貨號	規格	價格	上海	北京	武漢	南京
S81072-2mg	99.8%	￥400.00 S81072-2mg ￥400.00 現貨	5 5	-	-	-
S81072-5mg	99.8%	￥500.00 S81072-5mg ￥500.00 現貨	6 6	-	-	-
S81072-10mg	99.8%	￥900.00 S81072-10mg ￥900.00 現貨	6 6	-	-	-
S81072-25mg	99.8%	￥1250.00 S81072-25mg ￥1250.00 現貨	6 6	-	-	-
S81072-50mg	≥99%	￥2100.00 S81072-50mg ￥2100.00 2-3天	0 貨期：2-3天	-	-	-
S81072-100mg	≥99%	￥4000.00 S81072-100mg ￥4000.00 2-3天	0 貨期：2-3天	-	-	-

產品介紹

AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo

產品描述：

靶點：

Aurora A:3 nM (IC50);Aurora B:3 nM (IC50);JAK3:1.1 nM (IC50);JAK2:1.2 nM (IC50);ABL(T315I):4 nM (IC50);Flt-3;Apoptosis;?FLT;?JAK;?Bcr-Abl;?AuroraKinase;?Autophagy

體內研究：

In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, AT9283 also exhibits a significantly longer half-life in tumors (2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice. AT9283 (15 mg/kg) and docetaxel (10 mg/kg) alone has modest anti-tumor activity. T9283 at 20 mg/kg and AT9283 (15 or 20 mg/kg) plus docetaxel (10 mg/kg) demonstrate a statistically significant tumor growth inhibition and enhance survival inmouse xenograft model of mantle cell lymphoma. AT9283 (45 mg/kg, i.p.) inhibits tumor growth in mice. Two cycles of AT9283 45 mg/kg 14 hours after drug administration confirm decreased expression of phospho-Histone H3 and Aurora B in treated animals.

參考文獻：

1. Howard S, et al. Fragment-Based Discovery of the Pyrazol-4-yl Urea (AT9283), a Multitargeted Kinase Inhibitor with Potent Aurora Kinase Activity. Journal of Medicinal Chemistry (2009), 52(2), 379-388. 2. Qi W, et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int J Cancer. 2012 Jun 15;130(12):2997-3005. 3. Santo L, et al. Antimyeloma activity of a multitargeted kinase inhibitor, AT9283, via potent Aurora kinase and STAT3 inhibition either alone or in combination with lenalidomide. Clin Cancer Res. 2011 May 15;17(10):3259-71

溶解性：

DMSO : ≥ 100 mg/mL (262.17 mM)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.622 ml	13.108 ml	26.216 ml
5 mM	0.524 ml	2.622 ml	5.243 ml
10 mM	0.262 ml	1.311 ml	2.622 ml
50 mM	0.052 ml	0.262 ml	0.524 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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