A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity

Tissue factor-targeted antibody-drug conjugate

The invention discloses a method for building medicine transport models for research on BCRP (breast cancer resistance proteins) mediation for 3D (three-dimensional) organs of the small intestines of mice. The method includes separating crypts from the small intestines of the mice by means of digestion, suspending the crypts in matrigel and then joining the crypts with cell culture plates and promoting differentiation of the crypts by the aid of ADMEM/F12 media with Respondin-1, m-noggin and m-EGF cell differentiation growth factors to form the 3D organs; carrying out morphologic observation and detecting the expression level of BCRP genes and proteins to verify the feasibility of model theories; carrying out research on the trans-membrane transport activity of BCRP in the 3D organs by the aid of fluorescent substrates Hoechst 33342 of the BCRP and inhibitors Ko143 or YHO-13177 of the fluorescent substrates by co-incubation processes. The method has the advantages that the medicine trans-cell-membrane transport in-vitro models for the research on the BCRP mediation for the 3D organs of the small intestines of the mice are built for the first time, and the method for building the models is easy and convenient to implement and high in detection efficiency and speed and can be widely applied to screening BCRP substrates and inhibitors in an in-vitro manner.

Method for building BCRP (breast cancer resistance proteins) mediated medicine transport models for research on 3D (three-dimensional) organs of small intestines and application

Provided are an anti-ErbB2 antibody-drug conjugate, a composition comprising same, a preparation method therefor, and application thereof.

Anti-erbb2 antibody-drug conjugate and composition thereof, preparation method therefor, and application thereof

The present invention relates to immunoconjugates anti-AXL antibodies and compositions for treatment of non-small cell lung cancer.

Axl-specific antibodies for treatment of non-small cell lung cancer

Disclosed are a class of anti-human EGFR antibody drug conjugates and preparation method and application thereof. The anti-human EGFR antibody drug conjugate has the structure represented by formula (I). In the present invention, by means of using SCT-200 fully humanized monoclonal antibody, and coupling with Linker-MMAE by means of the chemical method of reducing the disulfide bonds between antibody chains, a class of anti-human EGFR antibody drug conjugates targeting EGFR for the treatment of solid tumors is constructed. The novel antibody drug conjugate SCT-200-Linker-MMAE provided by the present invention, in comparison with SCT-200 itself, does not affect the affinity, endocytic activity, and targeting of the antibody, better retains its biological function, and, in comparison with SCT-200, the activity is significantly improved, and can significantly inhibit the expression of related proteins during the process of tumor apoptosis, greatly improving the tumor inhibition effect.

Class of anti-human egfr antibody drug conjugate and preparation method and application thereof

ThThe invention provides a disubstituted maleic amide connexon coupled with an antibody as well as a preparation method and an application thereof, and concretely provides a new kind of connexon whichis used for coupling a substance with high cytotoxic activity and a biomacromolecule. The kind of connexon can be selectively effected on a disulfide chain, and substance homogeneity of a conjugate is substantially improved. A conjugate prepared by the connexon has high inhibitory activity for cell strains for expressing corresponding antigens. The invention also provides a preparation method andan application of the conjugate.

Disubstituted maleic amide connexon for coupling antibody and medicament as well as preparation method and application thereof

The invention discloses an antibody-drug conjugate Pertuzumab-MCC-DM1 (P-DM1) having a structure represented by a formula shown in the specification, and a therapeutic agent composition containing the P-DM1 and an HER2 dimerization inhibitor antibody. The therapeutic agent composition contains a therapeutically effective amount of the P-DM1 and a therapeutically effective amount of the HER2 dimerization inhibitor antibody. The invention also discloses a method for treating higher proliferation diseases of illnesses. The method is characterized in that the therapeutically effective amount of the P-DM1 and the therapeutically effective amount of the HER2 dimerization inhibitor antibody are applied to mammals or people needing like treatment. Pertuzumab is coupled with maytenin alkaloid DM1 to obtain the conjugate P-DM1, and the composition containing the conjugate P-DM1 and the HER2 dimerization inhibitor antibody has synergistic effects in cancer growth inhibition in vivo and in vitro in order to realize a good treatment effect on HER2 mediated illnesses, such as cancers.

Antibody-drug conjugate Pertuzumab-MCC-DM1, conjugate and Trastuzumab composition, and application of conjugate and composition

The invention provides a double-substituted maleic amide connexon coupled with an antibody as well as a preparation method and application of the connexon. Particularly, a strong cytotoxic activity substance and biological macromolecules are coupled through a kind of new connexon. The kind of connexon can selectively act with a disulfide chain at the same time, so that the substance homogeneity and stability of a conjugate are greatly improved. The conjugate prepared from the connexon has high inhibitory activity for cell strains which express corresponding antigens. The invention further provides a preparation method and application of the conjugate.

Double-substituted maleic amide connexon for antibody-medicine coupling as well as preparation method and application of connexon

Provided in the present invention are a di-substituted maleic amide linker conjugated to an antibody and a preparation method and use thereof. In particular, the present invention conjugates a strongly cytotoxic active substance to a biomacromolecule through a class of new linkers. The class of linkers can selectively act simultaneously with disulphide chains, so as to greatly improve the substance homogeneity of a conjugate. The conjugate prepared by the linker of the present invention has a high inhibitory activity on a cell strain expressing the corresponding antigen. Also provided is a method for preparing the above-mentioned conjugate and the use.

Di-substituted maleic amide linker for antibody-drug conjugating and preparation method and use thereof

Disclosed are a new AXL-targeting monoclonal antibody and antibody-drug conjugate. Also disclosed is a method for preparing said antibody and antibody-drug conjugate. The AXL antibody of the present invention can bind with purified human AXL protein and multiple AXL on tumor cell surface with high effectiveness and high specificity. Said humanized antibody also has high affinity and low immunogenicity. Said AXL antibody-drug conjugate has markable performance against tumors having high AXL expression.

Axl-targeting antibody, antibody-drug conjugate, preparation method therefor, and use thereof

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