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PF-3758309
别名: PF-03758309
PF-03758309 (PF-03758309) 是一种口服生物利用的，ATP竞争性的p21-activated kinase (PAK)抑制剂，其作用于PAK4的Kd为2.7 nM。PF-3758309 具有抗增殖的作用，在HCT116肿瘤模型中可诱导凋亡。
PF-3758309 Chemical Structure
CAS: 898044-15-0
产品质控
批次：
纯度：
99.98%
99.98
PF-3758309相关产品
| 相关靶点 | PAK1 PAK3 PAK2 PAK4 PAK5 PAK6 | 点击展开 |
|---|---|---|
| 相关产品 | IPA-3 FRAX597 FRAX486 FRAX1036 LCH-7749944 NVS-PAK1-1 | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 血管生成相关化合物库 TGF-beta/Smad信号通路库 细胞骨架信号通路化合物库 抗心血管疾病化合物库 | 点击展开 |
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息(PMID) |
|---|---|---|---|---|---|
| human MDA-MB-436 cells | Cytotoxic assay | 24-48 h | Cytotoxicity against human MDA-MB-436 cells assessed as reduction in cell viability after 24 to 48 hrs by Celltiter-glo luminescence assay, IC50=0.79 nM | 24432870 | |
| HCT116 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by CCK8 assay, IC50=0.039μM. | 29886323 | |
| A549 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay, IC50=0.463μM. | 29886323 | |
| TC32 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| U-2 OS | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 29435139 | ||
| Saos-2 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| BT-12 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| Rh18 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 29435139 | ||
| OHS-50 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| fibroblast cells | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 29435139 | ||
| Rh41 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 29435139 | ||
| A673 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| BT-12 | qHTS of pediatric cancer cell lines to identify multiple opportunities for | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | PF-03758309 (PF-03758309) 是一种口服生物利用的，ATP竞争性的p21-activated kinase (PAK)抑制剂，其作用于PAK4的Kd为2.7 nM。PF-3758309 具有抗增殖的作用，在HCT116肿瘤模型中可诱导凋亡。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | PF-3758309对来自不同肿瘤类型的广泛肿瘤细胞系都具有效力。 | |||||||||||
| 靶点 |
|
| 体外研究(In Vitro) | ||||
| 体外研究活性 | PF-3758309是一种有效的(Kd = 2.7 nM)，ATP竞争性PAK4抑制剂，Ki为18.7 nM。在细胞中，PF-3758309抑制PAK4基质GEF-H1 (IC50 = 1.3 nM)的磷酸化作用和肿瘤细胞系的锚定非依赖生长(IC50 = 4.7 nM)。PF-3758309也会抑制内源性pGEF-H1在HCT116细胞中的积累。PF-3758309能够有效抑制A549细胞的分化(IC50 = 20 nM)和锚定非依赖生长(IC50 = 27 nM)。[1] |
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|---|---|---|---|---|
| 激酶实验 | 磷酸-GEF-H1细胞试验 | |||
| TR-293-KDG细胞由HEK293细胞得到，被四环素诱导的PAK4激酶域(氨基酸291-591)稳定转染，并持续表达HA标记的GEFH1ΔDH (氨基酸210-921)。TR-293-KDG细胞与PF-3758309培育3小时，在抗-HA抗体包被的平板上被捕获，用抗-磷酸-S810-GEF-H1抗体检测，并通过辣根过氧化物酶-山羊抗兔子抗体结合物定量。 | ||||
| 细胞实验 | 细胞系 | HEK293T，HCT116，和 SKOV3 细胞 | ||
| 浓度 | ~1 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 使用一组癌细胞系测试PF-3758309的性能。第1天，细胞接种于384孔板上。第2天，将化合物加到细胞培养基。细胞在化合物存在下培育3天。第5天，所有培养基质从孔中抽吸出来。PF-3758309对细胞增殖的剂量依赖性作用通过CellTiter-Glo 发光细胞活性检测 (a,b,c)定量，这是测定培养基中活细胞数量的直接匀相测定法，基于代谢的活细胞指示剂，ATP存在下的定量。HEK293T，HCT116，和SKOV3细胞显示的增值数据按照制造商指定的Cyquant NF试验测定。药物处理72小时后，测定细胞的增殖。每种药物处理的结果标准化为载体对照，并表示为相对Bleomycin的最大测定抑制百分比。代表SD的误差线至少来自三个实验。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | PAK4 / PI3K / p-AKT / AKT / p-mTOR / mTOR |
|
28407679 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | PF-3758309阻断多种人类肿瘤异种移植物的生长，在大多敏感的模型中，血浆EC50值为0.4 nM。在HCT116肿瘤模型中，PF-3758309能够抗增殖并诱导细胞凋亡。[1] |
|
|---|---|---|
| 动物实验 | Animal Models | 移植瘤裸鼠模型 |
| Dosages | 7.5-30 毫克/千克 BID | |
| Administration | 口服 | |
|
化学信息&溶解度
| 分子量 | 490.62 | 分子式 | C25H30N8OS |
| CAS号 | 898044-15-0 | SDF | Download PF-3758309 SDF |
| Smiles | CC1=NC2=C(C(=N1)NC3=NNC4=C3CN(C4(C)C)C(=O)NC(CN(C)C)C5=CC=CC=C5)SC=C2 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 98 mg/mL ( (199.74 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 98 mg/mL (199.74 mM) Water : Insoluble |
摩尔浓度计算器 |
|
体内溶解配方 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | |||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 1:
If this compound crosses the blood brain barrier?
回答：
We're sorry we don't have any data on whether S7094 can cross BBB or not, the following reference indicate that it can not: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3490962/.
