GW273297X
GW273297X is a selective CYP27A1 inhibitor. GW273297X blocks 27-hydroxycholesterol biosynthesis and sterol product formation in human macrophages. GW273297X reduces cancer cells colonization by inhibiting pro-metastatic effects of 27-hydroxycholesterol. GW273297X can be used for the researches of cancer and metabolic disease, such as breast cancer.
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- CAS No.: 1713317-28-2
- Formule: C29H48O3
- Masse moléculaire:444.69
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
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CYP27A1 |
GW273297X (1 μM; 24 h) potently inhibits CYP27A1 enzyme activity in PMA-differentiated THP-1 human macrophage-like cells[2].
GW273297X (1 μM; 24 h) potently inhibits CYP27A1 enzyme activity in PMA (HY-18739)-differentiated THP-1 human macrophage-like cells when cholesterol is used as substrate[2].
GW273297X (1 μM; 24 h) potently and nearly completely inhibits CYP27A1 enzyme activity in primary human monocyte-derived macrophages (HMDMs)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
GW273297X (100 mg/kg; s.c.; daily; 5 days) reduces early-stage lung metastatic colonization by Met1 and E0771 breast cancer cells in naive wild-type mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Humanized APOE3 with E0771-iRFP cells (ovariectomized female, ~6 weeks of age at ovariectomy)[1]
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Dosage:100 mg/kg
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Administration:s.c.; daily; 28 days
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Result:Attenuated the increased lung metastatic burden induced by the high-fat diet, as measured by relative fluorescence of iRFP-expressing tumor cells.
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Animal Model:wild-type with Met1 and E0771 breast cancer cells (naive)[1]
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Dosage:100 mg/kg
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Administration:s.c.; daily; 5 days
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Result:Reduced the number of Met1 metastatic colonies in the lungs, as measured by relative fluorescence of iRFP-expressing tumor cells.
Reduced lung metastatic colonization by E0771 cells; this effect was reversed by co-pretreatment with exogenous 27-hydroxycholesterol.
Chemical Information
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CAS No. 1713317-28-2
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Masse moléculaire 444.69
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Formule C29H48O3
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SMILES
C[C@@]12[C@]3([H])[C@]([C@@H](C[C@]1([H])CC(OC)(CC2)OC)O)([H])[C@@]4([H])[C@](CC3)([C@H](CC4)[C@H](C)CCCCC#C)C
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Synonyms
G297X
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Baek AE, et al. The cholesterol metabolite 27 hydroxycholesterol facilitates breast cancer metastasis through its actions on immune cells. Nat Commun. 2017;8(1):864. Published 2017 Oct 11. [Content Brief]
[2]. Quinn CM, et al. Expression and regulation of sterol 27-hydroxylase (CYP27A1) in human macrophages: a role for RXR and PPARgamma ligands. Biochem J. 2005;385(Pt 3):823-830. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GW273297X Related Classifications
HY-176497 Related Classifications
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