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407247 IGF-1R Inhibitor, PPP - CAS 477-47-4 - Calbiochem

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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: Insulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin

Primary Target: IGF-1R both in vitro and in vivo
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
477-47-4C₂₂H₂₂O₈

Products

Catalogue NumberPackaging Qty/Pack
407247-1MGCN Plastic ampoule 1 mg
Description
OverviewA 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.
Catalogue Number407247
Brand Family Calbiochem®
SynonymsInsulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin
References
ReferencesMazitschek, R., and Giannis, A. 2004. Curr. Opin. Chem. Biol. 8, 432.
Vasilcanu, D., et al. 2004. Oncogene 23, 7854.
Girnita, A., et al. 2004. Cancer Res. 64, 236.
Product Information
CAS number477-47-4
ATP CompetitiveN
FormOff-white solid
Hill FormulaC₂₂H₂₂O₈
Chemical formulaC₂₂H₂₂O₈
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationIGF-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 TargetIGF-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 permeableY
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 InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Unstable in solution at room temperature.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
407247-1MGCN 04055977188660

Documentation

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

Title

Safety Data Sheet (SDS) 

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

TitleLot Number
407247

References

Reference overview
Mazitschek, R., and Giannis, A. 2004. Curr. Opin. Chem. Biol. 8, 432.
Vasilcanu, D., et al. 2004. Oncogene 23, 7854.
Girnita, A., et al. 2004. Cancer Res. 64, 236.
Data Sheet

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision09-May-2011 RFH
SynonymsInsulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin
DescriptionA 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.
FormOff-white solid
Intert gas (Yes/No) Packaged under inert gas
CAS number477-47-4
Chemical formulaC₂₂H₂₂O₈
Structure formulaStructure formula
Purity≥95% by HPLC
SolubilityDMSO (100 mg/ml) or Ethanol (5 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C. Unstable in solution at room temperature.
Toxicity Carcinogenic / Teratogenic
ReferencesMazitschek, R., and Giannis, A. 2004. Curr. Opin. Chem. Biol. 8, 432.
Vasilcanu, D., et al. 2004. Oncogene 23, 7854.
Girnita, A., et al. 2004. Cancer Res. 64, 236.