SJG-136研究進(jìn)展

SJG-136產(chǎn)品描述：SJG-136 is a novel rationally designed DNA minor groove interstrand cross-linking agent with potent and broad spectrum antitumor activity.IC50 value: 0.83 nM (TGI)Target: DNA cross-linkingin vitro: The dimeric pyrrolobenzodiazepine SJG-136 has potent in vitro antiproliferative activity associated with binding in the minor groove of DNA and formation of covalent interstrand DNA cross-links. [1] Sensitive cell lines exhibit total growth inhibition and 50% lethality after treatment with as little as 0.83 and 7.1 nmol/L SJG-136, respectively. Cell lines sensitive to SJG-136 exhibited an LC50 with as little as 7.1 nM and total growth inhibition (TGI) with as little as 0.83 nM.[2] SJG-136 selectively cross-links guanine residues located on opposite strands of DNA, and exhibits potent in vitro cytotoxicity. SJG-136 is active over a wide dosage range in athymic mouse xenografts. [3]in vivo: SJG-136 half-life, clearance and volume of distribution values were 9 min, 190 ml/min/m2, and 1


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