Estrogen receptor modulator 1

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本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

63676-22-2

Estrogen receptor modulator 1 (compound 18) 是一种口服活性选择性雌激素受体(estrogen receptor)调节剂 (SERM)，pIC₅₀为 0.46。Estrogen receptor modulator 1 诱导 Tamoxifen 耐药、激素非依赖性异种移植瘤的消退。

生物活性

Estrogen receptor modulator1 (compound 18) is an orally active and selectiveestrogen receptormodulator (SERM), with apIC₅₀of 0.46.Estrogen receptor modulator1 induces regression of Tamoxifen-resistant, hormone independent xenograft tumors^[1]^[2].

体外研究
(In Vitro)

Estrogen receptor modulator 1 (compound 18) (100 nM; 10 days) inhibits T47D:A18/PKCα and T47D:A18-TAM1 colony formation^[2].
Estrogen receptor modulator 1 (100 nM; 9 days) significantly inhibits the growth of MCF-7:5C cell, and induces apoptosis in these cells 6 days^[2].

Cell Proliferation Assay^[2]

Cell Line:	T47D:A18/PKCα and T47D:A18-TAM1 cells
Concentration:	100 nM
Incubation Time:	10 days
Result:	Inhibit T47D:A18/PKCα and T47D:A18-TAM1 colony formation.

Cell Viability Assay^[2]

Cell Line:	MCF-7:5C cells
Concentration:	100 nM
Incubation Time:	9 days
Result:	Significantly inhibited the growth of MCF-7:5C cells.

体内研究
(In Vivo)

Estrogen receptor modulator 1 (1.5 mg/animal; p.o. ; daily for 2 weeks) results in regression of T47D:A18/PKCα tumors^[2].

Animal Model:	4-6 week old athymic mice (Harlan-Sprague-Dawley)^[2]
Dosage:	1.5 mg/animal
Administration:	p.o. ; daily for 2 weeks
Result:	Significantly reduced tumor volume.

分子量

242.29

性状

Solid

Formula

C₁₄H₁₀O₂S

CAS 号

63676-22-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 100 mg/mL(412.73 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	4.1273 mL	20.6364 mL	41.2729 mL
5 mM	0.8255 mL	4.1273 mL	8.2546 mL
10 mM	0.4127 mL	2.0636 mL	4.1273 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。