PX20350

Cat. No.: HY-139418: Data Sheet Handling Instructions
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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.

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

PX20350 Chemical Structure

CAS No. : 1198085-23-2

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Description

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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 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 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 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 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	> 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 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 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]

Molecular Weight

592.39

Formula

C₂₈H₂₂Cl₂F₃N₃O₄

CAS No.

1198085-23-2

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Deuschle U, et al. FXR controls the tumor suppressor NDRG2 and FXR agonists reduce liver tumor growth and metastasis in an orthotopic mouse xenograft model. PLoS One. 2012;7(10):e43044. [Content Brief]

PX20350 Related Classifications

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The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

PX203501198085-23-2PX 20350PX-20350FXRNR1H4NDRG2SK-GI-18 cellsAnti-tumorigenicOrthotopic xenograft mouse modelsInhibitorinhibitorinhibit

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PX20350

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PX20350 Related Classifications

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