Powder: -20°C for 3 years | In solvent: -80°C for 1 year
UNC2025 (mrx-6313) 是高效的、具有口服活性的、ATP 竞争性的Mer/Flt3双抑制剂,IC50值分别为 0.74 nM 和 0.8 nM。它对MERTK 的选择性比 Axl 高 45 倍(IC50:122 nM;Ki:13.3 nM)。它具有良好的 PK 特性,可用于研究急性白血病。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 343 | 现货 | ||
2 mg | ¥ 497 | 现货 | ||
5 mg | ¥ 828 | 现货 | ||
10 mg | ¥ 1,390 | 现货 | ||
25 mg | ¥ 2,320 | 现货 | ||
50 mg | ¥ 3,960 | 现货 | ||
100 mg | ¥ 5,660 | 现货 | ||
500 mg | ¥ 11,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 869 | 现货 |
产品描述 | UNC2025 (mrx-6313)(IC50 of 0.74 nM and 0.8 nM) is a potent and orally bioavailable dual MER/FLT3 inhibitor. UNC-2025 is about 20-fold selectivity higher than Axl and Tyro3. |
靶点活性 | FLT3:0.8 nM, Mer:0.74 nM |
体外活性 | In 697 B-ALL cells, UNC-2025 potently inhibits Mer phosphorylation with IC50 of 2.7 nM. In A549 NSCLC and Molm-14 AML cell lines, UNC-2025 causes significant inhibition of colony formation dependent on Mer8 and Flt3. [1] In H2228 and H1299 cell lines, UNC-2025 inhibits MERTK oncogenic signaling downstream, such as basal and stimulated pAKT and pERK1/2. In four NSCLC cell lines, UNC-2025 also induces apoptotic cell death, and decreases colony formation. [2] |
体内活性 | In mice bearing 697 acute leukemia tumors, UNC-2025 (3 mg/kg, p.o.) shows good solubility and DMPK properties, and results in effective target inhibition. [1] In mice bearing H2228 or A549 tumors, UNC-2025 (50 mg/kg, p.o.) inhibits tumor growth. [2] |
别名 | mrx-6313, UNC-2025, UNC 2025 |
分子量 | 476.66 |
分子式 | C28H40N6O |
CAS No. | 1429881-91-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
Ethanol: 8 mg/mL(15.59 mM), Heating is recommended.
DMSO: 25 mg/mL(48.72 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
Ethanol / DMSO | 1 mM | 2.0979 mL | 10.4897 mL | 20.9793 mL | 52.4483 mL |
5 mM | 0.4196 mL | 2.0979 mL | 4.1959 mL | 10.4897 mL | |
10 mM | 0.2098 mL | 1.049 mL | 2.0979 mL | 5.2448 mL | |
DMSO | 20 mM | 0.1049 mL | 0.5245 mL | 1.049 mL | 2.6224 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
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。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
UNC2025 1429881-91-3 Angiogenesis Tyrosine Kinase/Adaptors FLT TAM Receptor Inhibitor inhibit FLT3 leukemia CD135 Fms like tyrosine kinase 3 acute mrx-6313 Cluster of differentiation antigen 135 cancer MERTK UNC-2025 UNC 2025 inhibitor