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PD173074

PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.

PD173074化学構造

CAS No. 219580-11-7

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 85500 国内在庫あり
JPY 448500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール：sales@selleck.co.jp
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製品安全説明書

現在のバッチを見る： 純度： 99.72%
99.72

PD173074関連製品

シグナル伝達経路

FGFR Signaling Pathways

FGFRシグナル伝達経路

FGFR阻害剤の選択性比較

阻害剤 Citation EGFR/ErbB1 HER2/ErbB2 ErbB3 ErbB4 mutant EGFR その他
Saracatinib (AZD0530) 299 c-Src,c-YES,LCK
Canertinib (CI-1033) 48
AG-490 132 JAK2 (V617F)
CP-724714 108
WZ4002 34
Sapitinib (AZD8931) 48
CUDC-101 23 HDAC,HDAC1,HDAC6
AG-1478 97
PD153035 HCl 17
Pelitinib (EKB-569) 11 Src,MEK/ERK,Raf
AEE788 (NVP-AEE788) 13 c-Abl,FLT1,c-Fms
AC480 (BMS-599626) 10
AP26113-analog (ALK-IN-1) 4 ALK,IGF1R,INSR
WZ3146 2
Allitinib tosylate 16
Rociletinib (CO-1686) 36
Varlitinib 8
Icotinib (BPI-2009H) 9
TAK-285 4 MEK1,Aurora B,LCK
WHI-P154 11 Src,VEGFR,JAK3
Daphnetin 4 PKA,PKC
PD168393 6
CNX-2006 2
Tyrphostin 9 1 PDGFR
AG-18 1
Icotinib Hydrochloride 0
HS-10296 hydrochloride 0
MTX-531 0 PI3Kα
Avitinib maleate 0 BTK
limertinib 0
AG 825 0 PDGFR
4-AMino-1-phenylpyrazolo[3,4-d]pyriMidine 0
AST-1306 0
ErbB2 inhibitor 0
Tuxobertinib (BDTX-189) 2 RIPK2,BLK
Epertinib hydrochloride 0
JND3229 0 EGFR C797S
BI-4020 1
Tyrphostin AG-528 0
AG 556 0
Canertinib dihydrochloride 8
EGFR Inhibitor 3 Microtubules
SU5214 0 VEGFR2
RG 13022 0
TQB3804 0
zipalertinib (TAS6417) 3 TXK,BMX
Pyrotinib dimaleate 4
PD153035 14
AG 494 0
AG 555 0
Theliatinib (HMPL-309) 0
Avitinib (Abivertinib) 2 JAK3,BTK
Lazertinib 7 Del19,L85R
Lifirafenib (BGB-283) 6 WT A-RAF,C-RAF (Y340/341D),BRAF(V600E)
Nazartinib (EGF816) 6
Zorifertinib (AZD3759) 6
CL-387785 (EKI-785) 5
Poziotinib 34
AZ5104 4 ACK1,BLK,BRK
AV-412 free base 0
HER2-Inhibitor-1 1
WZ8040 2
Genistein 32 topo II
Rezivertinib 0
BDTX-1535 0
Falnidamol 0
BLU-945 0
(S)-Sunvozertinib ((S)-DZD9008) 1
Licochalcone D 0 NF-κB,PARP,Caspase
Alflutinib (Furmonertinib) mesylate 2 CYP3A4
(Rac)-JBJ-04-125-02 0
Tyrphostin AG30 (AG30) 0
AG-1557 0
AG99 0
MTX-211 2 PI3K
RG14620 0 ABCG2
Almonertinib (HS-10296) 2
Cyasterone 1
Norcantharidin 3 c-Met
Naquotinib(ASP8273) 1
EAI045 2
Olmutinib (BI 1482694) 5 BTK
Butein 2
Chrysophanic Acid 3 mTOR
EGCG ((-)-Epigallocatechin Gallate) 41 DNMT,telomerase,FASN
もっと見る
1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
HUVEC Function assay 10 nM 14 hrs Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 10 nM after 14 hrs 16474387
HUVEC Function assay 100 nM 14 hrs Inhibition of FGFR-mediated angiogenesis in human HUVEC cells assessed as decrease in capillary tube sprouting at 100 nM after 14 hrs 16474387
SUM52 Antiproliferative assay 5 days Antiproliferative activity against human FGFR2-amplified SUM52 cells after 5 days by SRB assay, IC50 = 0.0123 μM. 28521156
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生物活性

製品説明 PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells.
Targets
FGFR1 [1]
(Cell-free assay)		 VEGFR2 [1]
(Cell-free assay)
~25 nM 100 nM-200 nM
In Vitro
In vitro PD173074 is an ATP-competitive inhibitor of FGFR1 with Ki of ~40 nM. PD173074 is also an effective inhibitor of VEGFR2. Compared to FGFR1, PD173074 weakly inhibits the activities of Src, InsR, EGFR, PDGFR, MEK, and PKC with 1000-fold or greater IC50 values. PD173074 inhibits autophosphorylation of FGFR1 and VEGFR2 in a dose-dependent manner with IC50 of 1-5 nM and 100-200 nM, respectively. [1] PD173074 inhibits FGF-2 promotion of granule neuron survival in a dose-dependent manner with IC50 of 12 nM, exhibiting 1,000-fold greater potency than that of SU 5402. [2] PD173074 specifically inhibits FGF-2-mediated effects on proliferation, differentiation, and MAPK activation in oligodendrocyte (OL) lineage cells. [3] PD173074 is active against the WT receptor and FGFR3 mutations in multiple myeloma (MM) cell lines. PD173074 also potently inhibits autophosphorylation of FGFR3 in a dose-dependent manner with IC50 of ~5 nM. PD173074 treatment potently reduces viability of FGFR3-expressing KMS11 and KMS18 cells with IC50 of <20 nM. Inhibition of aFGF-stimulated MM cell growth by PD173074 is highly correlated with the expression of FGFR3. PD173074 treatment completely abolishes NIH 3T3 transformation mediated by Y373C FGFR3 but not by Ras V12, demonstrating that PD173074 specifically targets FGFR3-mediated cell transformation and lacks nonspecific cytotoxic effect. PD173074 also induces functional maturation of KMS11 and KMS18 cells. [4]
Kinase Assay In vitro kinase inhibition assays
Assays using the full-length FGFR-1 kinase are performed in a total volume of 100 μL containing 25 mM HEPES buffer (pH 7.4), 150 mM NaCl, 10 mM MnCl2, 0.2 mM sodium orthovanadate, 750 μg/mL concentration of a random copolymer of glutamic acid and tyrosine (4:1), various concentrations of PD173074 and 60 to 75 ng of enzyme. The reaction is initiated by the addition of [γ-32P]ATP (5 μM ATP containing 0.4 μCi of [γ-32P]ATP per incubation), and samples are incubated at 25°C for 10 minutes. The reaction is terminated by the addition of 30% trichloroacetic acid and the precipitation of material onto glass-fiber filter mats. Filters are washed three times with 15% trichloroacetic acid, and the incorporation of [32P] into the glutamate tyrosine polymer substrate is determined by counting the radioactivity retained on the filters in a Wallac 1250 betaplate reader. Nonspecific activity is defined as radioactivity retained on the filters following incubation of samples without enzyme. Specific activity is determined as total activity (enzyme plus buffer) minus nonspecific activity. The concentration of PD173074 that inhibits FGFR-1 enzymatic activity by 50% (IC50) is determined graphically.
細胞実験 細胞株 KMS11 and KMS18
濃度 Dissolved in DMSO, final concentrations ~100 nM
反応時間 48 hours
実験の流れ Cells are incubated with increasing concentrations of PD173074 in the presence of aFGF/heparin for 48 hours. The percentage of viable cells is determined by MTT.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot pFGFR2 / FGFR2 p-S6RP / p-PRAS40 / p-p105 NFKB / P105 NFKB / P50 NFKB / p-AMPK / p-CRK II / p-PDK1 24968263
Growth inhibition assay Cell viability 24968263
In Vivo
In Vivo Administration of PD173074 at 1 mg/kg/day or 2 mg/ka/day in mice can effectively block angiogenesis induced by either FGF or VEGF in a dose-dependent manner with no apparent toxicity. [1] PD173074 inhibits in vivo growth of mutant FGFR3-transfected NIH 3T3 cells in nude mice. Inhibition of FGFR3 by PD173074 delays tumor growth and increases survival of mice in a KMS11 xenograft myeloma model. [4] In the H-510 xenograft, oral aministration of PD173074 blocks tumor growth similar to that seen with single-agent cisplatin administration, increasing median survival compared with control sham-treated animals. In H-69 xenografts, PD173074 induces complete responses lasting >6 months in 50% of mice. These effects are correlated with increased apoptosis in excised tumors, but not a consequence of disrupted tumor vasculature. [5]
動物実験 動物モデル Swiss Webster mice with induced corneal angiogenesis
投与量 ~2 mg/kg/day
投与経路 Administered intraperitoneally

化学情報

分子量 523.67 化学式

C28H41N7O3
CAS No. 219580-11-7 SDF Download PD173074 SDFをダウンロードする
Smiles CCN(CC)CCCCNC1=NC2=NC(=C(C=C2C=N1)C3=CC(=CC(=C3)OC)OC)NC(=O)NC(C)(C)C
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (190.95 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 : 100 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
Clear solution
2%DMSO 40% 5% 53%ddH2O
3.0mg/ml (5.73mM) Taking the 1 mL working solution as an example, add 20 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 530 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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 匹

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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よくある質問（FAQ）

質問1:
What is the half-life of PD173074(S1264) in vivo?

回答
According to literature research, PD173074 is given twice daily because it has a short half-life in vivo, please refer to the following link for detailed pharmacokinetic information (Supplementary Figure 8B): http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3990281/#!po=50.0000.

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