Name: PF-3758309
Brand: TargetMol
SKU: T6626
Price: 193 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

1 mg

¥ 193

In stock

5 mg

¥ 412

In stock

10 mg

¥ 663

In stock

25 mg

¥ 1,180

In stock

50 mg

¥ 1,980

In stock

100 mg

¥ 3,390

In stock

1 mL x 10 mM (in DMSO)

¥ 455

In stock

产品介绍

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

溶解度信息

DMSO: 91 mg/mL (185.48 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

DMSO/Ethanol

	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

体内实验配液计算器

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 ， TargetMol | Animal experiments

一共给药动物 10 只 ，您使用的配方为 5% TargetMol | reagent

DMSO+ 30%PEG300+ 5%Tween 80 + 60%Saline/PBS/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 μLDMSO TargetMol | reagent

（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 50μLDMSO TargetMol | reagent

母液，添加 300 μLPEG300 TargetMol | reagent

混匀澄清，再加 50μLTween 80, 混匀澄清，再加 600μLSaline/PBS/ddH₂O TargetMol | reagent

混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如： DMSO， PEG300/ PEG400， Tween 80， SBE-β-CD，玉米油等，均可在TargetMol网站点击购买。

PF-3758309

PF-3758309

产品介绍

计算器

体内实验配液计算器

剂量转换

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