货号	规格	价格	上海	北京	珠海	重庆	武汉
S81536-2mg买3赠1	99.60%	￥450.00 S81536-2mg ￥450.00 现货（买3赠1）	5 5	-	-	-	-
S81536-5mg买3赠1	99.60%	￥570.00 S81536-5mg ￥570.00 现货（买3赠1）	5 5	-	-	-	-
S81536-10mg买3赠1	99.60%	￥780.00 S81536-10mg ￥780.00 现货（买3赠1）	5 5	-	-	-	-
S81536-25mg买3赠1	99.60%	￥1340.00 S81536-25mg ￥1340.00 现货（买3赠1）	5 5	-	-	-	-
S81536-50mg买3赠1	≥99%	￥2270.00 S81536-50mg ￥2270.00 2-3天（买3赠1）	0 货期：2-3天	-	-	-	-
S81536-100mg	≥99%	￥3870.00 S81536-100mg ￥3870.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Danusertib is a pyrrolo-pyrazole and aurora kinase inhibitor with IC50 of 13, 79, and 61 nM for Aurora A, B, and C, respectively.

靶点：

Aurora A:13 nM (IC50);Aurora B:79 nM (IC50);Aurora C:61 nM (IC50);FGFR; Trkreceptor; c-RET; Bcr-Abl; AuroraKinase; Autophagy

体内研究：

PHA-739358 (15 mg/kg twice a day, i.p.) and IM are well tolerated, and significantly inhibit proliferation of K562 cells andvirtually suppressed tumor growth during the 10-day treatment period. In a subcutaneous murine xenograft model, danusertibsertib (2×15 mg/kg/d, i.p.) significantly reduces tumor growth in vivo compared with controls or mice treated with streptozotocine/5-fluorouracil

参考文献：

1. Zi D, et al. Danusertib Induces Apoptosis, Cell Cycle Arrest, and Autophagy but Inhibits Epithelial to Mesenchymal Transition Involving PI3K/Akt/mTOR Signaling Pathway in Human Ovarian Cancer Cells. Int J Mol Sci. 2015 Nov 13;16(11):27228-51. 2. Gontarewicz A, et al. Simultaneous targeting of Aurora kinases and Bcr-Abl kinase by the small molecule inhibitor PHA-739358 is effective against imatinib-resistant BCR-ABL mutations including T315I. Blood. 2008 Apr 15;111(8):4355-64. 3. Fraedrich K, et al. Targeting Aurora Kinases with Danusertib (PHA-739358) Inhibits Growth of Liver Metastases from Gastroenteropancreatic Neuroendocrine Tumors in an Orthotopic Xenograft Model. Clin Cancer Res. 2012 Sep 1;18(17):4621-32. Epub 2012 Jul 2.

溶解性：

DMSO : 50 mg/mL (105.36 mM; Need ultrasonic)

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.107 ml	10.536 ml	21.073 ml
5 mM	0.421 ml	2.107 ml	4.215 ml
10 mM	0.211 ml	1.054 ml	2.107 ml
50 mM	0.042 ml	0.211 ml	0.421 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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