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HDAC-IN-57

Name: HDAC-IN-57
Brand: TargetMol
SKU: T77334
Price: 258 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T77334 Copy Product Info

Purity: 98.62%

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HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.

Cas No. 2716217-79-5

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Pack Size	Price	USA Stock	Global Stock
1 mg	$117	In Stock	In Stock
5 mg	$258	In Stock	In Stock
10 mg	Inquiry	In Stock	In Stock
25 mg	Inquiry	In Stock	In Stock
50 mg	Inquiry	Inquiry	Inquiry
100 mg	Inquiry	Inquiry	Inquiry
200 mg	Inquiry	Inquiry	Inquiry

For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:98.62%

Appearance:Solid

Color:Yellow

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4 nM, and 107 nM, respectively. HDAC-IN-57 inhibits LSD1 with an IC50 value of 1.34 μΜ. HDAC-IN-57 has anti-tumor activity and can induce apoptosis.
Targets & IC50	HDAC2:4.71 nM, HDAC8:107 nM, HDAC6:2.4 nM, HDAC1:2.07 nM
In vitro	HDAC-IN-57 (Compound 5e) (1.0 μM, 2.5 μM, 5.0 μM; 48 h) effectively suppresses the migration and invasion of solid tumor cell lines, namely MGC-803, A549, and HCT-116. Furthermore, HDAC-IN-57 demonstrates significant growth inhibition in these solid tumor cell lines, exhibiting IC50 values of 0.45 μM, 1.48 μM, and 0.57 μM, respectively. Additionally, HDAC-IN-57 elicits apoptosis in MGC-803 and HCT-116 cells in a dose-dependent manner. It also exerts inhibitory effects on LSD1 and HDACs within the MGC-803 and HCT-116 cell lines. Moreover, HDAC-IN-57 induces cell cycle arrest in the G2/M phase for both MGC-803 and HCT-116 cells.[1] HDAC-IN-57 has high metabolic stability in vitro. Retains 86.1% and 87.4% of the parent compound after 1 hour of incubation in human liver (HLM) and rat liver microsomes (RLM), respectively, with a T1/2 of over 120 minutes.[1]
In vivo	HDAC-IN-57 (Compound 5e) (1 mg/kg, i.v.; 10 mg/kg, p.o.) demonstrated T1/2 of 0.37 hours (IV) and 2.75 hours (OR), with an oral bioavailability (F%) of 10.6%.[1] HDAC-IN-57 (25 or 50 mg/kg gavage; once daily for 21 days) achieved dose-dependent tumor growth inhibition in the NOD-SCID mouse MGC-803 xenograft model.[1]

Chemical Properties

Molecular Weight	377.39
Formula	C₂₁H₁₉N₃O₄
Cas No.	2716217-79-5
Smiles	C(NCC1=CC=C(C(NO)=O)C=C1)(=O)C=2C=C(N=CC2)C3=CC=C(OC)C=C3
Relative Density.	1.282 g/cm3 at 20℃ (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (662.44 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 10 mg/mL (26.5 mM), Solution.

10% DMSO+90% Saline: < 10 mg/mL (26.5 mM), Lower concentrations may be soluble, but exact solubility limit is unknown.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6498 mL	13.2489 mL	26.4978 mL	132.4889 mL
5 mM	0.5300 mL	2.6498 mL	5.2996 mL	26.4978 mL
10 mM	0.2650 mL	1.3249 mL	2.6498 mL	13.2489 mL
20 mM	0.1325 mL	0.6624 mL	1.3249 mL	6.6244 mL
50 mM	0.0530 mL	0.2650 mL	0.5300 mL	2.6498 mL
100 mM	0.0265 mL	0.1325 mL	0.2650 mL	1.3249 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc