Picropodophyllin (PPP)

別名：AXL1717

製品コード：S7668 純度：99.95%

Picropodophyllin (PPP, AXL1717) is a IGF-1R inhibitor with IC50 of 1 nM. It displays selectivity for IGF-1R and does not coinhibit tyrosine phosphorylation the IR, or of a selected panel of receptors less related to IGF-IR(FGF-R, PDGF-R, OR EGF-R). Picropodophyllin (PPP) induces apoptosis with antineoplastic activity.

CAS No. 477-47-4

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
5mg	JPY 22000	国内在庫あり
25mg	JPY 55500	国内在庫あり
100mg	JPY 104500	国内在庫あり
1g	JPY 445500	国内在庫なし(納期7~10日)

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（41）

製品安全説明書

現在のバッチを見る：純度： 99.95%

99.95

Picropodophyllin (PPP)関連製品

関連ターゲット	Insulin Receptor	もっと見る
関連製品	Linsitinib (OSI-906) NVP-AEW541 BMS-754807 GSK1904529A BMS-536924 AG-1024 NVP-ADW742 NT157 PQ 401	もっと見る
関連化合物ライブラリー	Kinase Inhibitor Library Tyrosine Kinase Inhibitor Library PI3K/Akt Inhibitor Library Cell Cycle compound library Angiogenesis Related compound Library	もっと見る

シグナル伝達経路

IGF-1Rシグナル伝達経路

IGF-1R阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	活性情報	PMID
P-388 neoplastic cell line	Cytotoxic assay	In vitro cytotoxicity against the P-388 (from DBA/2 mouse) neoplastic cell line, IC50=60 nM	14980682
A-549 (human lung carcinoma) neoplastic cell line	Cytotoxic assay	In vitro cytotoxicity against the A-549 (human lung carcinoma) neoplastic cell line, IC50=60 nM	14980682
HT-29 (human colon carcinoma) neoplastic cell line	Cytotoxic assay	In vitro cytotoxicity against the HT-29 (human colon carcinoma) neoplastic cell line, IC50=60 nM	14980682
amnion cells	Antiviral assay	Antiviral activity against HSV1 infected in human primary amnion cells assessed as inhibition of virus-induced pathogenic effect, Activity = 1.9 μM.	9834179
P388	Cytotoxicity assay	Cytotoxicity against mouse P388 cells, IC50 = 6 μM.	7673931
A549	Cytotoxicity assay	Cytotoxicity against human A549 cells, IC50 = 6 μM.	7673931
HT-29	Cytotoxicity assay	Cytotoxicity against human HT-29 cells, IC50 = 6 μM.	7673931
TC32	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells	29435139
DAOY	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
SJ-GBM2	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
A673	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
SK-N-MC	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
NB-EBc1	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
Saos-2	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells	29435139
LAN-5	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells	29435139
BT-12	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells	29435139
OHS-50	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
A673	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells)	29435139
SK-N-MC	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells	29435139
BT-12	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-12 cells	29435139
LAN-5	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells	29435139
DAOY	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for DAOY cells	29435139
NB-EBc1	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells	29435139
BT-37	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells	29435139
TC32	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells	29435139
MG 63 (6-TG R)	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells	29435139
U-2 OS	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells	29435139
RD	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Saos-2	qHTS assay	qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells	29435139
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生物活性

製品説明

Targets

IGF-1R ^[1]
(Cell-free assay)

1 nM

In Vitro
In vitro	In intact cells, PPP efficiently inhibits IGF-1-stimulated IGF-1R, Akt (Ser 473) and Erk1/2 phosphorylation. Picropodophyllin specifically inhibits cell growth, and induces apoptosis in cultured IGF-1R-positive tumor cells. ^[1] Picropodophyllin synergistically sensitizes HMCL, primary human MM and murine 5T33MM cells to ABT-737 and ABT-199 by further decreasing cell viability and enhancing apoptosis. ^[3] Picropodophyllin synergistically suppress the proliferation and motility of hepatocellular carcinoma cells. ^[4]
Kinase Assay	In vitro tyrosine kinase assays.
Kinase Assay	Assay of IGF-1R-catalyzed substrate phosphorylation of pTG, using a 96-well plate tyrosine kinase assay kit, is performed. We use recombinant epidermal growth factor receptor, immunoprecipitated IR from HEPG2, immunoprecipitated IGF-1R from P6 cells, and IGF-1R immunodepleted supernatant from P6 (representing “non-IGF-1R tyrosine kinases”). After 30-min treatment of the receptors with the desired compounds in the kinase buffer [50 mM HEPES buffer (pH 7.4), 20 mM MgCl₂, 0.1 MnCl₂, and 0.2 Na₃VO₄], the kinase reaction is activated by addition of ATP. The phosphorylated polymer substrate is probed with a phosphotyrosine-specific monoclonal antibody conjugated to horseradish peroxidase, clone PT-66. Color is developed with horseradish peroxidase chromogenic substrate O-phenylenediamine dihydrochloride and quantitated by spectrophotometry (ELISA reader). IGF-1R tyrosine autophosphorylation is analyzed by a sandwich ELISA assay. Briefly, 96-well plates are coated overnight at 4°C with 1 μg/well of an antibody to IGF-1R β-subunit. The plates are blocked with 1% BSA in PBS Tween for 1 h, and then 80 μg/well of total protein lysate from the P6 cell line is added. As a negative control we use total protein lysate from the R- cell line. The investigated compounds are added in tyrosine kinase buffer without ATP at room temperature for 30 min before kinase activation with ATP. Kinase assay is performed using the Sigma kit (see above). After spectrophotometry the IC50 values of inhibitors are determined using the REGRESSION function of Statistica program.
細胞実験	細胞株	Melanoma cells (FM 55, SK-MEL-28, SK-MEL-5, C8161, DFB, DFW and AA), sarcoma cells (RD-ES), breast carcinoma cells (MCF 7), prostate carcinoma cells (PC3), hepatoma cells (HepG2) and embryonic mouse fibroblasts (P6 and R-)
	濃度	~15 μM
	反応時間	48 hours
	実験の流れ	The determinations are performed using the Cell proliferation kit II, which is based on colorimetric change of the yellow tetrazolium salt 2,3-bis[2-methoxy-4-nitro-5-sulfophenyl]-2H-tetrazolium-5-carboxanilide inner salt in orange formazan dye by the respiratory chain of viable cell. All of the standards and experiments are performed in triplicates.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-IGFR1 / p-AKT / p-ERK		22363814
	Growth inhibition assay	Cell viability		22159423

In Vivo
In Vivo	In SCID mice xenografted with human ES-1, BE, and PC3, Picropodophyllin (20 mg/kg/12 h, i.p.) causes complete tumor regression. ^[1] In the 5T33MM mouse model, Picropodophyllin also shows a marked antitumor activity, and causes a significant increase in survival. ^[2]
動物実験	動物モデル	SCID mice bearing ES-1, BE, or PC3 xenografts that express IGF-1R, or R- v-src (IGF-1R negative) and P12 (overexpressing IGF-1 and IGF-1R)
	投与量	20 mg/kg/12 h
	投与経路	i.p.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06357884	Recruiting	Diabetic Neuropathies\|Plantar Callus	Chinese University of Hong Kong\|Princess Margaret Hospital Hong Kong	February 23 2024	Not Applicable
NCT05710185	Recruiting	Palmoplantar Pustulosis	Brigham and Women''s Hospital\|University of Pennsylvania	July 1 2023	Phase 4
NCT06025422	Recruiting	Diabetic Foot Ulcer\|Diabetic Neuropathies	University Hospitals Leicester\|University of Salford	March 13 2023	--
NCT04433052	Recruiting	Coronary Heart Disease	Tampere University	February 1 2023	Not Applicable
NCT05740137	Active not recruiting	Colorectal Cancer\|Colorectal Adenoma\|Colorectal Neoplasms	Ismail Gögenur\|Nykøbing Falster County Hospital\|Naestved Hospital\|Holbaek Sygehus\|Slagelse Hospital\|Zealand University Hospital	October 1 2022	Not Applicable

参考
[1] Girnita A, et al. Cancer Res. 2004, 64(1), 236-242. [2] Menu E, et al. Blood. 2006, 107(2), 655-660. [3] Bieghs L, et al. Oncotarget. 2014, 5(22), 11193-11208. [4] Tomizawa M, et al. Oncol Lett. 2014, 8(5), 2023-2026. + 展開

参考

[4] Tomizawa M, et al. Oncol Lett. 2014, 8(5), 2023-2026.

+ 展開

化学情報

分子量	414.41	化学式	C₂₂H₂₂O₈
CAS No.	477-47-4	SDF	Download Picropodophyllin (PPP) SDFをダウンロードする
Smiles	COC1=CC(=CC(=C1OC)OC)C2C3C(COC3=O)C(C4=CC5=C(C=C24)OCO5)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 83 mg/mL ( (200.28 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 : 1.5 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
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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Handling Instructions

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よくある質問（FAQ）

質問1:
I am currently setting the conditions for in vivo experiments, how should I reconstitute the drug?

回答
Other than DMSO:vegetable oil 10:1 (v/v) cited from reference. We tested another formulation: 4% DMSO+corn oil. S7668 Picropodophyllin (PPP) can be dissolved in it at 5 mg/ml clearly. But after stayed for about 20-30 min, the two phase would separate and wouldn't get together again. So if you are going to use this formulation, please prepare the fresh solution just before use.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):