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PF-3758309
別名: PF-03758309
PF-03758309 (PF-03758309) 是一種口服生物利用的，ATP競爭性的p21-activated kinase (PAK)抑制劑，其作用于PAK4的Kd為2.7 nM。PF-3758309 具有抗增殖的作用，在HCT116腫瘤模型中可誘導(dǎo)凋亡。
PF-3758309 Chemical Structure
CAS: 898044-15-0
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
PF-3758309相關(guān)產(chǎn)品
| 相關(guān)靶點 | PAK1 PAK3 PAK2 PAK4 PAK5 PAK6 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | IPA-3 FRAX597 FRAX486 FRAX1036 NVS-PAK1-1 LCH-7749944 | 點擊展開 |
| 相關(guān)化合物庫 | 激酶抑制劑庫 血管生成相關(guān)化合物庫 TGF-beta/Smad信號通路庫 細胞骨架信號通路化合物庫 抗心血管疾病化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | PF-03758309 (PF-03758309) 是一種口服生物利用的，ATP競爭性的p21-activated kinase (PAK)抑制劑，其作用于PAK4的Kd為2.7 nM。PF-3758309 具有抗增殖的作用，在HCT116腫瘤模型中可誘導(dǎo)凋亡。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | PF-3758309對來自不同腫瘤類型的廣泛腫瘤細胞系都具有效力。 | |||||||||||
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | PF-3758309是一種有效的(Kd = 2.7 nM)，ATP競爭性PAK4抑制劑，Ki為18.7 nM。在細胞中，PF-3758309抑制PAK4基質(zhì)GEF-H1 (IC50 = 1.3 nM)的磷酸化作用和腫瘤細胞系的錨定非依賴生長(IC50 = 4.7 nM)。PF-3758309也會抑制內(nèi)源性pGEF-H1在HCT116細胞中的積累。PF-3758309能夠有效抑制A549細胞的分化(IC50 = 20 nM)和錨定非依賴生長(IC50 = 27 nM)。[1] |
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|---|---|---|---|---|
| 激酶實驗 | 磷酸-GEF-H1細胞試驗 | |||
| TR-293-KDG細胞由HEK293細胞得到，被四環(huán)素誘導(dǎo)的PAK4激酶域(氨基酸291-591)穩(wěn)定轉(zhuǎn)染，并持續(xù)表達HA標(biāo)記的GEFH1ΔDH (氨基酸210-921)。TR-293-KDG細胞與PF-3758309培育3小時，在抗-HA抗體包被的平板上被捕獲，用抗-磷酸-S810-GEF-H1抗體檢測，并通過辣根過氧化物酶-山羊抗兔子抗體結(jié)合物定量。 | ||||
| 細胞實驗 | 細胞系 | HEK293T，HCT116，和 SKOV3 細胞 | ||
| 濃度 | ~1 μM | |||
| 孵育時間 | 72小時 | |||
| 方法 | 使用一組癌細胞系測試PF-3758309的性能。第1天，細胞接種于384孔板上。第2天，將化合物加到細胞培養(yǎng)基。細胞在化合物存在下培育3天。第5天，所有培養(yǎng)基質(zhì)從孔中抽吸出來。PF-3758309對細胞增殖的劑量依賴性作用通過CellTiter-Glo 發(fā)光細胞活性檢測 (a,b,c)定量，這是測定培養(yǎng)基中活細胞數(shù)量的直接勻相測定法，基于代謝的活細胞指示劑，ATP存在下的定量。HEK293T，HCT116，和SKOV3細胞顯示的增值數(shù)據(jù)按照制造商指定的Cyquant NF試驗測定。藥物處理72小時后，測定細胞的增殖。每種藥物處理的結(jié)果標(biāo)準(zhǔn)化為載體對照，并表示為相對Bleomycin的最大測定抑制百分比。代表SD的誤差線至少來自三個實驗。 |
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| 實驗圖片 | 檢測方法 | 檢測指標(biāo) | 實驗圖片 | PMID |
| Western blot | PAK4 / PI3K / p-AKT / AKT / p-mTOR / mTOR |
|
28407679 | |
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | PF-3758309阻斷多種人類腫瘤異種移植物的生長，在大多敏感的模型中，血漿EC50值為0.4 nM。在HCT116腫瘤模型中，PF-3758309能夠抗增殖并誘導(dǎo)細胞凋亡。[1] |
|
|---|---|---|
| 動物實驗 | Animal Models | 移植瘤裸鼠模型 |
| Dosages | 7.5-30 毫克/千克 BID | |
| Administration | 口服 | |
化學(xué)信息&溶解度
| 分子量 | 490.62 | 分子式 | C25H30N8OS |
| CAS號 | 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 | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 98 mg/mL ( (199.74 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 98 mg/mL (199.74 mM) Water : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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常見問題及建議解決方法
問題 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/.
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