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SAR439859
CAS No. 2114339-57-8
SAR439859( —— )
Catalog No. M23964 CAS No. 2114339-57-8
SAR439859 is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 282 | In Stock |
|
| 10MG | 430 | In Stock |
|
| 25MG | 710 | In Stock |
|
| 50MG | 972 | In Stock |
|
| 100MG | 1332 | In Stock |
|
| 200MG | Get Quote | In Stock |
|
| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
|
Biological Information
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Product NameSAR439859
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NoteResearch use only, not for human use.
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Brief DescriptionSAR439859 is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD).
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DescriptionSAR439859 is an orally active, nonsteroidal and selective degrader of estrogen receptor (SERD). SAR439859 is a potent antagonist of ER (with an EC50 of 0.2 nM for ERα degradation).
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In Vitro——
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In VivoAnimal Model:Nu/nu mouse with MCF7 tumor xenograft model Dosage:2.5, 5, 12.5, 25 mg/kg Administration:Orally; twice daily for 30 days Result:Exhibited substantial tumor-growth inhibition and displayed tumor regression at the dose of 25 mg/kg/BID.Animal Model:Mouse, rat and dog Dosage:3 mg/kg (iv) and 10 mg/kg (po) (Pharmacokinetic Analysis) Administration:Iv or po Result:Showed a low to moderate clearance in the three animal species tested (0.03-1.92 L/h?kg), low to moderate volume of distribution (Vss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species.
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Synonyms——
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PathwayEndocrinology/Hormones
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TargetEstrogen Receptor/ERR
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RecptorERα
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Research Area——
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Indication——
Chemical Information
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CAS Number2114339-57-8
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Formula Weight554.48
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Molecular FormulaC31H30Cl2FNO3
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Purity>98% (HPLC)
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SolubilityDMSO:125 mg/mL?(225.44 mM;?Need ultrasonic)
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SMILESC1CC2=C(C=CC(=C2)C(=O)O)C(=C(C1)C3=C(C=C(C=C3)Cl)Cl)C4=CC=C(C=C4)O[C@H]5CCN(C5)CCCF
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Chemical Name——
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.El-Ahmad Y, et al. Discovery of 6-(2,4-Dichlorophenyl)-5-[4-[(3S)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7H-benzo[7]annulene-2-carboxylic acid (SAR439859), a Potent and Selective Estrogen Receptor Degrader (SERD) for the Treatment of Estrogen-Receptor-Positive Breast Cancer. J Med Chem. 2019 Nov 27.
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