PF-3758309

別名: PF-03758309

目錄號(hào)：S7094 Purity: 99.98%

PF-03758309 (PF-03758309) 是一種口服生物利用的，ATP競(jìng)爭(zhēng)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

規(guī)格	價(jià)格	庫存
10mM (1mL in DMSO)	958.23	現(xiàn)貨
10mg	899.25	現(xiàn)貨
50mg	2757.17	現(xiàn)貨
200mg	6936.93	現(xiàn)貨
1g	30212.91	現(xiàn)貨
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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(diǎn)	PAK1 PAK3 PAK2 PAK4 PAK5 PAK6	點(diǎn)擊展開
相關(guān)產(chǎn)品	IPA-3 FRAX597 FRAX486 FRAX1036 LCH-7749944 NVS-PAK1-1	點(diǎn)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(hào)通路庫細(xì)胞骨架信號(hào)通路化合物庫抗心血管疾病化合物庫	點(diǎn)擊展開

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類型	孵育時(shí)間	活性描述	文獻(xiàn)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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

特性

PF-3758309對(duì)來自不同腫瘤類型的廣泛腫瘤細(xì)胞系都具有效力。

靶點(diǎn)

PAK1 (Cell-free assay)	PAK6 (Cell-free assay)	PAK5 (Cell-free assay)	PAK4 (Cell-free assay)	PAK3 (Cell-free assay)	點(diǎn)擊更多
13.7 nM(Ki)	17.1 nM(Ki)	18.1 nM(Ki)	18.7 nM(Ki)	99 nM	點(diǎn)擊更多

體外研究(In Vitro)
體外研究活性	PF-3758309是一種有效的(K_d = 2.7 nM)，ATP競(jìng)爭(zhēng)性PAK4抑制劑，K_i為18.7 nM。在細(xì)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(xì)胞系的錨定非依賴生長(IC50 = 4.7 nM)。PF-3758309也會(huì)抑制內(nèi)源性pGEF-H1在HCT116細(xì)胞中的積累。PF-3758309能夠有效抑制A549細(xì)胞的分化(IC50 = 20 nM)和錨定非依賴生長(IC50 = 27 nM)。
激酶實(shí)驗(yàn)	磷酸-GEF-H1細(xì)胞試驗(yàn)
激酶實(shí)驗(yàn)	TR-293-KDG細(xì)胞由HEK293細(xì)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(dá)HA標(biāo)記的GEFH1ΔDH (氨基酸210-921)。TR-293-KDG細(xì)胞與PF-3758309培育3小時(shí)，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(cè)，并通過辣根過氧化物酶-山羊抗兔子抗體結(jié)合物定量。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	HEK293T，HCT116，和 SKOV3 細(xì)胞
	濃度	~1 μM
	孵育時(shí)間	72小時(shí)
	方法	使用一組癌細(xì)胞系測(cè)試PF-3758309的性能。第1天，細(xì)胞接種于384孔板上。第2天，將化合物加到細(xì)胞培養(yǎng)基。細(xì)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(duì)細(xì)胞增殖的劑量依賴性作用通過CellTiter-Glo 發(fā)光細(xì)胞活性檢測(cè) (a,b,c)定量，這是測(cè)定培養(yǎng)基中活細(xì)胞數(shù)量的直接勻相測(cè)定法，基于代謝的活細(xì)胞指示劑，ATP存在下的定量。HEK293T，HCT116，和SKOV3細(xì)胞顯示的增值數(shù)據(jù)按照制造商指定的Cyquant NF試驗(yàn)測(cè)定。藥物處理72小時(shí)后，測(cè)定細(xì)胞的增殖。每種藥物處理的結(jié)果標(biāo)準(zhǔn)化為載體對(duì)照，并表示為相對(duì)Bleomycin的最大測(cè)定抑制百分比。代表SD的誤差線至少來自三個(gè)實(shí)驗(yàn)。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
實(shí)驗(yàn)圖片	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(xì)胞凋亡。
動(dòng)物實(shí)驗(yàn)	Animal Models	移植瘤裸鼠模型
	Dosages	7.5-30 毫克/千克 BID
	Administration	口服

參考文獻(xiàn)
[1]https://pubmed.ncbi.nlm.nih.gov/20439741/

參考文獻(xiàn)

[1]https://pubmed.ncbi.nlm.nih.gov/20439741/

化學(xué)信息&溶解度

分子量	490.62	分子式	C₂₅H₃₀N₈OS
CAS號(hào)	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(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 98 mg/mL ( (199.74 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 98 mg/mL (199.74 mM)

Water : Insoluble

DMSO : 98 mg/mL ( (199.74 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Ethanol : 98 mg/mL (199.74 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑				動(dòng)物體內(nèi)配方計(jì)算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過Selleck實(shí)驗(yàn)室實(shí)測(cè)。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測(cè)試。	5.000mg/ml (10.19mM)	以 1 mL 工作液為例,取50μL100mg/ml的澄清DMSO儲(chǔ)備液加到400μLPEG300中,混合均勻使其澄清;向上述體系中加入50μLTween80,混合均勻使其澄清;然后繼續(xù)加入500μLddH2O定容至1mL。工作液請(qǐng)現(xiàn)配現(xiàn)用!
澄清溶液	5% DMSO 1 95% Corn oil 該配方已經(jīng)過Selleck實(shí)驗(yàn)室實(shí)測(cè)。如果上述溶解方案不能滿足您的需求，可聯(lián)系Selleck銷售提供定制化測(cè)試。	5.000mg/ml (10.19mM)	以1 mL工作液為例，取50μL 100mg/ml的澄清DMSO儲(chǔ)備液加到950μL玉米油中，混合均勻。工作液請(qǐng)現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)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(qǐng)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(jìn)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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操作手冊(cè)

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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 it can cross BBB or not, the following reference indicate that this compound can not: http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3490962/.

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