Art. -Nr.: HY-114414

HDACs/mTOR Inhibitor 1

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

HDACs/mTOR Inhibitor 1 is a dual HDACs and mTOR inhibitor, with IC₅₀s of 0.19 nM, 1.8 nM, 1.2 nM for HDAC1, HDAC6, mTOR, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induces tumor cell apoptosis with low toxicity in vivo. HDACs/mTOR Inhibitor 1 can be used in the research of hematologic malignancies.

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Reinheit: 98.10%
CAS. Nr.: 2271413-06-8
Formel: C₂₈H₃₈N₈O₅
Molecular Weight:566.65

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

HDACs/mTOR Inhibitor 1 Chemical Structure

CAS. Nr.: 2271413-06-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

HDAC1

0.19 nM (IC₅₀)

HDAC6

1.8 nM (IC₅₀)

mTOR

1.2 nM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Alle mTOR Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	IC₅₀	17.2 nM Compound: 12l	Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay	[PMID: 30629434]
MM1.S	IC₅₀	7.3 nM Compound: 12l	Antiproliferative activity against human MM1S cells after 72 hrs by MTT assay Antiproliferative activity against human MM1S cells after 72 hrs by MTT assay	[PMID: 30629434]
MV4-11	IC₅₀	4.05 nM Compound: 12l	Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay	[PMID: 30629434]
OCI-AML2	IC₅₀	9.01 nM Compound: 12l	Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML2 cells after 72 hrs by MTT assay	[PMID: 30629434]
OCI-AML-3	IC₅₀	9.98 nM Compound: 12l	Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay Antiproliferative activity against human OCI-AML3 cells after 72 hrs by MTT assay	[PMID: 30629434]
Raji	IC₅₀	1.9 nM Compound: 12l	Antiproliferative activity against human Raji cells after 72 hrs by MTT assay Antiproliferative activity against human Raji cells after 72 hrs by MTT assay	[PMID: 30629434]
Sf9	IC₅₀	0.58 nM Compound: 12l	Inhibition of recombinant full length N-terminal FLAG-tagged human HDAC10 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay Inhibition of recombinant full length N-terminal FLAG-tagged human HDAC10 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay	[PMID: 30629434]
Sf9	IC₅₀	>1000 nM Compound: 12l	Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay Inhibition of recombinant full length human HDAC4 expressed in baculovirus infected sf9 cells using Ac-peptide-AMC as substrate preincubated for 15 mins followed by substrate addition and measured after 1 hr by fluorescence assay	[PMID: 30629434]

In Vitro

HDACs/mTOR Inhibitor 1 (Compound 12l) inhibits leukemia cells proliferation with IC₅₀s of 4.05, 9.01, 9.98 μM for MV4-11, OCI-AML2, OCI-AML3 cells^[1].
HDACs/mTOR Inhibitor 1 (0-10 μM, 6 h or 24 h) downregulates p-ERK and increases Ac-H3 in MV4-11 cells^[1].
HDACs/mTOR Inhibitor 1 (10 to 1000 nM, 48 h) reduces S-phase cells and increases the percentage of cells in G0/G1 phase in MV4-11 cells^[1].

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

Western Blot Analysis^[1]

Cell Line:

MV4-11 cells
Concentration:

0.01, 0.1, 1, 10 μM
Incubation Time:

6 h or 24 h
Result:

Downregulated p-ERK (24 h) and increased of the Ac-H3 (6 h) in a dose-dependent manner.

In Vivo

HDACs/mTOR Inhibitor 1 (Compound 12l) (10 or 20 mg/kg, i.v.) inhibits tumor growth without significant toxicity in MV4-11 and MM1S xenograft NOD/SCID mouse model^[1].

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

Animal Model:

MV4-11 xenograft NOD/SCID mouse model^[1]
Dosage:

10 mg/kg
Administration:

Intravenous injection (i.v.), every two days (Q2D)×6
Result:

The TGI (tumor growth inhibitory rate) was 53.1%.

Chemical Information

CAS. Nr. 2271413-06-8
Appearance Solid
Molecular Weight 566.65
Formel C₂₈H₃₈N₈O₅
Color White to off-white
SMILES

O=C(NO)CCCCCCN1C2=NC(C3=CC=C(NC(N4C[C@@H](C)OCC4)=O)C=C3)=NC(N5CCOCC5)=C2C=N1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

Front Pharmacol

CC-223, NSC781406, and BGT226 Exerts a Cytotoxic Effect Against Pancreatic Cancer Cells via mTOR Signaling. [Abstract]

2020 Nov 11;11:580407. PMID: 33343350

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 32.5 mg/mL (57.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7648 mL

8.8238 mL

17.6476 mL

5 mM

0.3530 mL

1.7648 mL

3.5295 mL

10 mM

0.1765 mL

0.8824 mL

1.7648 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.17 mg/mL (3.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.17 mg/mL (3.83 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Chen Y, et al. Discovery of a Novel Dual Histone Deacetylases (HDACs) and Mammalian Target of Rapamycin (mTOR) Target Inhibitor as a Promising Strategy for Cancer Therapy. J Med Chem. 2019 Jan 10. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.7648 mL	8.8238 mL	17.6476 mL	44.1189 mL
	5 mM	0.3530 mL	1.7648 mL	3.5295 mL	8.8238 mL
	10 mM	0.1765 mL	0.8824 mL	1.7648 mL	4.4119 mL
	15 mM	0.1177 mL	0.5883 mL	1.1765 mL	2.9413 mL
	20 mM	0.0882 mL	0.4412 mL	0.8824 mL	2.2059 mL
	25 mM	0.0706 mL	0.3530 mL	0.7059 mL	1.7648 mL
	30 mM	0.0588 mL	0.2941 mL	0.5883 mL	1.4706 mL
	40 mM	0.0441 mL	0.2206 mL	0.4412 mL	1.1030 mL
	50 mM	0.0353 mL	0.1765 mL	0.3530 mL	0.8824 mL

Keywords

HDACs/mTOR Inhibitor 1

1 Cited Publications

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HDACs/mTOR Inhibitor 1

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Publications Citing Use of MedChemExpress (MCE) HDACs/mTOR Inhibitor 1

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle mTOR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

HDACs/mTOR Inhibitor 1 Related Classifications

HY-114414 Related Classifications