HDAC-IN-57 

HDAC-IN-57 is an orally active inhibitor of histone deacetylases (HDAC), with IC₅₀s of 2.07 nM, 4.71 nM, 2.4 nM and 107 nM for HDAC1, HDAC2, HDAC6, HDAC8, respectively. HDAC-IN-57 can inhibits LSD1, with IC₅₀ of 1.34 μΜ. HDAC-IN-57 induces apoptosis, and has anti-tumor activity^[1].

HDAC-IN-57 (Compound 5e) (1.0 μM，2.5 μM，5.0 μΜ； 48 小时) 抑制实体肿瘤细胞系 MGC-803，A549，HCT-116 的迁移和侵袭^[1]。
HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 显著抑制实体肿瘤细胞系 MGC-803，A549，HCT-116 的生长，IC₅₀s 值分别为 0.45 μM, 1.48 μM 和 0.57 μM^[1]。
HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 以剂量依赖性方式触发 MGC-803 和 HCT-116 细胞凋亡^[1]。
HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 抑制 MGC-803 和 HCT-116 细胞系内 LSD1 和 HDACs^[1]。
HDAC-IN-57 (1.0 μM，2.5 μM，5.0 μΜ；48小时) 诱导 MGC-803 和 HCT-116 细胞周期 G2/M 期阻滞^[1]。
HDAC-IN-57 在体外代谢稳定性高。在人肝脏 (HLM) 和大鼠肝脏微粒体 (RLM) 中孵育1 小时后分别保持母体化合物的 86.1% 和 87.4%，T_1/2超过 120 分钟^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

HDAC-IN-57 (Compound 5e) (静脉注射1 mg/kg，口服10 mg/kg) 显示 T_1/2 为 0.37 小时 (静脉注射) 和 2.75 小时 (口服) ，口服生物利用度 (F%) 为 10.6%^[1]。
HDAC-IN-57 (25 或 50 mg/kg灌胃；每天 1 次，连续 21 天) 在 NOD-SCID 小鼠 MGC-803 异种移植模型中实现了剂量依赖性肿瘤生长抑制^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	MGC-803 xenograft model in NOD-SCID mice[1]
Dosage:	25 or 50 mg/ kg
Administration:	Oral gavage (p.o.);
Result:	Achieved a dose-dependent tumor growth inhibition (TGI) of 44.8% at 25 mg/kg and 71.5% at 50 mg/kg.

Animal Model:	Male SD rats (Pharmacokinetic assay)[1]
Dosage:	1 mg/kg; 10 mg/kg
Administration:	Intravenous injection (i.v.); Oral gavage (p.o.)
Result:	Pharmacokinetic parameters for HDAC-IN-57 (Compound 5e) in SD rats[1] Route Dose (mg/kg) T1/2 (h) Tmax (h) CL (mL•min-1/kg-1) AUC0-t (h•ng/mL) AUC0-Ꝏ (h•ng/mL) Cmax (ng/mL) VZ (L/kg) F (%) i.v. 1 0.37 / 1.61 644.1 645.8 1892.8 0.82 / p.o. 10 2.75 0.25 / 685.2 766.2 716.4 52.2 10.6
分子量	377.39
Formula	C21H19N3O4
CAS 号	2716217-79-5
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.
纯度 & 产品资料	Data Sheet (548 KB) 产品使用指南 (1538 KB)
参考文献	[1]. Duan Y, et al. Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors. Eur J Med Chem. 2023 Jun 5;254:115367.  [Content Brief]

• [1]. Duan Y, et al. Discovery of novel, potent, and orally bioavailable HDACs inhibitors with LSD1 inhibitory activity for the treatment of solid tumors. Eur J Med Chem. 2023 Jun 5;254:115367.

HDAC-IN-57 相关分类

• Cancer
• 肿瘤靶向治疗 肿瘤代谢与转移

• Cell Cycle/DNA Damage Epigenetics Apoptosis
• HDAC Apoptosis Histone Demethylase

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量		浓度		体积		分子量 *
kg g mg μg ng pg	=	M mM μM nM pM	×	L mL μL	×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 (start)	×	体积 (start)	=	浓度 (final)	×	体积 (final)
M mM μM nM pM	×	L mL μL	=	M mM μM nM pM	×	L mL μL
C1		V1		C2		V2

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Keywords:

HDAC-IN-572716217-79-5HDACApoptosisHistone DemethylaseHistone deacetylasesHDAC1 inhibitoranti-tumorMGC-803HCT-116xenograft modelsInhibitorinhibitorinhibit

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