Skip to Content
Merck
CN

407247

IGF-1R Inhibitor, PPP

The IGF-1R Inhibitor, PPP, also referenced under CAS 477-47-4, controls the biological activity of IGF-1R. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

IGF-1R Inhibitor, PPP, Insulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin

Sign In to View Organizational & Contract Pricing.

Select a Size

About This Item

Empirical Formula (Hill Notation):
C22H22O8
CAS Number:
477-47-4
Molecular Weight:
414.41
UNSPSC Code:
12352200
NACRES:
NA.77
MDL number:
MFCD01742647

Key Documents

View All Documentation
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist
Technical Service
Need help? Our team of experienced scientists is here for you.
Let Us Assist

Product Name

IGF-1R Inhibitor, PPP, The IGF-1R Inhibitor, PPP, also referenced under CAS 477-47-4, controls the biological activity of IGF-1R. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

SMILES string

O1COc2c1cc3c(c2)[C@H]([C@H]5[C@@H]([C@H]3O)COC5=O)c4cc(c(c(c4)OC)OC)OC

InChI

1S/C22H22O8/c1-25-16-4-10(5-17(26-2)21(16)27-3)18-11-6-14-15(30-9-29-14)7-12(11)20(23)13-8-28-22(24)19(13)18/h4-7,13,18-20,23H,8-9H2,1-3H3/t13-,18+,19+,20-/m0/s1

InChI key

YJGVMLPVUAXIQN-HAEOHBJNSA-N

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

off-white

solubility

DMSO: 100 mg/mL
ethanol: 5 mg/mL

shipped in

ambient

storage temp.

2-8°C

Quality Level

100

Related Categories

Packaging

Packaged under inert gas

Biochem/physiol Actions

Cell permeable: yes
Primary Target
IGF-1R both in vitro and in vivo
Product does not compete with ATP.
Reversible: yes
Target IC50: 1 nM against IGF-1R in cell-free kinase assay; ≤ 60 nM for cell viability and receptor autophosphorylation in melanoma cell lines

Disclaimer

Toxicity: Carcinogenic / Teratogenic (D)

General description

A cell-permeable cis-cyclolignan compound that acts as a substrate competitive, reversible, potent, and specific inhibitor of IGF-1R both in vitro (IC50 = 1 nM in cell-free kinase assay; ≤ 60 nM for cell viability and receptor autophosphorylation in melanoma cell lines) and in vivo (complete inhibition of IGF-1R-dependent tumor cell growth at 20 mg/kg/12 hr, i.p., in SCID mice) with minimum toxic effect (LD50 >500 mg/kg). Exhibits little effect towards IR, FGFR, PDGFR and EGFR, and exerts no effects on microtubules and DNA topoisomerase II. Targets the phosphorylation of Y1136 in the activation loop and is the first inhibitor reported to discriminate between IGF-1R and IR.
A cell-permeable, reversible, potent, substrate competitive, and specific inhibitor of IGF-1R both in vitro (IC50 = 1 nM in cell-free kinase assay; ≤60 nM and for cell viability and receptor autophosphorylation in melanoma cell lines) and in vivo (complete inhibition of IGF-1R-dependent tumor cell growth at 20 mg/kg/12 hr i.p. in SCID mice with only minimal toxic effects (LD50 >500 mg/kg). Exhibits little inhibition towards IR, FGFR, PDGFR and EGFR, and exerts no effects on microtubules and DNA topoisomerase II. Targets the phosphorylation of Y1136 in the activation loop and is the first inhibitor reported to discriminate between IGF-1R and IR.

Other Notes

Mazitschek, R., and Giannis, A. 2004. Curr. Opin. Chem. Biol.8, 432.
Vasilcanu, D., et al. 2004. Oncogene23, 7854.
Girnita, A., et al. 2004. Cancer Res.64, 236.

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Unstable in solution at room temperature.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

pictograms

Skull and crossbones
GHS06

signalword

Danger

Hazard Classifications

Acute Tox. 3 Oral - Acute Tox. 4 Dermal - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

Storage Class

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

Already Own This Product?

Find documentation for the products that you have recently purchased in the Document Library.

Visit the Document Library

Fang Chen et al.
Scientific reports, 14(1), 2509-2509 (2024-01-31)
This study investigates the potential of ellagic acid (EA), a phytochemical with antioxidant and anti-inflammatory properties, in managing perioperative neurocognitive disorders (PND). PND, which represents a spectrum of cognitive impairments often faced by elderly patients, is principally linked to surgical
Li Ji et al.
Physiological reports, 12(3), e15939-e15939 (2024-02-06)
Recurrent spontaneous abortion (RSA) is a serious condition that adversely affects women's health. Differentially expressed proteins (DEPs) in plasma of patients experiencing RSA is helpful to find new therapeutic targets and identified with mass spectrometry. In 57 DEPs, 21 were

Our team of scientists has experience in all areas of research including Life Science, Material Science, Chemical Synthesis, Chromatography, Analytical and many others.

Contact Technical Service