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.
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.
Product Information
CAS number
477-47-4
ATP Competitive
N
Form
Off-white solid
Hill Formula
C₂₂H₂₂O₈
Chemical formula
C₂₂H₂₂O₈
Reversible
Y
Structure formula Image
Applications
Application
IGF-1R Inhibitor, PPP, CAS 477-47-4, is a cell-permeable, substrate competitive, reversible, potent, and specific inhibitor of IGF-1R both in vitro (IC50 = 1 nM in cell-free kinase assay) & in vivo.
Biological Information
Primary Target
IGF-1R both in vitro and in vivo
Primary Target IC<sub>50</sub>
1 nM against IGF-1R in cell-free kinase assay; ≤ 60 nM for cell viability and receptor autophosphorylation in melanoma cell lines
Purity
≥95% by HPLC
Physicochemical Information
Cell permeable
Y
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code
Ambient Temperature Only
Toxicity
Carcinogenic / Teratogenic
Storage
+2°C to +8°C
Protect from Light
Protect from light
Do not freeze
Ok to freeze
Special Instructions
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.
新浪微博
腾讯微博
QQ空间
客服
