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Picropodophyllin

Catalog No. T6943 CAS 477-47-4

Synonyms: AXL1717, Picropodophyllin (PPP), Picropodophyllotoxin, PPP

Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT).

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Picropodophyllin, CAS 477-47-4

Pack Size	Availability	Price/USD
5 mg	In stock	$ 58.00
10 mg	In stock	$ 80.00
25 mg	In stock	$ 178.00
50 mg	In stock	$ 333.00
100 mg	In stock	$ 563.00
500 mg	In stock	$ 1,180.00
1 mL * 10 mM (in DMSO)	In stock	$ 63.00

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Purity: 99.55%

Purity: 99.41%

Purity: 98.88%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT).
Targets&IC50	IGF-1R:1 nM
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 5T33 mM cells to ABT-737 and ABT-199 by further decreasing cell viability and enhancing apoptosis. [3] Picropodophyllin and sorafenib synergistically suppress the proliferation and motility of hepatocellular carcinoma cells. [4]
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 5T33 mM mouse model, Picropodophyllin also shows a marked antitumor activity, and causes a significant increase in survival. [2]
Kinase Assay	In vitro tyrosine kinase assays.: 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.
Cell Research	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. (Only for Reference)
Source	Natural Products > Berberidaceae > Dysosma

Synonyms	AXL1717, Picropodophyllin (PPP), Picropodophyllotoxin, PPP
Molecular Weight	414.41
Formula	C22H22O8
CAS No.	477-47-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 76 mg/mL (183.4 mM)

Ethanol: 1 mg/mL (2.41 mM), Heating is recommended.

References and Literature

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.

Citations

1. Wu, Qi, et al. IGF1 receptor inhibition amplifies the effects of cancer drugs by autophagy and immune-dependent mechanisms. Journal for Immunotherapy of Cancer. 9.6 (2021): e002722

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Kinase Inhibitor Library Highly Selective Inhibitor Library Tyrosine Kinase Inhibitor Library Anti-Cancer Drug Library Covalent Inhibitor Library Selected Plant-Sourced Compound Library

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Keywords

Picropodophyllin 477-47-4 Apoptosis Tyrosine Kinase/Adaptors IGF-1R Inhibitor AXL1717 Picropodophyllin (PPP) Picropodophyllotoxin AXL-1717 PPP inhibit AXL 1717 inhibitor

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