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UNC2025 hydrochloride

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产品编号 T39474Cas号 2070015-17-5
别名 UNC2025 hydrochloride

UNC2025 hydrochloride is a potent, ATP-competitive, highly orally active Mer/Flt3 inhibitor. It has IC50 values of 0.74 nM and 0.8 nM, respectively, for Mer and Flt3. UNC2025 hydrochloride demonstrates over 45-fold selectivity for MERTK compared to Axl (IC50 = 122 nM; Ki = 13.3 nM). Additionally, UNC2025 hydrochloride exhibits excellent PK properties, making it suitable for investigating acute leukemia.

UNC2025 hydrochloride

UNC2025 hydrochloride

Rating icon 还可以
产品编号 T39474 别名 UNC2025 hydrochlorideCas号 2070015-17-5

UNC2025 hydrochloride is a potent, ATP-competitive, highly orally active Mer/Flt3 inhibitor. It has IC50 values of 0.74 nM and 0.8 nM, respectively, for Mer and Flt3. UNC2025 hydrochloride demonstrates over 45-fold selectivity for MERTK compared to Axl (IC50 = 122 nM; Ki = 13.3 nM). Additionally, UNC2025 hydrochloride exhibits excellent PK properties, making it suitable for investigating acute leukemia.

规格价格库存数量
2 mg
¥ 495
5日内发货
5 mg
¥ 828
5日内发货
10 mg
¥ 1,450
5日内发货
100 mg
¥ 6,650
5日内发货
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实验操作小课堂
常见问题解答
收到化合物后,是否需要称量后配制储备液?
对于小包装,如 1 mg、5 mg、10 mg 等,不建议二次称量。这样会导致化合物损耗,且无法估算。TargetMol 所有产品原装进口,精准称量,您收到后可直接添加相应量溶剂。 对于大包装,如果您需要分批次实验,可每次称量后配制储备液,建议您 10 mg 起称,称量的误差会小一些;当然条件允许,也可以先配制成高浓度母液,分装备用。
抑制剂母液的储存方式?
母液配置完成后,一般储存于 -80℃,可以存 1 年以上。建议多分装几管,避免反复冻融,常用的存于 4 度,可放一周以上。
抑制剂能否用于细胞实验?
可以的,我们的抑制剂都可以用于细胞/体外实验。但有些化合物还没有用于细胞实验的文献,这种情况下,建议您先做预实验,确保研究的可行性。
准备进行动物实验,收到大包装粉末后,如何分装溶解?
根据配制出来的溶液是不是澄清的确定一次性能配多少:如果配制出来是澄清溶液,可以一次性多配制一些,储存于4度冰箱,大概一周配一次,放久了可能会失效;如果配制出来是混悬液,建议每次使用的时候都现配现用。
动物不能耐受 DMSO,给药时 DMSO量应该如何控制?
对于普通的老鼠,DMSO 的浓度应控制在 10% 以下,对于裸鼠、转基因小鼠、耐受性弱的老鼠等,DMSO 浓度需控制在2%以下。对于首次操作的抑制剂,建议先做溶剂阴性对照,确认溶解对动物无非特异性影响。
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产品介绍

生物活性
产品描述
UNC2025 hydrochloride is a potent, ATP-competitive, highly orally active Mer/Flt3 inhibitor. It has IC50 values of 0.74 nM and 0.8 nM, respectively, for Mer and Flt3. UNC2025 hydrochloride demonstrates over 45-fold selectivity for MERTK compared to Axl (IC50 = 122 nM; Ki = 13.3 nM). Additionally, UNC2025 hydrochloride exhibits excellent PK properties, making it suitable for investigating acute leukemia.
靶点活性
FLT3:0.8 nM (IC50), Mer:0.74 nM (IC50)
体外活性
UNC2025 is against FLT3, MER, AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, KIT and Met with IC 50 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[1].

UNC2025 (0-60 nM; 1 hour) mediates potent inhibition of Mer phosphorylation with an IC 50 of 2.7 nM?in 697 B-ALL cells[1].

UNC2025 (0-60 nM; 1 hour) results in decreased phosphorylation of Flt3 with an IC 50 of 14 nM in Flt3-ITD positive Molm-14 acute myeloid leukemia cells[1].UNC2025 (3 nM-3 μM; 1 hour) decreases p-MEK, p-AXL, p-TYRO3 expression as a concentration manner in 32D Cells[1].

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[2].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[2]. Western Blot Analysis[1]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[1]Cell Line: Mononuclear cells Concentration: 14 nM–10 μM Incubation Time: 48 hours Result: Showed IC 50 values ranged from 9.0 nM to >10 μM with a median IC 50 of 2.38 μM. Western Blot Analysis[2]Cell Line: Kasumi-1 AML and 697 B-ALL cells Concentration: 25-300 nM Incubation Time: 48 hours Result: Decresed p-MERTK, p-STAT6, p- AKT and p-ERK1/2 expression as a dose-dependent manner.
体内活性
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 T max , C max , and AUClast 0.50 hour, 1.6 μM, and 9.2 h?μM, respectively[2].

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[2]. Animal Model: NSG mice injected with 697 B-ALL cells[2]Dosage: 50 or 75 mg/kg Administration: Oral adminstration Result: Delayed the disease progression.
别名UNC2025 hydrochloride
化学信息
分子量513.13
分子式C28H41ClN6O
CAS No.2070015-17-5
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

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