貨號	規格	價格	上海	北京	武漢	南京
S80713-2mg	99.8%	￥90.00 S80713-2mg ￥90.00 現貨	4 4	-	-	-
S80713-5mg	99.8%	￥120.00 S80713-5mg ￥120.00 現貨	5 5	-	-	-
S80713-10mg	99.8%	￥220.00 S80713-10mg ￥220.00 現貨	3 3	-	-	-
S80713-25mg	99.8%	￥440.00 S80713-25mg ￥440.00 現貨	6 6	-	-	-
S80713-50mg	≥99%	￥750.00 S80713-50mg ￥750.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively

產品描述：

Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively

靶點：

PKCθ:0.22 nM (Ki);PKCβI:0.64 nM (Ki);PKCα:0.95 nM (Ki);PKCη:1.8 nM (Ki);PKCδ:2.1 nM (Ki);PKCε:3.2 nM (Ki);PKC

體內研究：

The combination therapy results in a significantly enhanced reduction in tumor volume when compared to either Sotrastaurin (AEB071) or BYL719 alone (p=0.049 vs. BYL719 and p=0.022 vs. Sotrastaurin at day 26). There is even a greater effect when compared to vehicle control (p=0.016). Sotrastaurin (STN) treatment of liver donors and orthotopic liver transplantation (OLT) recipients (Gr.I) or of OLT recipients alone (Gr.II) prolongs animal survival, as 9 out of 10 rats in Gr. I, and 6 out of 6 rats in Gr.II survive >14 days. In contrast, only 4 out of 10 control OLT recipients remain alive at day 14 (p<0.01)

參考文獻：

1. Evenou JP, et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. J Pharmacol Exp Ther. 2009 Sep;330(3):792-801. 2. Musi E, et al. The phosphoinositide 3-kinase α selective inhibitor BYL719 enhances the effect of the protein kinase C inhibitor AEB071 in GNAQ/GNA11-mutant uveal melanoma cells. Mol Cancer Ther. 2014 May;13(5):1044-53 3. Kamo N, et al. Sotrastaurin, a protein kinase C inhibitor, ameliorates ischemia and reperfusion injury in rat orthotopic liver transplantation. Am J Transplant. 2011 Nov;11(11):2499-507.

溶解性：

DMSO : ≥ 50 mg/mL (114.03 mM)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.281 ml	11.403 ml	22.806 ml
5 mM	0.456 ml	2.281 ml	4.561 ml
10 mM	0.228 ml	1.14 ml	2.281 ml
50 mM	0.046 ml	0.228 ml	0.456 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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