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EPI-001
CAS No. 227947-06-0
EPI-001( EPI001 )
Catalog No. M13623 CAS No. 227947-06-0
EPI-001 is a small molecule that blocks transactivation of the androgen Receptor (AR) NTD (IC50=6 uM).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 45 | In Stock |
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| 2MG | 29 | In Stock |
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| 5MG | 41 | In Stock |
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| 10MG | 67 | In Stock |
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| 25MG | 123 | In Stock |
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| 50MG | 198 | In Stock |
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| 100MG | 296 | In Stock |
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| 200MG | 440 | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameEPI-001
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NoteResearch use only, not for human use.
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Brief DescriptionEPI-001 is a small molecule that blocks transactivation of the androgen Receptor (AR) NTD (IC50=6 uM).
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DescriptionEPI-001 is a small molecule that blocks transactivation of the androgen Receptor (AR) NTD (IC50=6 uM) and specificly inhibits AR without attenuating transcriptional activities of related steroid receptors; targets the transactivation unit 5 of AR and interacts with AF-1 in the NTD to prevent protein-protein interactions; inhibits endogenous expression of androgen-regulated genes, inhibits both androgen-dependent and androgen-independent (OCM-induced) proliferation of LNCaP cells; reduces the growth of CRPC xenografts; also is a selective PPAR-gamma modulator.
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In VitroCell Proliferation Assay Cell Line:PCa, CRPC, PC-3, DU 145, and T47D cell lines Concentration:0, 5, 10, 25, 50, 100 μM Incubation Time:7 days Result:Inhibited growth of LNCaP cells at low concentrations.Inhibited growth of AR-negative PC-3 and DU 145 cell lines as well as the T47D breast carcinoma cell line.Western Blot Analysis Cell Line:LNCaP, VCaP LAPC4, C4-2,22Rv1, and CWR-R1 cells Concentration:50 μM Incubation Time:8-16 hours Result:Decreased expression of full-length AR protein to varying degrees.
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In VivoAnimal Model:Male NOD-SCID mice (6-8 weeks) bearing LNCaP Dosage:20 mg/kg Administration:I.v. every 5 days for 25 days Result:Reduced tumors from 100.3±1.72 mm3 to 73.03±29.6 mm3 within 2 weeks.Did not cause general toxicity indicated by no change in animal behavior or body weight.
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SynonymsEPI001
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PathwayEndocrinology/Hormones
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TargetAndrogen Receptor (AR)
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RecptorAndrogen Receptor
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Research AreaCancer
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Indication——
Chemical Information
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CAS Number227947-06-0
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Formula Weight394.89
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Molecular FormulaC21H27ClO5
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 33.33 mg/mL (84.40 mM)
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SMILESOCC(O)COC1=CC=C(C(C)(C2=CC=C(OCC(O)CCl)C=C2)C)C=C1
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Chemical Name3-[4-[1-[4-(3-chloro-2-hydroxypropoxy)phenyl]-1-methylethyl]phenoxy]-1,2-propanediol
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Myung JK, et al. J Clin Invest. 2013 Jul;123(7):2948-60.
2. De Mol E, et al. ACS Chem Biol. 2016 Sep 16;11(9):2499-505.
3. Andersen RJ, et al. Cancer Cell. 2010 Jun 15;17(6):535-46.
4. Brand LJ, et al. Oncotarget. 2015 Feb 28;6(6):3811-24.
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