货号	规格	价格	上海	北京	珠海	重庆	武汉
S89278-5mg买3赠1	98.40%	￥600.00 S89278-5mg ￥600.00 现货（买3赠1）	6 6	-	-	-	-
S89278-10mg促销	98.40%	￥1040.00 ￥832.00 S89278-10mg ￥832.00 现货	7 7	-	-	-	-
S89278-25mg促销	98.40%	￥1600.00 ￥1280.00 S89278-25mg ￥1280.00 现货	5 5	-	-	-	-
S89278-100mg促销	≥98%	￥4200.00 ￥3360.00 S89278-100mg ￥3360.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

JNJ-63576253 (TRC-253)是一种有效且具有选择性的下一代 androgen receptor (AR) 拮抗剂，IC50 为 6.9 nM。JNJ-63576253 在 WT 和 LBD 突变、enzalutamide耐药的前列腺癌模型中显示出强大的抑制作用

靶点：

Androgen receptor(Cell-free assay):6.9 nM;ndrogenReceptor

体外研究：

JNJ-63576253 can inhibit transcriptional activity in reporter assays, cellular proliferation, and AR downstream target gene expression, as a potent and selective next-generation AR pathway inhibitor.

体内研究：

JNJ-63576253 causes tumor growth inhibition in an enzalutamide-resistant LNCaP F877 L xenograft model.

细胞实验：

Cell lines: HepG2, VCaP, PC3, LNCaP AR/cs, LNCaP F877L Concentrations: 0.0001 μΜ-1.5 μM Incubation Time: 6 h, 24h Method: LNCaP AR/cs, LNCaP F877L, VCaP, and PC3 are seeded at densities of 5,000 or 250 cells per well into 96-well plates and incubated overnight. Following compound treatment, the cells are incubated for 6 days for assessing proliferation. For transcriptional reporter assays, LNCaP reporter lines are seeded at a density of 10,000 cells per well, incubated overnight, then treated for 24 hours with JNJ-63576253 in the presence of 0.1 nmol/L R1881. After treatment, cells are assayed using the SteadyGlo-luciferase Kit.

动物实验：

Animal Models: Castrated male rats (Sprague Dawley;ages 42–45 days) Dosages: 10, 30, 50 mg/kg Administration: p.o.

参考文献：

1. Jonathan R Branch, et al. Discovery of JNJ-63576253, a Next-Generation Androgen Receptor Antagonist Active Against Wild-Type and Clinically Relevant Ligand Binding Domain Mutations in Metastatic Castration-Resistant Prostate Cancer. Mol Cancer Ther. 2021 May;20(5):763-774.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.855 ml	9.277 ml	18.554 ml
5 mM	0.371 ml	1.855 ml	3.711 ml
10 mM	0.186 ml	0.928 ml	1.855 ml
50 mM	0.037 ml	0.186 ml	0.371 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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