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SAR-439859

Product Name
SAR-439859
CAS No.
2114339-57-8
Chemical Name
SAR-439859
Synonyms
SAR-439859;Amcenestrant;Bromfenac Impurity 64;Amcenestrant (SAR439859);Amcenestrant, 10 mM in DMSO;(S)-8-(2,4-dichlorophenyl)-9-(4-((1-(3-fluoropropyl)pyrrolidin-3-yl)oxy)phenyl)-6,7-dihydro-5H-benzo[7]annulene-3-carboxylic acid;5H-Benzocycloheptene-3-carboxylic acid, 8-(2,4-dichlorophenyl)-9-[4-[[(3S)-1-(3-fluoropropyl)-3-pyrrolidinyl]oxy]phenyl]-6,7-dihydro-;breast,Amcenestrant,Inhibitor,degradation,SAR 439859,SAR-439859,antitumor,cancer,SERD,inhibit,cross-resistance,degrader,Orally,Estrogen Receptor/ERR,nonsteroidal
CBNumber
CB06226248
Molecular Formula
C31H30Cl2FNO3
Formula Weight
554.48
MOL File
2114339-57-8.mol
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SAR-439859 Property

Boiling point:
676.7±55.0 °C(Predicted)
Density 
1.297±0.06 g/cm3(Predicted)
solubility 
DMSO:100.0(Max Conc. mg/mL);180.35(Max Conc. mM)
pka
4.18±0.20(Predicted)
form 
Solid
color 
White to off-white
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Hazard and Precautionary Statements (GHS)

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SAR-439859 Chemical Properties,Usage,Production

Uses

SAR439859 (compound 43d) is an orally active, non-steroidal, and selective estrogen receptor degrader (SERD). SAR439859 is an effective ER antagonist with ER degradation activity, an EC50 of 0.2 nM. SAR439859 can show potent anti-tumor effects and limited cross-resistance in ER+ breast cancer.

in vivo

SAR439859 (compound 43d; orally; 2.5-25 mg/kg; twice daily for 30 days) exhibits substantial tumor-growth inhibition and displays tumor regression at the dose of 25 mg/kg/BID[1].
SAR439859 (3 mg/kg for iv and 10 mg/kg for po) shows 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. It is noticed that T1/2 was variable across species (1.98 h in mouse, 4.13 h in rat and 9.80 h in dog)[1].

Animal Model:Nu/nu mouse with MCF7 tumor xenograft model[1]
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[1]
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.

IC 50

ERα: 0.2 nM (EC50)

References

[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. DOI:10.1021/acs.jmedchem.9b01293
[2] Monsif Bouaboula, et al. Abstract 943: SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that demonstrates robust antitumor efficacy and limited cross-resistance in ER+ breast cancer.

SAR-439859 Preparation Products And Raw materials

Raw materials

Preparation Products

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SAR-439859 Suppliers

China 52 United States 4 Global 56
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070 13913916777;
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
15724
Advantage
64
BOC Sciences
Tel
1-631-485-4226; 16314854226
Email
info@bocsci.com
Country
United States
ProdList
12952
Advantage
65
ShangHai Caerulum Pharma Discovery Co., Ltd.
Tel
18149758185 18149758185;
Email
sales-cpd@caerulumpharma.com
Country
China
ProdList
3505
Advantage
58
Hygeia (Chengdu) pharmaceutical technique Co., Ltd
Tel
028-84502008 13568869383
Fax
028-66476329
Email
sales@hygeiapharm.com
Country
China
ProdList
300
Advantage
55
Shanghai Lollane Biological Technology Co.,Ltd.
Tel
021-52996696，15000506266 15000506266
Fax
+86-21-52996696
Country
China
ProdList
4795
Advantage
55
Shanghai YuanYe Biotechnology Co., Ltd.
Tel
021-61312847; 18021002903
Fax
QQ:3008007432
Email
3008007409@qq.com
Country
China
ProdList
71826
Advantage
60
ShangHai Biochempartner Co.,Ltd
Tel
177-54423994 17754423994
Fax
QQ:2853530913
Email
2853530910@QQ.com
Country
China
ProdList
8000
Advantage
62
Shanghai Rechem science Co., Ltd.
Tel
021-31433387 15618786686
Fax
QQ:1369748377
Email
sales@rechemscience.com
Country
China
ProdList
2968
Advantage
58
Wellman Pharmaceutical Group Limited
Tel
027-027-83778875 15807197853
Fax
027-83991220
Email
15807197853@163.com
Country
China
ProdList
3945
Advantage
58
Shanghai Jinsheng Pharmaceutical Co., Ltd.
Tel
1365-13651960330 13651960330
Email
xiangfeixia@jspharmatech.com
Country
China
ProdList
373
Advantage
58

2114339-57-8, SAR-439859Related Search:


  • SAR-439859
  • 5H-Benzocycloheptene-3-carboxylic acid, 8-(2,4-dichlorophenyl)-9-[4-[[(3S)-1-(3-fluoropropyl)-3-pyrrolidinyl]oxy]phenyl]-6,7-dihydro-
  • (S)-8-(2,4-dichlorophenyl)-9-(4-((1-(3-fluoropropyl)pyrrolidin-3-yl)oxy)phenyl)-6,7-dihydro-5H-benzo[7]annulene-3-carboxylic acid
  • Amcenestrant
  • breast,Amcenestrant,Inhibitor,degradation,SAR 439859,SAR-439859,antitumor,cancer,SERD,inhibit,cross-resistance,degrader,Orally,Estrogen Receptor/ERR,nonsteroidal
  • Bromfenac Impurity 64
  • Amcenestrant, 10 mM in DMSO
  • Amcenestrant (SAR439859)
  • 2114339-57-8
  • C31H30Cl2FNO3