IGF-1R Inhibitor, PPP - CAS 477-47-4 - Calbiochem

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.

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

Packaging

Packaged under inert gas

Warning

Toxicity: Carcinogenic / Teratogenic (D)

Reconstitution

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.

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.

Legal Information

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