Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-3758309 (PF-03758309) 是一种可口服的、可逆的 ATP 竞争性 PAK4抑制剂。它是一种 PAK4 抑制剂,可抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 193 | 现货 | ||
5 mg | ¥ 412 | 现货 | ||
10 mg | ¥ 663 | 现货 | ||
25 mg | ¥ 1,180 | 现货 | ||
50 mg | ¥ 1,980 | 现货 | ||
100 mg | ¥ 3,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 455 | 现货 |
产品描述 | PF-3758309 (PF-03758309) (IC50=1.3 nM), a pyrrolopyrazole inhibitor of PAK4, has effective ATP-competition. |
靶点活性 | PAK3:99 nM, PAK4:1.3 nM, PAK4:18.7 nM(Ki), PAK6:17.1 nM(Ki), PAK5:18.1 nM(Ki) |
体外活性 | PF-3758309 (Kd = 2.7 nM), an effective inhibitor of PAK4 (Ki=18.7 nM), has ATP competition. PF-3758309 (IC50 = 1.3 nM) inhibits phosphorylation of the PAK4 substrate GEF-H1 in cells. In the tumor cell, PF-3758309(IC50 = 4.7 nM) grows in a linesanchorage-independent manner. In HCT116 cells, PF-3758309 inhibits endogenous pGEF-H1 accumulation. In A549 cells, PF-3758309 effectively inhibits cellular proliferation in IC50 of 20 nM and anchorage-independent growth in IC50 of 27 nM. |
体内活性 | In the HCT116 tumor model, PF-3758309 act as an antiproliferative inducing apoptosis. In the sensitive model, PF-3758309 (EC50=0.4 nM) blocks the growth of multiple human tumor xenografts. |
激酶实验 | In phospho-GEF-H1 cellular assay, TR-293-KDG cells are incubated for 3 hours with PF-3758309. TR-293-KDG cells were captured on an anti-HA antibody-coated plate, which is detected with an anti-phospho-S810-GEF-H1 antibody, and quantified with a horseradish peroxidase-goat anti-rabbit antibody conjugate. TR-293-KDG cells are constructed from HEK293 cells, which is transfected with tetracycline-inducible PAK4-kinase domain (amino acids 291-591) and expressed HA-tagged GEFH1ΔDH (amino acids 210-921). |
细胞实验 | HEK293T, HCT116, and SKOV3 cells are plated on 384-well plates for 24 hours culture. PF-3758309( ~1 μM) is added to the cell culture incubating 72 hours. After drug treatment,cell proliferation and other indicators of metabolism are measured. |
动物实验 | Nude mice with Xenograft tumors were orally fed with PF-3758309(7.5-30 mg/kg BID)dissolved in 0.5% methylcellulose. |
别名 | PF-309, PF-03758309, PF 3758309 |
分子量 | 490.62 |
分子式 | C25H30N8OS |
CAS No. | 898044-15-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 91 mg/mL (185.5 mM)
Ethanol: 91 mg/mL (185.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 2.0382 mL | 10.1912 mL | 20.3824 mL | 50.9559 mL |
5 mM | 0.4076 mL | 2.0382 mL | 4.0765 mL | 10.1912 mL | |
10 mM | 0.2038 mL | 1.0191 mL | 2.0382 mL | 5.0956 mL | |
20 mM | 0.1019 mL | 0.5096 mL | 1.0191 mL | 2.5478 mL | |
50 mM | 0.0408 mL | 0.2038 mL | 0.4076 mL | 1.0191 mL | |
100 mM | 0.0204 mL | 0.1019 mL | 0.2038 mL | 0.5096 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。
PF-3758309 898044-15-0 Apoptosis Cytoskeletal Signaling PAK PF-309 proliferation tumor oncogenic PF-03758309 PF 3758309 survival PF03758309 inhibit p21 activated kinases signaling ATP-competitive PF 309 PF 03758309 Inhibitor PF3758309 growth PF309 inhibitor