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UNC2025 hydrochloride

产品编号 T39474 CAS 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.

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UNC2025 hydrochloride Chemical Structure

UNC2025 hydrochloride, CAS 2070015-17-5

规格	价格/CNY	货期
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	6-8周

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UNC2025 hydrochloride 的其他形式现货产品:

UNC2025 UNC2025 2HCl (1429881-91-3(free base))

其他形式的 UNC2025 hydrochloride:

UNC2025
现货
UNC2025 2HCl (1429881-91-3(free base))
现货

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生物活性

化学信息

存储 & 溶解度

参考文献

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
分子量	513.13
分子式	C28H41ClN6O
CAS No.	2070015-17-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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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.

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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：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 μL，一共给药动物10 只，您使用的配方为5% 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 μL DMSO (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：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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