液，建议您现?现配，当天使?； 以下溶剂前显?的百分?是指该溶剂在您配制终溶液中的体积占?；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的?式助溶1. 请依序添加每种溶剂：?10% DMSO ?? 40% PEG300 ?? 5% Tween-80 ?? 45% salineSolubility: ≥ 2.08 mg/mL (3.85 mM); Clear solution此?案可获得 ≥ 2.08 mg/mL (3.85 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加? 50 μL Tween-80，混合均匀；然后继续加? 450 μL ?理盐?定容? 1 mL。2. 请依序添加每种溶剂：?10% DMSO ?? 90% (20% SBE-β-CD in saline)Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (4.62 mM，饱和度未知) 的澄清溶液。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD ?理盐??溶液中，混合均匀。3. 请依序添加每种溶剂：?10% DMSO ?? 90% corn oilPage 1 of 2 www.MedChemExpress.cn
Solubility: ≥ 2.5 mg/mL (4.62 mM); Clear solution此?案可获得 ≥ 2.5 mg/mL (4.62 mM，饱和度未知) 的澄清溶液，此?案不适?于实验周期在半个?以上的实验。 以 1 mL ?作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL ??油中，混合均匀。BIOLOGICAL ACTIVITY?物活性Romidepsin (FK 228) 是具有抗肿瘤活性的组蛋?去?酰化酶 (HDAC) 抑制剂，抑制 HDAC1，HDAC2，HDAC4 和 HDAC6，IC50 值分别为 36 nM，47 nM，510 nM 和 1.4 μM。Romidepsin (FK 228) 由紫?杆菌产?，诱导 G2/M 细胞周期阻滞和凋亡 (apoptosis)。IC?? & TargetHDAC136 nM (IC50)体外研究HDAC247 nM (IC50)HDAC4510 nM (IC50)HDAC614000 nM (IC50)Romidepsin (0-72 hours; 0-80 nM) inhibits proliferation of HCC cells in dose-dependent manner[2]. Romidepsin (0-48 hours; 0-60 nM) leads to a time- and dose-dependent induction of cell cycle arrest in the G2/M phase in HCC cells[2]. Romidepsin (0-48 hours; 0-60 nM) promotesapoptosis in HCC cells, increases c-caspase-3, c-caspase-9, and c-PARP protein expression[2]. Cell Proliferation Assay[2]Cell Line:Concentration:Incubation Time:Result:Cell Cycle Analysis[2]Cell Line:Concentration:Incubation Time:Result:Western Blot Analysis[2]Cell Line:Concentration:Incubation Time:Result:HCC cells0 nM; 15 nM; 30 nM; 60 nM12 hours;24 hours; 48 hoursIncreaesd c-caspase-3, c-caspase-9, and c-PARP expression in HCC cells.HCC cells0 nM; 15 nM; 30 nM; 60 nM12 hours;24 hours; 48 hoursCaused a G2/M arrest.HCC cells0 nM; 10 nM; 20 nM; 30 nM; 40 nM; 50 nM; 60 nM; 70 nM; 80 nM0 hours; 12 hours; 24 hours; 48 hours; 72 hoursInhibited HCC cells proliferation.体内研究Romidepsin (intraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 days) inhibited the tumor growth, reveals a higher expression of p-cdc25C, ki67, c-caspase-3 and c-PARP, and a lower expression of Ki-67 in Romidepsin treated tumors [2].Page 2 of 3 www.MedChemExpress.cn
Animal Model:Dosage:Administration:Result:Nude mice with Huh7 cells[2]0.5 and 1 mg/kgIntraperitoneal injection; 0.5 and 1 mg/kg; every 3 day; 21 daysSuppressed tumor growth in mouse xenograft models.客户使?本产品发表的科研?献????Cancer Res. 2016 Dec 1;76(23):7001-7011.????PLoS Pathog.?2018 Sep 13;14(9):e1007267.?????Cancers (Basel).?2019 Sep 7;11(9). pii: E1327.????J Med Chem. 2015 Nov 12;58(21):8638-46.????ACS Med Chem Lett. 2018 Feb 6;9(3):268-273.See more customer validations on www.MedChemExpress.cnREFERENCES[1].?Furumai R, et al. FK228 (depsipeptide) as a natural prodrug that inhibits class I histone deacetylases. Cancer Res. 2002 Sep 1;62(17):4916-21.[2].?Sun WJ, et al. Romidepsin induces G2/M phase arrest via Erk/cdc25C/cdc2/cyclinB pathway and apoptosis induction through JNK/c-Jun/caspase3 pathway in hepatocellular carcinoma cells. Biochem Pharmacol. 2017 Mar 1;127:90-100.McePdfHeightCaution: Product has not been fully validated for medical applications. For research use only.
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