Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sonidegib diphosphate (LDE225 diphosphate) 是 Smo 的选择性拮抗剂,能够抑制鼠 Smo (IC50:1.3 nM)和人 Smo (IC50:2.5 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 413 | 现货 | ||
10 mg | ¥ 497 | 现货 | ||
25 mg | ¥ 766 | 现货 | ||
50 mg | ¥ 997 | 现货 | ||
100 mg | ¥ 1,810 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 621 | 现货 |
产品描述 | Sonidegib diphosphate (LDE225 diphosphate) is an effective and selective Smo antagonist (IC50: 1.3 nM and 2.5 nM for mouse and human Smo in a binding assay, respectively). |
靶点活性 | Smo:2.5 nM (IC50), Smo (mouse):1.3 nM (IC50) |
体外活性 | Erismodegib diphosphate, a small molecule, clinically investigated SMO inhibitor. Erismodegib diphosphate is used alone and in combination with Nilotinib, inhibits the Hh pathway in CD34+ chronic phase (CP)-chronic myeloid leukaemia (CML) cells, reducing the number and self-renewal capacity of CML leukaemia stem cell (LSC). In a similar fashion to cyclopamine, Erismodegib interacts directly with SMO, to reduce the expression of downstream Hh signaling targets. The IC50 values for Erismodegib diphosphate for the major human CYP450 drug-metabolizing enzymes are greater than 10 μM. Primary CD34+ CP-CML cells are cultured in serum-free media (SFM)±Erismodegib for 6, 24, and 72 hours (h). At 72 h, while there is variability between the biological samples, GLI1 is obviously downregulated following exposure to Erismodegib (10 nM; 0.78-fold and 100 nM; 0.73-fold, respectively (p<0.01)[2]. |
体内活性 | Erismodegib diphosphate is a weak base with a measured pKa of 4.2 and exhibits relatively poor aqueous solubility. Erismodegib diphosphate demonstrates dose-related antitumor activity after 10 days of oral administration of a suspension of the diphosphate salt, in the subcutaneous Ptch+/-p53-/- medulloblastoma allograft mouse model. Bone marrow cells and spleen cells from a subset of treated mice are transplanted into secondary recipient mice. Erismodegib diphosphate (5 mg/kg/day; once daily) obviously inhibits tumor growth, corresponding to a T/C value of 33% (p<0.05 as compared to vehicle controls). Erismodegib affords 51 and 83% regression respectively when dosed at 10 and 20 mg/kg/day qd [1]. Transplantation of either bone marrow (BM) or spleen cells from mice treated with Erismodegib diphosphate+ Nilotinib results in reduced white cell count (WCC) and reduces leukaemia development in secondary recipients compared to Erismodegib or Nilotinib alone[2]. |
别名 | NVP-LDE 225 diphosphate, Erismodegib diphosphate, LDE225 diphosphate |
分子量 | 681.49 |
分子式 | C26H32F3N3O11P2 |
CAS No. | 1218778-77-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 99 mg/mL(145.27 mM)
H2O: Insoluble
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.4674 mL | 7.3369 mL | 14.6737 mL | 36.6843 mL |
5 mM | 0.2935 mL | 1.4674 mL | 2.9347 mL | 7.3369 mL | |
10 mM | 0.1467 mL | 0.7337 mL | 1.4674 mL | 3.6684 mL | |
20 mM | 0.0734 mL | 0.3668 mL | 0.7337 mL | 1.8342 mL | |
50 mM | 0.0293 mL | 0.1467 mL | 0.2935 mL | 0.7337 mL | |
100 mM | 0.0147 mL | 0.0734 mL | 0.1467 mL | 0.3668 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。
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