貨號	規格	價格	上海	北京	武漢	南京
S84202-1mg	99.9%	￥400.00 S84202-1mg ￥400.00 現貨	5 5	-	-	-
S84202-5mg	99.9%	￥1230.00 S84202-5mg ￥1230.00 現貨	5 5	-	-	-
S84202-10mg	99.9%	￥1400.00 S84202-10mg ￥1400.00 現貨	6 6	-	-	-
S84202-50mg	99.9%	￥1700.00 S84202-50mg ￥1700.00 現貨	1 1	-	-	-
S84202-100mg	≥99%	￥2900.00 S84202-100mg ￥2900.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

ARV-771 是一種有效的 pan-(bromodomain and extra-terminal)BET 降解劑，一種新型的BET-PROTAC(proteolysis-targeting chimera)，對于BRD2(1)、BRD2(2)、BRD3(1)、BRD3(2)、BRD4(1) 和 BRD4(2)的Kd值分別為34 nM、4.7 nM、8.3 nM、7.6 nM、9.6 nM 和 7.6 nM。

產品描述：

靶點：

BRD2-BD2(Cell-free assay):4.7 nM(Kd); BRD3-BD2(Cell-free assay):7.6 nM(Kd); BRD4-BD2(Cell-free assay):7.6 nM(Kd); BRD3-BD1(Cell-free assay):8.3 nM(Kd); BRD4-BD1(Cell-free assay):9.6 nM(Kd); BRD2-BD1:34 Nm;EpigeneticReaderDomain

體外研究：

ARV-771 is a potent small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. ARV-771 treatment of CRPC cells results in apoptosis

體內研究：

ARV-771 induces degradation in vivo. ARV-771 results in suppression of both AR signaling and AR levels and leads to tumor regression in a CRPC mouse xenograft model.

細胞實驗：

Cell lines: 22Rv1 cells, VCaP cells, LnCaP95 cells Concentrations: 1-300 nM Incubation Time: 24 h, 72 h Method: c-MYC ELISA. 22Rv1 cells (30,000 cells per well) were dosed with ARV-771 serially diluted at 1:3 ratio for an eight-point dose curve. AR ELISA. VCaP cells (40,000 cells per well) were dosed with ARV-771 serially diluted at 1:3 ratio for an eight-point dose curve. Cell Proliferation Assay Protocol. 22Rv1 cells (5,000 cells per well) were dosed with ARV-771 serially diluted 1:3 for a 10-point dose curve for 72 h.

動物實驗：

Animal Models: Mice implanted subcutaneously with 5 × 106 22Rv1 or VCaP cells Dosages: 30 mg/kg Administration: IH/SC

參考文獻：

1. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9.

溶解性：

Soluble in DMSO、Ethanol

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	1.014 ml	5.068 ml	10.135 ml
5 mM	0.203 ml	1.014 ml	2.027 ml
10 mM	0.101 ml	0.507 ml	1.014 ml
50 mM	0.02 ml	0.101 ml	0.203 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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