SAR439859

Dangerous Goods

CAS number：2114339-57-8 molecular formula：C31H30Cl2FNO3

overview

Specs

numbering system

physicochemical properties

Safety information

Production methods and uses

MSDS

overview

compound introduction

Information SAR439859 (compound 43d) is an orally available and nonsteroidal selectiveestrogen receptordegrader (SERD) with potential antineoplastic activity. SAR439859 is a potentestrogen receptor (ER)antagonist with EC50 of 0.2 nM for ERα degradation. Targets ERα (Cell-free assay) 0.2 nM(EC50) In vitro SAR439859 is a novel, orally bioavailable SERD with potent antagonist and degradation activities against both wild-type and mutant Y537S ER. Driven by its fluoropropyl pyrrolidinyl side chain, SAR439859 has demonstrated broader and superior ER antagonist and degrader activities across a large panel of ER+ cells, including inhibition of ER signaling and tumor cell growth. In vivo SAR439859 shows promising antitumor activity in breast cancer mice xenograft models. In vivo treatment with SAR439859 demonstrates significant tumor regression in ER+ breast cancer models, including MCF7-ESR1 wild-type and mutant-Y537S mouse tumors, and HCI013, a patient-derived tamoxifen-resistant xenograft tumor. Cell Research(from reference) Cell lines：LCC2 cells, MCF7 cells Concentrations：0.01-1000 nM Incubation Time：7 days, 4 hours

Specs

Chinese alias	-
English alias	AMCENESTRANT [WHO-DD] \| AMCENESTRANT [JAN] \| MS-30114 \| WHO 11312 \| AKOS040737414 \| SCHEMBL19131426 \| Amcenestrant [USAN] \| Q66885452 \| NSC-827675 \| 6-(2,4-dichlorophenyl)-5-[4-[(3~{S})-1-(3-fluoranylpropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7~{H}-ben
CAS number	2114339-57-8	molecular formula	C31H30Cl2FNO3
molecular weight	554.48 g/mol	Exact mass	≥98%
PSA	49.800 Å²	logp	4.73

numbering system

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physicochemical properties

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Safety information

pictogram：

GHS07

Signal word：

Warning

Hazard Statement：

H315: 引起皮肤刺激 H319: 引起严重眼睛刺激 H335: 可能引起呼吸道刺激 H302: 吞食有害

Statement of Preventive Measures：

P261: 避免吸入灰尘/烟雾/气体/雾/蒸汽/喷雾 P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P302+P352: 如皮肤沾染：用水充分清洗。 P301+P312: 如误吞咽：如感觉不适，呼叫急救中心/医生。