PF-3758309

別名:PF-03758309

PF-03758309 (PF-03758309) is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with Kd of 2.7 nM. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model.

PF-3758309化学構造

CAS No. 898044-15-0

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 21800 国内在庫あり
JPY 20200 国内在庫あり
JPY 57900 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(25)

カスタマーフィードバック3个实验数据

製品安全説明書

現在のバッチを見る: 純度: 99.98%
99.98

PF-3758309関連製品

シグナル伝達経路

PAK阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 PF-03758309 (PF-03758309) is a potent, ATP-competitive, pyrrolopyrazole inhibitor of PAK4 with Kd of 2.7 nM. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model.
特性 PF-3758309 is potent toward a broad array of tumor cell lines from different tumor types.
Targets
PAK1 [1]
(Cell-free assay)
PAK6 [1]
(Cell-free assay)
PAK5 [1]
(Cell-free assay)
PAK4 [1]
(Cell-free assay)
PAK3 [1]
(Cell-free assay)
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13.7 nM(Ki) 17.1 nM(Ki) 18.1 nM(Ki) 18.7 nM(Ki) 99 nM
In Vitro
In vitro

PF-3758309 is a potent (Kd = 2.7 nM), ATP-competitive inhibitor of PAK4 with Ki of 18.7 nM. In cells, PF-3758309 inhibits phosphorylation of the PAK4 substrate GEF-H1 (IC50 = 1.3 nM) and anchorage-independent growth of a panel of tumor cell lines (IC50 = 4.7 nM). PF-3758309 also inhibits endogenous pGEF-H1 accumulation in HCT116 cells. PF-3758309 potently inhibits cellular proliferation (IC50 = 20 nM) and anchorage-independent growth (IC50 = 27 nM) of A549 cells. [1]

Kinase Assay Phospho-GEF-H1 Cellular Assay
TR-293-KDG cells are constructed from HEK293 cells stably transfected with tetracycline-inducible PAK4-kinase domain (amino acids 291-591) and constitutively expressed HA-tagged GEFH1ΔDH (amino acids 210-921). TR-293-KDG cells are incubated for 3 h with PF-3758309, captured on an anti-HA antibody-coated plate, detected with an anti-phospho-S810-GEF-H1 antibody, and quantified with a horseradish peroxidase-goat anti-rabbit antibody conjugate.
細胞実験 細胞株 HEK293T, HCT116, and SKOV3 cells
濃度 ~1 μM
反応時間 72 hours
実験の流れ

A panel of cancer cell lines is used to test the potency of PF-3758309. On day 1, cells are plated on 384-well plates. Onday2, compounds are added to the cell culture. The cells are incubated with the compound for 3 days. On day 5, all media are aspirated from the wells. Dose-dependent effects of PF-3758309 on cell proliferation are quantified via the CellTiter-Glo Luminescent Cell Viability Assay(a,b,c), which is a homogeneous method of determining the number of viable cells in culture based on quantitation of the ATP present, an indicator of metabolically active cells. Proliferation data displayed for HEK293T, HCT116, and SKOV3 cells are measured using the Cyquant NF assay as specified by the manufacturer. Briefly, 24 h after seeding on 384-well plates, cells are treated with vehicle or PF-3758309, Dasatinib, or the positive control, Bleomycin (60 mU/ mL).72 hours after drug treatment, cell proliferation is measured. Results for each drug are normalized to vehicle control and expressed as a percentage of maximum assay inhibition relative to Bleomycin. Error bars represent the SD from at least three experiments.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot PAK4 / PI3K / p-AKT / AKT / p-mTOR / mTOR 28407679
In Vivo
In Vivo

PF-3758309 blocks the growth of multiple human tumor xenografts, with a plasma EC50 value of 0.4 nM in the most sensitive model. PF-3758309 is antiproliferative and induces apoptosis in a HCT116 tumor model. [1]

動物実験 動物モデル Xenograft tumors in nude mice
投与量 7.5-30 mg/kg BID
投与経路 p.o.

化学情報

分子量 490.62 化学式

C25H30N8OS

CAS No. 898044-15-0 SDF Download PF-3758309 SDFをダウンロードする
Smiles CC1=NC2=C(C(=N1)NC3=NNC4=C3CN(C4(C)C)C(=O)NC(CN(C)C)C5=CC=CC=C5)SC=C2
保管

In vitro
Batch:

DMSO : 98 mg/mL ( (199.74 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 98 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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Handling Instructions

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よくある質問(FAQ)

質問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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