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    • 3. 发明公开
    • Antibodies against insulin-like growth factor I receptor and uses thereof
    • Reikeptor und deren Verwendungen
    • EP2272873A2
    • 2011-01-12
    • EP10180710.5
    • 2004-07-09
    • F. Hoffmann-La Roche AG
    • Graus, YvoKopetzki, ErhardKuenkele, Klaus-PeterMundigl, OlafParren, PaulRebers, FrankSchumacher, Ralfvan de Winkel, Janvan Vugt, Martine
    • C07K16/28C12N15/13C12N5/16A61K39/395
    • C07K16/2863A61K2039/505C07K16/2896C07K2317/73
    • An antibody binding to IGF-IR and inhibiting the binding of IGF-I and IGF-II to IGF-IR which is characterized in that said antibody is a) is of IgG1 isotype, b) shows a ratio of IC 50 values of inhibition of the binding of IGF-I to IGF-IR to the inhibition of binding of IGF-II to IGF-IR of 1:3 to 3:1,c) inhibits for at least 80% at a concentration of 5 nM IGF-IR phosphorylation in a cellular phosphorylation assay using 3T3 cells providing 400,000 to 600,000 molecules IGF-IR per cell in a medium containing 0.5% heat inactivated fetal calf serum (FCS) when compared to such an assay without said antibody, andd) shows no IGF-IR stimulating activity measured as IGF-IR phosphorylation at a concentration of 10 µM in a cellular phosphorylation assay using 3T3 cells providing 400,000 to 600,000 molecules IGF-1R per cell in a medium containing 0.5% heat inactivated fetal calf serum (FCS) when compared to such an assay without said antibody has improved properties in antitumor therapy.
    • 与IGF-1R结合并抑制IGF-I和IGF-II与IGF-1R结合的抗体,其特征在于所述抗体是a)是IgG1同种型,b)显示IC 50的抑制值 IGF-I与IGF-1R的结合抑制IGF-II与IGF-1R的结合为1:3至3:1,c)在5nM IGF-1R磷酸化浓度下抑制至少80% 在使用3T3细胞的细胞磷酸化测定中,当与没有所述抗体的这种测定相比时,在含有0.5%热灭活胎牛血清(FCS)的培养基中,每个细胞提供40万至600,000分子IGF-1R,并且d)显示没有IGF-1R刺激 在细胞磷酸化测定中,使用3T3细胞,在含有0.5%热灭活的胎牛血清(FCS)的培养基中,每细胞提供40,000至600,000分子IGF-1R,在10μM浓度下作为IGF-1R磷酸化测量活性。 没有所述抗体的测定在抗肿瘤治疗中具有改善的性质。
    • 4. 发明公开
    • Antibodies against insulin-like growth factor I receptor and uses thereof
    • Antikörpergegen insulinartigen Wachstumsfaktor-1-Rezeptor und deren Verwendung
    • EP2243835A2
    • 2010-10-27
    • EP10167052.9
    • 2004-07-09
    • F. Hoffmann-La Roche AG
    • Graus, YvoKopetzki, ErhardKuenkele, Klaus-PeterMundigl, OlafParren, PaulRebers, FrankSchumacher, Ralfvan de Winkel, Janvan Vugt, Martine
    • C12N15/13C12N5/16A61K39/395
    • C07K16/2863A61K2039/505C07K16/2896C07K2317/73
    • An antibody binding to IGF-IR and inhibiting the binding of IGF-I and IGF-II to IGF-IR which is characterized in that said antibody is a) is of IgG1 isotype, b) shows a ratio of IC 50 values of inhibition of the binding of IGF-1 to IGF-IR to the inhibition of binding of IGF-II to IGF-IR of 1:3 to 3:1,c) inhibits for at least 80% at a concentration of 5 nM IGF-IR phosphorylation in a cellular phosphorylation assay using 3T3 cells providing 400,000 to 600,000 molecules IGF-IR per cell in a medium containing 0.5% heat inactivated fetal calf serum (FCS) when compared to such an assay without said antibody, andd) shows no IGF-IR stimulating activity measured as IGF-IR phosphorylation at a concentration of 10 µM in a cellular phosphorylation assay using 3T3 cells providing 400,000 to 600,000 molecules IGF-1R per cell in a medium containing 0.5% heat inactivated fetal calf serum (FCS) when compared to such an assay without said antibody has improved properties in antitumor therapy.
    • 与IGF-1R结合并抑制IGF-I和IGF-II与IGF-1R结合的抗体,其特征在于所述抗体是a)是IgG1同种型,b)显示IC 50的抑制值 IGF-1与IGF-IR的结合抑制IGF-II与IGF-IR的结合为1:3至3:1,c)在5nM IGF-1R磷酸化浓度下抑制至少80% 在使用3T3细胞的细胞磷酸化测定中,当与没有所述抗体的这种测定相比时,在含有0.5%热灭活胎牛血清(FCS)的培养基中,每个细胞提供40万至600,000分子IGF-1R,并且d)显示没有IGF-1R刺激 在细胞磷酸化测定中,使用3T3细胞,在含有0.5%热灭活的胎牛血清(FCS)的培养基中,每细胞提供40,000至600,000分子IGF-1R,在10μM浓度下作为IGF-1R磷酸化测量活性。 没有所述抗体的测定在抗肿瘤治疗中具有改善的性质。