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Picropodophyllotoxin

Chemical Structure : Picropodophyllotoxin

CAS No.: 477-47-4

Picropodophyllotoxin (AXL1717)

Catalog No.: PC-49763Not For Human Use, Lab Use Only.

Picropodophyllotoxin (AXL1717, PPT) is a selective orally active insulin-like growth factor 1 receptor (IGF1R) inhibitor with IC50 of 1 nM, no activity against insulin receptor, FGFR, PDGFR or EGFR.

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Biological Activity

Picropodophyllotoxin (AXL1717, PPT) is a selective orally active insulin-like growth factor 1 receptor (IGF1R) inhibitor with IC50 of 1 nM, no activity against insulin receptor, FGFR, PDGFR or EGFR.
Picropodophyllin (AXL1717) (0.5-10 μM) potently inhibits IGF-1-stimulated IGF-1R, Akt (Ser 473) and Erk1/2 phosphorylation in intact cells.
Picropodophyllin (AXL1717) inhibits cell growth, and induces apoptosis in cultured IGF-1R-positive tumor cells.
Picropodophyllin (AXL1717) synergistically sensitizes HMCL, primary human MM and murine 5T33MM cells to ABT-737 and ABT-199.
Picropodophyllin (AXL1717) (20 mg/kg, i.p.) causes complete tumor regression in SCID mice xenografted with human ES-1, BE, and PC3, increases survival in the 5T33MM mouse model.

Physicochemical Properties

M.Wt 414.41
Formula C22H22O8
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(5R,5aS,8aR,9R)-5,8,8a,9-Tetrahydro-9-hydroxy-5-(3,4,5-trimethoxyphenyl)-furo[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one

References

1. Menu E, et al. Blood. 2006 Jan 15;107(2):655-60.

2. Vasilcanu D, et al. Oncogene. 2004 Oct 14;23(47):7854-62.

3. Menu E, et al. Int J Cancer. 2007 Oct 15;121(8):1857-61.

4. Girnita A, et al. Cancer Res. 2004 Jan 1;64(1):236-42.

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