ChemicalBook CAS DataBase List Sar-439859

Sar-439859

Product NameSar-439859
CAS2114339-57-8
CBNumberCB06226248
MFC31H30Cl2FNO3
MW554.48
EINECS-0
MOL File2114339-57-8.mol
MSDS FileSDS

Chemical Properties

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
FDA UNII	TBF1NHY02O

Sar-439859 Price

Product number	Packaging	Price	Product description	Buy
Cayman Chemical 40748	1mg	$75	SAR439859 ≥98%	Buy
Cayman Chemical 40748	5mg	$262	SAR439859 ≥98%	Buy
Cayman Chemical 40748	10mg	$412	SAR439859 ≥98%	Buy
Cayman Chemical 40748	25mg	$655	SAR439859 ≥98%	Buy
ChemScene CS-0109407	5mg	$271	Amcenestrant 99.79%	Buy

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 (V_ss=0.5-6.1 L/kg), and good bioavailability (54-76%) across species. It is noticed that T_1/2 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/hkg), low to moderate volume of distribution (V_ss=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.

Preparation Products And Raw materials

Sar-439859 Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
Nanjing Chemlin Chemical Co., Ltd	025-83697070 13770331960	info@chemlin.com.cn	China	16307	64
ShangHai Caerulum Pharma Discovery Co., Ltd.	18149758185 18149758185	sales-cpd@caerulumpharma.com	China	3493	58
Hygeia (Chengdu) pharmaceutical technique Co., Ltd	028-84502008 13568869383	sales@hygeiapharm.com	China	294	55
Shanghai Lollane Biological Technology Co.,Ltd.	021-52996696，15000506266 15000506266		China	4864	55
Shanghai YuanYe Biotechnology Co., Ltd.	18916372613	yanzihan@shyuanye.com	China	87240	60
ShangHai Biochempartner Co.,Ltd	177-54423994 17754423994	2853530910@QQ.com	China	8000	62
Shanghai Rechem science Co., Ltd.	021-31433387 15618786686	sales@rechemscience.com	China	2962	58
Wellman Pharmaceutical Group Limited	15807197853 18971451745	15807197853@163.com	China	3981	58
Shanghai Jinsheng Pharmaceutical Co., Ltd.	1365-13651960330 13651960330	xiangfeixia@jspharmatech.com	China	401	58
Henan Alfachem Co.,Ltd.	0371-55051623 18137891487	3983243027@qq.com	China	9986	58

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