Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Glasdegib (PF-04449913) 是一种口服具有活力的 smoothened 抑制剂,能够结合到人 SMO(181-787氨基酸位点),IC50=4 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 398 | 现货 | ||
5 mg | ¥ 913 | 现货 | ||
10 mg | ¥ 1,530 | 现货 | ||
25 mg | ¥ 3,220 | 现货 | ||
50 mg | ¥ 4,770 | 现货 | ||
100 mg | ¥ 6,790 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 983 | 现货 |
产品描述 | Glasdegib (PF-04449913) (PF-04449913) is a potent, and orally bioavailable Smoothened (Smo) inhibitor with IC50 of 5 nM. Phase 2. |
靶点活性 | Smo:5 nM |
体外活性 | In vitro microsomal assays, PF-04449913 have high clearance in rat and low clearance in dog and human, without inhibiting any of the major cytochrome P450 isoforms. [1] |
体内活性 | In rat and dog, PF-04449913 shows high clearance, and good oral bioavailability. [1] |
细胞实验 | PF-04449913 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[1]. Normal or BC CML CD34+ cells are plated on confluent mitomycin-C treated SL/M2 cells with vehicle, PF-04449913 (1 μM), Dasatinib (50 nM), or combination treatment. Mouse bone marrow stromal cell lines, M2-10B4 (M2) and SL/SL (SL) are treated with mitomycin-C (1 mg/mL) and plated in a 1:1 mixture at a total concentration of 100,000 cells/mL one day prior to co-culture with 10,000-20,000 CD34+ BC CML or normal progenitors. After 1 week of culture, progenitors are FACS sorted into hematopoietic progenitor assays and colonies are scored at 14 days. To assess survival of normal human hematopoietic stem and progenitor cells, irradiated (20 Gray) OP9 (M2 clone) stromal cells are co-cultured with 50,000 human CD34+ cord blood cells, vehicle or PF-04449913 in AlphaMEM with 20% Hyclone FBS, 1% pen strep glutamine and supplemented with 50 ng/mL SCF, 10 ng/mL thrombopoietin, and 10 ng/mL Flt3 and quantified by weekly FACS analysis[1]. |
别名 | PF-04449913 |
分子量 | 374.44 |
分子式 | C21H22N6O |
CAS No. | 1095173-27-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: < 1 mg/mL (insoluble or slightly soluble)
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
DMSO: 44 mg/mL (117.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.6707 mL | 13.3533 mL | 26.7065 mL | 66.7664 mL |
5 mM | 0.5341 mL | 2.6707 mL | 5.3413 mL | 13.3533 mL | |
10 mM | 0.2671 mL | 1.3353 mL | 2.6707 mL | 6.6766 mL | |
20 mM | 0.1335 mL | 0.6677 mL | 1.3353 mL | 3.3383 mL | |
50 mM | 0.0534 mL | 0.2671 mL | 0.5341 mL | 1.3353 mL | |
100 mM | 0.0267 mL | 0.1335 mL | 0.2671 mL | 0.6677 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。
Glasdegib 1095173-27-5 GPCR/G Protein Stem Cells Hedgehog/Smoothened Smo Inhibitor PF04449913 PF-04449913 inhibit Smoothened PF 04449913 inhibitor