规格

价格

库存

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 x 10 mM (in DMSO)

¥ 455

现货

生物活性

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	PAK5:18.1 nM(Ki), PAK4:1.3 nM, PAK4:18.7 nM(Ki), PAK6:17.1 nM(Ki), PAK3:99 nM, PAK2:190 nM, PAK1:13.7 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

化学信息

分子量	490.62
分子式	C₂₅H₃₀N₈OS
CAS No.	898044-15-0
Smiles	CN(C)C[C@@H](NC(=O)N1Cc2c(Nc3nc(C)nc4ccsc34)n[nH]c2C1(C)C)c1ccccc1
密度	1.325 g/cm3 (Predicted)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

DMSO: 150 mg/mL (305.74 mM), Sonication is recommended.

Ethanol: 91 mg/mL (185.48 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.73 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0382 mL	10.1912 mL	20.3824 mL	101.9119 mL
5 mM	0.4076 mL	2.0382 mL	4.0765 mL	20.3824 mL
10 mM	0.2038 mL	1.0191 mL	2.0382 mL	10.1912 mL
20 mM	0.1019 mL	0.5096 mL	1.0191 mL	5.0956 mL
50 mM	0.0408 mL	0.2038 mL	0.4076 mL	2.0382 mL
100 mM	0.0204 mL	0.1019 mL	0.2038 mL	1.0191 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

PF-3758309

PF-3758309

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词

PF-3758309

PF-3758309

PF-3758309 相关产品

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词