Art. -Nr.: HY-143411

GEM144

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GEM144 is a potent and orally active DNA polymerase α (POLA1) and HDAC 11 dual inhibitor. GEM144 induces acetylation of p53, activation of p21, G1/S cell cycle arrest, and apoptosis. GEM144 has significant antitumor activity in human orthotopic malignant pleural mesothelioma xenografts.

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CAS. Nr.: 2487526-28-1
Formel: C₂₈H₃₁NO₅
Molecular Weight:461.55

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Data Sheet (277 KB)

GEM144 Chemical Structure

CAS. Nr.: 2487526-28-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

DNA Polymerase

HDAC11

8.23 μM (IC₅₀)

Alle HDAC Isoform-spezifische Produkte anzeigen :

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen :

In Vitro

GEM144 (0-10 μM; 24 hours) exhibits antiproliferative activity in tested cancer cell lines with IC₅₀s of 0.26 ~ 2.2 μM^[1].
GEM144 (0.1 - 0.4 μM; 24 hours) strongly increases levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulates p21 expression in a dose-dependent manner^[1].
GEM144 (0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473; 72 hours) induced G1/S cell cycle arrest^[1].

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

Cell Proliferation Assay

Cell Line:

NCI-H460, H460-R9A, A2780 and A2780-DX^[1]
Concentration:

0-10 μM
Incubation Time:

24 hours (further 48 h growth in drug-free medium)
Result:

Exhibited antiproliferative activity in tested cancer cell lines with IC₅₀s of 0.26 ~ 2.2 μM.

Western Blot Analysis

Cell Line:

NCI-H460^[1]
Concentration:

0.1 μM, 0.25 μM and 0.4 μM
Incubation Time:

24 hours
Result:

Strongly increased levels of H2AX phosphorylation on Ser 39 (γH2AX), and strongly upregulated p21 expression in a dose-dependent manner.

Cell Cycle Analysis

Cell Line:

NCI-H4609, A2780 and MM473^[1]
Concentration:

0.26 μM in NCI-H4609, 0.95 μM in A2780 and 1.4 μM in MM473
Incubation Time:

72 hours
Result:

Induced G1/S cell cycle arrest.

In Vivo

GEM144 (50 mg/kg; p.o., bid, 5 days a week, for 3-4 weeks) significantly reduces tumor burden of MM487 with TGI of 72% in xenografts mice^[1].

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

Animal Model:

Female CD-1 nude mice (injected with MM473 and MM487)^[1]
Dosage:

50 mg/kg
Administration:

PO, bid, 5 days a week, for 3-4 weeks
Result:

Significantly reduced tumor burden of MM487 with TGI of 72%.

Chemical Information

CAS. Nr. 2487526-28-1
Appearance Solid
Molecular Weight 461.55
Formel C₂₈H₃₁NO₅
Color White to off-white
SMILES

ONC(C(C)OC1=C(C=C(C2=CC=C(C=C2)/C=C/C(O)=O)C=C1)C34CC5CC(CC(C5)C4)C3)=O
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 200 mg/mL (433.32 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

2.1666 mL

10.8331 mL

21.6661 mL

5 mM

0.4333 mL

2.1666 mL

4.3332 mL

10 mM

0.2167 mL

1.0833 mL

2.1666 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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 90% Corn Oil

Solubility: ≥ 5 mg/mL (10.83 mM); Clear solution

This protocol yields a clear solution of ≥ 5 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 (50.0 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 (277 KB)
SDS (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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]. Dallavalle S, et al. Antitumor activity of novel POLA1-HDAC11 dual inhibitors. Eur J Med Chem. 2022;228:113971. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1666 mL	10.8331 mL	21.6661 mL	54.1653 mL
	5 mM	0.4333 mL	2.1666 mL	4.3332 mL	10.8331 mL
	10 mM	0.2167 mL	1.0833 mL	2.1666 mL	5.4165 mL
	15 mM	0.1444 mL	0.7222 mL	1.4444 mL	3.6110 mL
	20 mM	0.1083 mL	0.5417 mL	1.0833 mL	2.7083 mL
	25 mM	0.0867 mL	0.4333 mL	0.8666 mL	2.1666 mL
	30 mM	0.0722 mL	0.3611 mL	0.7222 mL	1.8055 mL
	40 mM	0.0542 mL	0.2708 mL	0.5417 mL	1.3541 mL
	50 mM	0.0433 mL	0.2167 mL	0.4333 mL	1.0833 mL
	60 mM	0.0361 mL	0.1806 mL	0.3611 mL	0.9028 mL
	80 mM	0.0271 mL	0.1354 mL	0.2708 mL	0.6771 mL
	100 mM	0.0217 mL	0.1083 mL	0.2167 mL	0.5417 mL

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GEM144

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GEM144

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Epigenetics Compound Library

Histone Modification Research Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Reprogramming Compound Library

Oxygen Sensing Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Liver Cancer Compound Library

Osteogenesis Compound Library

Cell Death Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Brain Cancer Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Lactylation Compound Library

Alle HDAC Isoform-spezifische Produkte anzeigen

Alle DNA/RNA Synthesis Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GEM144 Related Classifications

Art. -Nr.: HY-143411