(ADCs) for the treatment of hematological cancers and solid tumors. Their ADCs are developed using the latest-generation pyrrolobenzodiazepine (PBD) dimer technology providing a superior therapeutic index compared to first-generation PBD ADCs in preclinical studies. PBD dimers are very potent toxins ...
Pyrrolo benzodiazepine-antibody conjugateThe present disclosure relates to the use of an antibody-drug conjugate (ADC) comprising a pyrrolobenzodiazepine (PBD) dimer and an anti-CD25 antibody in the treatment of a disorder characterized by the presence of CD25 + ve cells.Selection drawing None...
In vitro, pyrrolobenzodiazepines typically demonstrate IC50 values in the low to mid picomolar range in a variety of cell types, and unlike the anti-tubulin agents, they can induce cell death in both dividing and non-dividing cells. Fully synthetic PBD dimers are ideally suited for the role o...
This early work led to the design and synthesis of PBD dimers, the rationale being that a dimer could form two covalent bonds with guanine bases and thus enable the PBD dimer to span greater lengths of DNA via cross-linking.104 Early generations of dimerized PBD warheads such as SG2000 have...
Methods: An HPLC/MS method was used to assess the kinetics and thermodynamics of adduct formation between the PBD dimer SJG-136 and the cognate recognition sequence of the TFs NF-魏B, EGR-1, AP-1, and STAT3. CD spectroscopy, molecular dynamics simulations, and gene expression anal...
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SGN-CD33A was generated by conjugating a PBD dimer (SGD-1882) via the maleimidocaproyl-valine-alanine dipeptide linker to engineered cysteine residues (S239C) on h2H12ec (Figure 1A). The latter was introduced to facilitate precise loading of the mAb; indeed, as determined by reverse-phase li...
The present invention provides PBDs, and related PBD dimer conjugates wherein the PBDs are conjugated to antibodies that are modified so as to have at least one free conjugation site on each heavy chain, and where the conjugation is via substituents on both C2 groups of the PBD via respective...
from a C aryl group and C heterocyclyl group, are independently selected from halo and Me Sn NRR ', NO It is a dimer with each monomer consisting of (M) equation,where the R groups, or R groups of each monomer, taken together, the compound is a monomer or; are "forms a dimer ...
Compound B differs from compound 30 by only having a (CH2)3 tether between the PBD moieties, instead of a (CH2)5 tether, which reduces the lipophilicity of the released PBD dimer. The linking group is attached to the C2-phenyl group in the para rather than meta position. WO 2011/130613...