Art. -Nr.: HY-175243

ADAR1-IN-1

Name: ADAR1-IN-1
Brand: MedChemExpress
SKU: HY-175243
Price: 190.00 USD
Availability: InStock
Rating: 5 (1 reviews)

Kundenbewertung

Based on 1 Customer Validation

ADAR1-IN-1 is a potent ADAR1 inhibitor. ADAR1-IN-1 significantly suppressed DU-145 cell proliferation (IC₅₀ = 1.11 μM), clonogenicity, migration, and invasion, arrests cell cycle, and induces apoptosis. ADAR1-IN-1 safely and effectively inhibits tumor growth. ADAR1-IN-1 can be used for the study of prostate cancer (PCa).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 98.18%
CAS. Nr.: 2734853-87-1
Formel: C₁₇H₁₅F₄N₅O₆S
Molecular Weight:493.39

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

ADAR1-IN-1 Chemical Structure

CAS. Nr.: 2734853-87-1

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

In Vitro

ADAR1-IN-1 (Compound C12) (1-3 μM, 1-4 days) significantly inhibits the growth and colony formation of DU-145 cells at a concentration of 1 μM, with maximal inhibition observed at 3 μM^[1].
ADAR1-IN-1 (1-3 μM, 24 h) dose-dependently inhibits the migration and invasion of DU-145 cells by ^[1].
ADAR1-IN-1 (1-3 μM, 24-48 h) significantly arrests DU-145 cells in the G0/G1 phase and induces apoptosis in a dose-dependent manner^[1].
ADAR1-IN-1 (1-3 μM, 48 h) induces a downregulation of N-cadherin and vimentin and a upregulation of p53 in DU-145 cells^[1].
ADAR1-IN-1 (72 h) exhibits significant proliferation inhibition against androgen receptor-dependent VCaP cells, castration-resistant 22Rv1 cells, and AR-negative PC-3 cells with IC50 values of 1.76 μM, 1.79 μM, and 0.72 μM, respectively^[1].

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

Cell Migration Assay ^[1]

Cell Line:

DU-145 cells
Concentration:

1, 2 and 3 μM
Incubation Time:

24 h
Result:

Dose-dependently inhibited the migration.

Cell Cycle Analysis^[1]

Cell Line:

DU-145 cells
Concentration:

1, 2 and 3 μM
Incubation Time:

24 h
Result:

Arrested cells in the G0/G1 phase.

Apoptosis Analysis^[1]

Cell Line:

DU-145 cells
Concentration:

1, 2 and 3 μM
Incubation Time:

24 h
Result:

Induced apoptosis in a dose-dependent manner.

Western Blot Analysis^[1]

Cell Line:

DU-145 cells
Concentration:

1, 2 and 3 μM
Incubation Time:

48 h
Result:

Induced a concentration-dependent downregulation of N-cadherin and vimentin.
Decreased CDk6 and c-MYC, and increased p53.

Parmacokinetics

Species	Dose	Route	C_max	AUC_0-∞	MRT_0-∞	T_max	T_1/2	Bioavailability	CL	F
Rat^[1]	10 mg/kg	i.p.	4713.83 ng/mL	9137.65 ng·h/mL	1.59 h	0.39 h	1.46 h	2.30 L/kg	1.10 L/h/kg	210.75 %
Rat^[1]	2 mg/kg	i.v.	957.66 ng/mL	868.29 ng·h/mL	0.91 h	/	1.15 h	3.86 L/kg	2.31 L/h/kg	/

In Vivo

ADAR1-IN-1 (Compound C12) (15-30 mg/kg, i.p., twice daily for 19 days) has potent antitumor efficacy and safety properties in DU-145 and 22Rv1 xenograft mice models^[1].

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

Animal Model:

DU-145 and 22Rv1 xenograft models established in male BALB/c nude mice^[1]
Dosage:

15 and 30 mg/kg
Administration:

Intraperitoneal injection (i.p.), twice daily for 19 days
Result:

Significantly inhibited tumor growth with tumor growth inhibition (TGI) rates of 41.8% and 52.8%, respectively in DU-145 model and 46.4% and 59.0%, respectively in 22Rv1 model.
No obvious lesions were observed in the main organs of the mice.

Chemical Information

CAS. Nr. 2734853-87-1
Appearance Solid
Molecular Weight 493.39
Formel C₁₇H₁₅F₄N₅O₆S
Color White to off-white
SMILES

O[C@@H]1[C@H](O)[C@@H](COS(=O)(C2=CC=C(C=C2)C(F)(F)F)=O)O[C@H]1N3C4=NC(F)=NC(N)=C4N=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 100 mg/mL (202.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

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

2.0268 mL

10.1340 mL

20.2679 mL

5 mM

0.4054 mL

2.0268 mL

4.0536 mL

10 mM

0.2027 mL

1.0134 mL

2.0268 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 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (5.07 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 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 (278 KB)
SDS (252 KB)
- English - EN (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]. Zhu Y, et al. Design, Synthesis, and Activity Evaluation of Novel Nucleosides as ADAR1 Inhibitor for the Treatment of Prostate Cancer. J Med Chem. 2025 Jul 24;68(14):14495-14513. [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	2.0268 mL	10.1340 mL	20.2679 mL	50.6699 mL
	5 mM	0.4054 mL	2.0268 mL	4.0536 mL	10.1340 mL
	10 mM	0.2027 mL	1.0134 mL	2.0268 mL	5.0670 mL
	15 mM	0.1351 mL	0.6756 mL	1.3512 mL	3.3780 mL
	20 mM	0.1013 mL	0.5067 mL	1.0134 mL	2.5335 mL
	25 mM	0.0811 mL	0.4054 mL	0.8107 mL	2.0268 mL
	30 mM	0.0676 mL	0.3378 mL	0.6756 mL	1.6890 mL
	40 mM	0.0507 mL	0.2533 mL	0.5067 mL	1.2667 mL
	50 mM	0.0405 mL	0.2027 mL	0.4054 mL	1.0134 mL
	60 mM	0.0338 mL	0.1689 mL	0.3378 mL	0.8445 mL
	80 mM	0.0253 mL	0.1267 mL	0.2533 mL	0.6334 mL
	100 mM	0.0203 mL	0.1013 mL	0.2027 mL	0.5067 mL

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

ADAR1-IN-1