1. JAK/STAT Signaling Stem Cell/Wnt Metabolic Enzyme/Protease
  2. STAT Cytochrome P450
  3. AS1810722

AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research.

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

AS1810722 Chemical Structure

AS1810722 Chemical Structure

CAS No. : 909561-15-5

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 315 In-stock
Solution
10 mM * 1 mL in DMSO USD 315 In-stock
Solid
1 mg USD 130 In-stock
5 mg USD 300 In-stock
10 mg USD 450 In-stock
25 mg USD 765 In-stock
50 mg USD 1100 In-stock
100 mg USD 1570 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

AS1810722 is an orally active and potent STAT6 inhibitor with an IC50 of 1.9 nM. AS1810722 shows a good profile of CYP3A4 inhibition. AS1810722, a derivative of fused bicyclic pyrimidine, has the potential for allergic diseases such as asthma and atopic diseases research[1].

IC50 & Target[1]

STAT6

1.9 nM (IC50)

CYP3A4

 

Cellular Effect
Cell Line Type Value Description References
T-cell IC50
2.4 nM
Compound: 24, AS1810722
Inhibition of IL4 production in C57BL/6 mouse T cell after 16 hrs by T cell differentiation assay
Inhibition of IL4 production in C57BL/6 mouse T cell after 16 hrs by T cell differentiation assay
[PMID: 19747833]
In Vitro

AS1810722 (compound 24) inhibits production of IL-4 with an IC50 of 2.4 nM, but shows no effect on production of IFN-γ[1].

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

In Vivo

AS1810722 (compound 24; 0.03-0.3 mg/kg; orally; 30 min before, and 24h and 48 h after OVA exposure) suppress eosinophil infiltration in the lung in a dose-dependent manner in an antigen-induced mouse asthmatic model[1].
AS1810722 inhibits in vitro Th2 differentiation with an IC50 of 2.4 nM without affecting type 1 helper T (Th1) cell differentiation and eosinophil infiltration in an antigen-induced mouse asthmatic model after oral administration[1].

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

Animal Model: Female Balb/c mice asthmatic model by intraperitoneal injection of ovalbumin (OVA)-containing aluminum hydroxide gel[1]
Dosage: 0.03-0.3 mg/kg
Administration: Orally; 30 min before, and 24 and 48 h after OVA exposure
Result: Suppressed eosinophil infiltration in the lung in a dose-dependent manner.
Molecular Weight

477.51

Formula

C25H25F2N7O

CAS No.
Appearance

Solid

Color

Brown to black

SMILES

O=C(N)CN1CCN(C2=CC=C(NC3=NC=C4C(N(CC5=CC(F)=CC(F)=C5)C=C4)=N3)C=C2)CC1

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 : 62.5 mg/mL (130.89 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0942 mL 10.4710 mL 20.9420 mL
5 mM 0.4188 mL 2.0942 mL 4.1884 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (4.36 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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 2.0942 mL 10.4710 mL 20.9420 mL 52.3549 mL
5 mM 0.4188 mL 2.0942 mL 4.1884 mL 10.4710 mL
10 mM 0.2094 mL 1.0471 mL 2.0942 mL 5.2355 mL
15 mM 0.1396 mL 0.6981 mL 1.3961 mL 3.4903 mL
20 mM 0.1047 mL 0.5235 mL 1.0471 mL 2.6177 mL
25 mM 0.0838 mL 0.4188 mL 0.8377 mL 2.0942 mL
30 mM 0.0698 mL 0.3490 mL 0.6981 mL 1.7452 mL
40 mM 0.0524 mL 0.2618 mL 0.5235 mL 1.3089 mL
50 mM 0.0419 mL 0.2094 mL 0.4188 mL 1.0471 mL
60 mM 0.0349 mL 0.1745 mL 0.3490 mL 0.8726 mL
80 mM 0.0262 mL 0.1309 mL 0.2618 mL 0.6544 mL
100 mM 0.0209 mL 0.1047 mL 0.2094 mL 0.5235 mL
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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.

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Product Name:
AS1810722
Cat. No.:
HY-134772
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