货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
V54160-1ml	10mM in DMSO	￥930.00 V54160-1ml ￥930.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

V54160-1ml

10mM in DMSO

￥930.00

货期：3-5天

产品描述：

UNC2025 hydrochloride 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 hydrochloride is >45-fold selectivity for MERTK relative to Axl (IC50= 122 nM; Ki = 13.3 nM). UNC2025 hydrochloride exhibits an excellent PK properties, and can be used for the investigation of acute leukemia

靶点：

IC50: 0.74 nM (Mer); 0.8 nM (Flt3)

体外研究：

UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC50 values of 0.35 nM, 0.46 nM, 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM , 8.18 nM and 364 nM, respectively. UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC50 of 2.7 nM in 697 B-ALL cells. UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC50 of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells. UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells. UNC2025 (14 nM–10 μM; 48 hours) inhibits MERTK signaling and colony-forming potential in a MERTK-expressing patient sample with a 20-fold difference in sensitivity of MERTK-expressing leukemia blasts relative to normal cord or marrow blood mononuclear cells. UNC2025 (25-300 nM; 1 hour) mediates potent and dose-dependent decreases in MERTK phosphorylation/activation in both cell lines and inhibition of MERTK correlated with decreased phosphorylation of previously reported MERTK-dependent signaling components STAT6, AKT, and ERK1/2. Western Blot Analysis Cell Line: 32D Cells Concentration: 0 nM, 3 nM, 10 nM, 20 nM, 30 nM, 100 nM, 1000 nM, 3000 nM Incubation Time: 1 hour Result: Inhibited p-MEK, p-AXL, p-TYRO3 expression. Cell Proliferation Assay Cell Line: Mononuclear cells Concentration: 14 nM–10 μM Incubation Time: 48 hours Result: Showed IC50 values ranged from 9.0 nM to >10 μM with a median I

体内研究：

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. Animal Model: NSG mice injected with 697 B-ALL cells Dosage: 50 or 75 mg/kg Administration: Oral adminstration Result: Delayed the disease progression.

参考文献：

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：

Soluble in DMSO、H2O

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.949 ml	9.744 ml	19.489 ml
5 mM	0.39 ml	1.949 ml	3.898 ml
10 mM	0.195 ml	0.974 ml	1.949 ml
50 mM	0.039 ml	0.195 ml	0.39 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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