貨號	規格	價格	上海	北京	武漢	南京
S80238-1mg	99.0%	￥120.00 S80238-1mg ￥120.00 現貨	10 10	-	-	-
S80238-2mg	99.0%	￥220.00 S80238-2mg ￥220.00 現貨	10 10	-	-	-
S80238-5mg	99.0%	￥500.00 S80238-5mg ￥500.00 現貨	9 9	-	-	-
S80238-10mg	99.0%	￥800.00 S80238-10mg ￥800.00 現貨	10 10	-	-	-
S80238-25mg	≥99%	￥1700.00 S80238-25mg ￥1700.00 2-3天	0 貨期：2-3天	-	-	-
S80238-50mg	≥99%	￥2800.00 S80238-50mg ￥2800.00 2-3天	0 貨期：2-3天	-	-	-
S80238-100mg	≥99%	￥4500.00 S80238-100mg ￥4500.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.

產品描述：

Molibresib (I-BET762; GSK525762) is a BET bromodomain inhibitor with IC50 of 32.5-42.5 nM.

靶點：

IC50: 32.5-42.5 nM (BET);EpigeneticReaderDomain

體內研究：

The antimyeloma activity of Molibresib (I-BET 762) is tested dosed orally in an in vivo systemic xenograft model generated by injecting OPM-2 cells into NOD-SCID mice. Daily oral doses of Molibresib up to 10 mg/kg and 30 mg/kg given every other day are well tolerated with no clear impact on body weight compared with vehicle control. The plasma hLC concentration is significantly reduced in mice treated with Molibresib

參考文獻：

1. Nicodeme E, et al. Suppression of inflammation by a synthetic histone mimic. Nature. 2010 Dec 23;468(7327):1119-23. 2. Asangani IA, et al. Therapeutic targeting of BET bromodomain proteins in castration-resistant prostate cancer. Nature. 2014 Jun 12;510(7504):278-82. 3. Chaidos A, et al. Potent antimyeloma activity of the novel bromodomain inhibitors I-BET151 and I-BET762. Blood. 2014 Jan 30;123(5):697-705.

溶解性：

DMSO : 200 mg/mL (471.81 mM; Need ultrasonic) 1M HCl : 100 mg/mL (235.90 mM; ultrasonic and adjust pH to 1 with HCl)

保存條件：

2-8℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.359 ml	11.795 ml	23.59 ml
5 mM	0.472 ml	2.359 ml	4.718 ml
10 mM	0.236 ml	1.18 ml	2.359 ml
50 mM	0.047 ml	0.236 ml	0.472 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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GSK 525762A