Powder: -20°C for 3 years | In solvent: -80°C for 1 year
LDC1267 是一种特异性 TAM(Tyro3, Axl and Mer) 激酶抑制剂,能够作用于 Mer( IC50<5 nM)、Tyro3(IC50:8 nM) 和 Axl(IC50:29 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 338 | 现货 | ||
2 mg | ¥ 482 | 现货 | ||
5 mg | ¥ 822 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,430 | 现货 | ||
50 mg | ¥ 3,630 | 现货 | ||
100 mg | ¥ 5,230 | 现货 | ||
500 mg | ¥ 10,900 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 987 | 现货 |
产品描述 | LDC1267 is a excellently specific TAM(Tyro3, Axl and Mer) kinase inhibitor, for Mer( IC50<5 nM), Tyro3(IC50=8 nM), and Axl(IC50=29 nM). |
靶点活性 | Tyro3:8 nM, Mer:<5 nM, Axl:29 nM |
体外活性 | 在负荷B16F10黑素瘤的小鼠体内, 腹腔内注射LDC1267(20 mg/kg)具有较高的安全性,能够抑制肿瘤代谢,增强具有抗转移NK细胞的活性. |
体内活性 | 在多种的细胞系中,LDC1267对于细胞产生抑制增殖的作用,IC50 >5 μM。在NKG2D激活的NK细胞中,LDC1267能够阻断由Gas6刺激引起的抑制作用。 |
激酶实验 | Kinase binding assays: For optimization of Axl/TAM receptor inhibitors, an Axl binding assay is established (HTRF method; Kinase tracer 236). This assay is based on the binding and displacement of the Alexa Fluor 647-labelled Kinase tracer 236 to each glutathione S-transferase (GST)-tagged kinase used in the binding assay. Binding of the tracer to the kinase was detected by using europium (Eu)-labelled anti-GST antibodies. Simultaneous binding of both the fluorescent tracer and the Eu-labelled antibodies to the GST-tagged kinase generates a fluorescence resonance energy transfer (FRET) signal. Binding of inhibitor to the kinase competes for binding with the tracer, resulting in a loss of the FRET signal. For the assay, the compound is diluted in 20?mM HEPES, pH?8.0, 1?mM DTT, 10?mM MgCl2 and 0.01% Brij35. Then, the kinase of interest (5?nM final concentration), fluorescent tracer (15?nM final concentration) and LanthaScreen Eu-anti-GST antibody (2?nM final concentration) are mixed with the respective compound dilutions (from 5?nM to 10?μM) and incubated for 1?h. The FRET signal is quantified using an EnVision Multilabellreader 2104. |
细胞实验 | After incubation for 72?hours with LDC1267, CellTiterGlow reagent is used to determine the proliferation relative to the corresponding DMSO control.(Only for Reference) |
分子量 | 560.55 |
分子式 | C30H26F2N4O5 |
CAS No. | 1361030-48-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (165.9 mM)
Ethanol: 2 mg/mL (3.56 mM), Heating is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.784 mL | 8.9198 mL | 17.8396 mL | 44.5991 mL |
DMSO | 5 mM | 0.3568 mL | 1.784 mL | 3.5679 mL | 8.9198 mL |
10 mM | 0.1784 mL | 0.892 mL | 1.784 mL | 4.4599 mL | |
20 mM | 0.0892 mL | 0.446 mL | 0.892 mL | 2.23 mL | |
50 mM | 0.0357 mL | 0.1784 mL | 0.3568 mL | 0.892 mL | |
100 mM | 0.0178 mL | 0.0892 mL | 0.1784 mL | 0.446 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。
LDC1267 1361030-48-9 Tyrosine Kinase/Adaptors TAM Receptor LDC-1267 LDC 1267 Tyro3 Inhibitor inhibit Axl Mer inhibitor