貨號	規格	價格	上海	北京	武漢	南京
S81326-2mg	99.9%	￥340.00 S81326-2mg ￥340.00 現貨	4 4	-	-	-
S81326-5mg	99.9%	￥385.00 S81326-5mg ￥385.00 現貨	3 3	-	-	-
S81326-10mg	99.9%	￥610.00 S81326-10mg ￥610.00 現貨	5 5	-	-	-
S81326-25mg	99.9%	￥1290.00 S81326-25mg ￥1290.00 現貨	4 4	-	-	-
S81326-50mg	≥99%	￥2150.00 S81326-50mg ￥2150.00 2-3天	0 貨期：2-3天	-	-	-
S81326-100mg	≥99%	￥3536.00 S81326-100mg ￥3536.00 2-3天	0 貨期：2-3天	-	-	-

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產品介紹

UNC2025 is a potent, ATP-competitive and highly orally active Mer/Flt3 inhibitor with IC50 values of 0.74 nM and 0.8 nM, respectively. UNC2025 is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 exhibits an excellent PK properties, and can be used for the investigation of acute leukemia

產品描述：

靶點：

IC50: 0.74 nM (Mer); 0.8 nM (Flt3);FLT;?TAMReceptor

體內研究：

UNC2025 (intravenous injection or oral adminstration; 3 mg/kg) exhibits an excellent PK properties: low clearance (9.2 mL/min kg), longer half-life (3.8 h), and high oral exposure (100%), it shows Tmax, Cmax, and AUClast 0.50 hour, 1.6 μM, and 9.2 h μM, respectively. UNC2025 (orally adminstration; 50 or 75 mg/kg; 34 and 70 days) mediates a statistically significant dose-dependent reduction in tumor burden relative to vehicle. mediates dose-dependent increases in median survival from 26 days after initiation of treatment in vehicle-treated mice, to 34 and 70 days in mice treated with 50 or 75 mg/kg UNC2025, respectively.

參考文獻：

1. Zhang W, et al. UNC2025, a Potent and Orally Bioavailable MER/FLT3 Dual Inhibitor. J Med Chem. 2014 Aug 28;57(16):7031-41. 2. DeRyckere D, et al. UNC2025, a MERTK Small-Molecule Inhibitor, Is Therapeutically Effective Alone and in Combination with CL14377 in Leukemia Models.Clin Cancer Res. 2017 Mar 15;23(6):1481-1492.

溶解性：

DMSO : 100 mg/mL (209.79 mM; Need ultrasonic)

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	2.098 ml	10.49 ml	20.979 ml
5 mM	0.42 ml	2.098 ml	4.196 ml
10 mM	0.21 ml	1.049 ml	2.098 ml
50 mM	0.042 ml	0.21 ml	0.42 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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