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.
别名:
IGF-1R Inhibitor, PPP, Insulin-like Growth Factor-1 Receptor Inhibitor, Picropodophyllin
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
off-white
溶解性
DMSO: 100 mg/mL
ethanol: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
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
一般描述
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.
生化/生理作用
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
Target IC50: 1 nM against IGF-1R in cell-free kinase assay; ≤ 60 nM for cell viability and receptor autophosphorylation in melanoma cell lines
包装
Packaged under inert gas
制备说明
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.
其他说明
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Carcinogenic / Teratogenic (D)
警示用语：
Danger
危险分类
Acute Tox. 3 Oral - Acute Tox. 4 Dermal - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
靶器官
Respiratory system
储存分类代码
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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