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Chemical Structure| 1126084-37-4 Chemical Structure| 1126084-37-4

Structure of ASP-9521
CAS No.: 1126084-37-4

Chemical Structure| 1126084-37-4

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ASP 9521 is a potent and selective AKR1C3 inhibitor with IC50 of 11 nM for human AKR1C3.

4.5 *For Research Use Only !

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Product Details of ASP-9521

CAS No. :1126084-37-4
Formula : C19H26N2O3
M.W : 330.42
SMILES Code : O=C(N1CCC(CC1)CC(C)(O)C)C2=CC3=CC(OC)=CC=C3N2
MDL No. :MFCD30532740
InChI Key :OXSCPDKUZWPWFR-UHFFFAOYSA-N
Pubchem ID :25210792

Safety of ASP-9521

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
VCaP cells 50 nM 48 h To evaluate the inhibitory effect of ASP-9521 on AKR1C3 expression, results showed that ASP-9521 alone or in combination with genistein significantly reduced AKR1C3 expression. Food Nutr Res. 2023 Jan 31;67
KATO/DDP cells 5 μM and 10 μM 24 h Enhance cisplatin-induced cell death, but no influence on percent cell apoptosis Int J Mol Sci. 2021 Nov 19;22(22):12512
MCF-7 1 µM 24 h Evaluate the effect of ASP9521 on cell migration, results showed an increase in cell migration Int J Mol Sci. 2024 Jan 25;25(3):1471
SUM-159 1 µM 24 h Evaluate the effect of ASP9521 on cell migration, results showed a decrease in cell migration Int J Mol Sci. 2024 Jan 25;25(3):1471
SUM-149 1 µM 24 h Evaluate the effect of ASP9521 on cell migration, results showed a reduction in cell migration by approximately 15% Int J Mol Sci. 2024 Jan 25;25(3):1471
rat cardiomyocyte H9c2 25 μM 24 h To assess the cardioprotective effect of ASP9521 against DOX/DNR-induced toxicity in H9c2 cells. Results showed that ASP9521 significantly reduced the toxicity of DOX and DNR on H9c2 cells. Molecules. 2023 Apr 27;28(9):3767
human lung carcinoma cell line A549 25 μM 48 h To evaluate the enhancement of anticancer activity of DNR on A549 cells by co-administration with ASP9521. Results showed that ASP9521 significantly increased the cytotoxicity of DNR. Molecules. 2023 Apr 27;28(9):3767
HeLa-AR3A-PSA-(ARE)4-Luc13 cells 300 μM No inhibition of AR reporter gene activity observed J Steroid Biochem Mol Biol. 2019 Sep;192:105283
LNCaP-AKR1C3 cells 30 μM 48 h Inhibited conversion of 4-AD to testosterone, 100% inhibition at 30 μM J Steroid Biochem Mol Biol. 2019 Sep;192:105283

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT01352208 Castrate Resistant Prostate Ca... More >>ncer Less << Phase 1 Phase 2 Terminated(It was decided to d... More >>iscontinue the development in consideration of the results of a P1 study) Less << - Belgium ... More >> Site 131 Antwerp, Belgium, 2650 France Site: 121 Villejuif, France United Kingdom Site:109 Glasgow, United Kingdom Site: 101 Surrey, United Kingdom Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.03mL

0.61mL

0.30mL

15.13mL

3.03mL

1.51mL

30.26mL

6.05mL

3.03mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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