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SG2057 is a pentyldioxy linked PBD dimer which binds sequence selectively in the minor groove of DNA forming DNA interstrand and intrastrand cross-linked adducts, and also mono-adducts depending on sequence. SG2057 has multilog differential in vitro cytotoxicity against a panel of human tumour cell lines with a mean GI(50) of 212 pM. The agent is highly efficient at producing DNA interstrand cross-links in cells which form rapidly and persist over a 48h period. Cures were obtained in a LOX-IMVI melanoma model following a single administration and dose-dependent activity, including regression responses, observed in SKOV-3 ovarian and HL-60 promyelocytic leukemia models following repeat dose schedules. In the advanced stage LS174T model, SG2057 administered either as a single dose, or in two repeat dose schedules, was superior to irinotecan. SG2057 is therefore a highly active antitumor agent, with more potent in vitro activity and superior in vivo activity to SG2000.
| Catalog Number | Size | Price | Quantity |
|---|---|---|---|
| BADC-01380 | -- | $-- |
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BOC Sciences offers comprehensive services for ADC manufacturing, including antibody modification, linker chemistry, payload conjugation, and formulation development. In particular, our payload-linker customization service offers a convenient and fast raw material channel for many ADC researchers.
BOC Sciences provides one-stop site-specific conjugation services for amino acids, glycans, unnatural amino acids, and short peptide tags. In addition, cysteine conjugation, lysine conjugation, enzymatic conjugation, thio-engineered antibody can also be obtained quickly.
BOC Sciences offers a full range of linkers, including peptide linkers, PEG linkers, click chemistry, PROTAC linkers, non-cleavable linkers, etc. We also provide custom development services for chemically labile linkers and enzymatically cleavable linkers.
