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.
別名:
IGF-1R Inhibitor, PPP, Insulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin
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この商品について
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
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
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
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
Target IC50: 1 nM against IGF-1R in cell-free kinase assay; ≤ 60 nM for cell viability and receptor autophosphorylation in melanoma cell lines
Cell permeable: yes
Primary Target
IGF-1R both in vitro and in vivo
IGF-1R both in vitro and in vivo
Product does not compete with ATP.
Reversible: yes
Packaging
Packaged under inert gas
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.
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.
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
Disclaimer
Toxicity: Carcinogenic / Teratogenic (D)
注意喚起語
Danger
ハザードコード
Hazard Classifications
Acute Tox. 3 Oral - Acute Tox. 4 Dermal - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
標的臓器
Respiratory system
保管分類
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
一体何が起きているの？
WGK 3
引火点 (F)
Not applicable
引火点（°C）
Not applicable