2. Metabolic Enzyme/Protease Apoptosis
  3. Adenosine Deaminase Apoptosis
  4. ADAR1-IN-1

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).

For research use only. We do not sell to patients.

ADAR1-IN-1

ADAR1-IN-1 Chemical Structure

CAS No. : 2734853-87-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

ADAR1-IN-1 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

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)[1].

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.

ADAR1-IN-1 Related Antibodies

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 Cmax AUC0-∞ MRT0-∞ Tmax T1/2 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.
Molecular Weight

493.39

Formula

C17H15F4N5O6S
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0268 mL 10.1340 mL 20.2679 mL
5 mM 0.4054 mL 2.0268 mL 4.0536 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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ADAR1-IN-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ADAR1-IN-12734853-87-1Adenosine DeaminaseApoptosisNucleoside analogsProstate cancerDU-145 cells22Rv1 cellsXenograft modelInhibitorinhibitorinhibit

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