PX20350
PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models.
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- CAS No.: 1198085-23-2
- 화학식: C28H22Cl2F3N3O4
- 분자량:592.39
-
보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at androgen receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at androgen receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at CAR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at CAR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at ERalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at ERalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at ERbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at ERbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at GR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at GR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at LXRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at LXRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at LXRbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at LXRbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at mineralocorticoid receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at mineralocorticoid receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at PPARalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at PPARalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at PPAR-beta/delta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at PPAR-beta/delta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at PPARgamma-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at PPARgamma-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at progesterone receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at progesterone receptor-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at RARalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at RARalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at RARbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at RARbeta-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at RARgamma-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at RARgamma-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at RXRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at RXRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at TRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at TRalpha-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
>10 μM
Compound: 22
|
Agonist activity at VDR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at VDR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
30 nM
Compound: 22
|
Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay
Agonist activity at human GST-fused FXR LBD expressed in HEK293 cells coexpressing GAL4-DNA bindig domain and pFRluc by mammalian one-hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
3871 μM
Compound: 22
|
Agonist activity at PXR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
Agonist activity at PXR-LBD expressed in HEK293 cells assessed as Gal4-DBD interaction by cellular mammalian one hybrid assay
|
[PMID: 20638278] |
| HEK293 | EC50 |
6 nM
Compound: 22
|
Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay
Agonist activity at human full length FXR transfected in HEK293 cells coexpressing pTRexDest/pGL2promotor assessed as luciferase activity by direct reporter cellular assay
|
[PMID: 20638278] |
Chemical Information
-
CAS No. 1198085-23-2
-
분자량 592.39
-
화학식 C28H22Cl2F3N3O4
-
SMILES
O=C(C1=CC=C(CN(C)C2=CC=C(OCC3=C(C4CC4)ON=C3C5=C(Cl)C=CC=C5Cl)N=C2C(F)(F)F)C=C1)O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)