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
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About This Item
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品質等級
化驗
≥95% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
protect from light
顏色
off-white
溶解度
DMSO: 100 mg/mL
ethanol: 5 mg/mL
運輸包裝
ambient
儲存溫度
2-8°C
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 密鑰
YJGVMLPVUAXIQN-HAEOHBJNSA-N
一般說明
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
包裝
Packaged under inert gas
警告
Toxicity: Carcinogenic / Teratogenic (D)
重構
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.
其他說明
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.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
訊號詞
Danger
危險分類
Acute Tox. 3 Oral - Acute Tox. 4 Dermal - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
標靶器官
Respiratory system
儲存類別代碼
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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