貨號	規格	價格	上海	北京	武漢	南京
S80497-2mg	99.1%	￥544.00 S80497-2mg ￥544.00 現貨	10 10	-	-	-
S80497-5mg	99.1%	￥690.00 S80497-5mg ￥690.00 現貨	8 8	-	-	-
S80497-10mg	99.1%	￥1110.00 S80497-10mg ￥1110.00 現貨	6 6	-	-	-
S80497-25mg	99.1%	￥2200.00 S80497-25mg ￥2200.00 現貨	10 10	-	-	-
S80497-100mg	99.1%	￥5440.00 S80497-100mg ￥5440.00 現貨	6 6	-	-	-

產品介紹

SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2

產品描述：

SBI-0206965 is a potent, selective and cell permeable autophagy kinase ULK1 inhibitor with IC50s of 108 nM for ULK1 kinase and 711 nM for the highly related kinase ULK2

靶點：

ULK1:108 nM (IC50);ULK2:711 nM (IC50);Apoptosis;Autophagy

體外研究：

SBI-0206965 (5-20 μM; 24 hours) induces apoptosis of A498 and ACHN cells during starvation. SBI-0206965 (5-20 μM; 24 hours) attenuates the phosphorylation of Ser108 of the AMPK β1 subunit and increases the levels of cleaved Caspase 8 and PARP, markers of apoptosis. Apoptosis Analysis Cell Line: A498 and ACHN cells (starvation medium (EBSS) treatment) Concentration: 5, 10 ,20 μM Incubation Time: 24 hours Result: Induced significant levels of apoptosis. Western Blot Analysis Cell Line: A498 and ACHN cells (EBSS treatment) Concentration: 5, 10, 20?μM Incubation Time: 24 hours Result: Attenuated the phosphorylation of Ser108 of the AMPK β1 subunit and increased the levels of cleaved Caspase 8 and PARP, markers of apoptosis. Autophagy was evaluated by analysis of LC3B and p62.

體內研究：

SBI-0206965 (50?mg/kg; i.p.; once every 3 days for 37 days) inhibites tumour growth and induces apoptosis in A498 xenograft tumours. Animal Model: Six-week-old male BALB/c nude mice (A498 xenograft tumours) Dosage: 50?mg/kg Administration:Intraperitoneal injection; once every three days for 37 days Result: Significantly suppressed tumour growth.

參考文獻：

1. Lu J, et al. Overexpression of ULK1 Represents a Potential Diagnostic Marker for Clear Cell RenalCarcinoma and the Antitumor Effects of SBI-0206965. EBioMedicine. 2018 Aug;34:85-93. 2. Egan DF, et al. Small Molecule Inhibition of the Autophagy Kinase ULK1 and Identification of ULK1 Substrates. Mol Cell. 2015 Jul 16;59(2):285-97.

溶解性：

soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.044 ml	10.218 ml	20.437 ml
5 mM	0.409 ml	2.044 ml	4.087 ml
10 mM	0.204 ml	1.022 ml	2.044 ml
50 mM	0.041 ml	0.204 ml	0.409 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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