Identification | Back Directory | [Name]
MP-PEG8-VA-PABC-PBD Dimer | [CAS]
1595275-62-9 | [Synonyms]
SG3249 SG-3249 MP-PEG8-VA-PABC-PBD Dimer L-Alaninamide, N-[31-(2,5-dihydro-2,5-dioxo-1H-pyrrol-1-yl)-1,29-dioxo-4,7,10,13,16,19,22,25-octaoxa-28-azahentriacont-1-yl]-L-valyl-N-[4-[[[[(11S,11aS)-8-[[5-[[(11aS)-5,11a-dihydro-7-methoxy-2-methyl-5-oxo-1H-pyrrolo[2,1-c][1,4]benzodiazepin-8-yl]oxy]pentyl]oxy]-11,11a-dihydro-11-hydroxy-7-methoxy-... | [Molecular Formula]
C75H101N9O23 | [MDL Number]
MFCD32220462 | [MOL File]
1595275-62-9.mol | [Molecular Weight]
1496.65 |
Chemical Properties | Back Directory | [Boiling point ]
1428.0±65.0 °C(Predicted) | [density ]
1.33±0.1 g/cm3(Predicted) | [solubility ]
DMSO : 200 mg/mL (133.63 mM; Need ultrasonic) | [form ]
Solid | [pka]
12.42±0.40(Predicted) | [color ]
White to light yellow |
Hazard Information | Back Directory | [Uses]
Tesirine (SG3249) is an antibody-drug conjugate (ADC) pyrrolobenzodiazepine (PBD) dimer payload. Tesirine combines potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics. SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 retains picomolar activity in a panel of cancer cell lines. PBD dimers are highly efficient DNA minor groove cross-linking agents with potent cytotoxicity[1][2]. | [IC 50]
Pyrrolobenzodiazepines | [References]
[1] Tiberghien AC, et al. Design and Synthesis of Tesirine, a Clinical Antibody-Drug Conjugate Pyrrolobenzodiazepine Dimer Payload. ACS Med Chem Lett. 2016;7(11):983-987. Published 2016 May 24. DOI:10.1021/acsmedchemlett.6b00062 [2] Hartley JA, et al. Pre-clinical pharmacology and mechanism of action of SG3199, the pyrrolobenzodiazepine (PBD) dimer warhead component of antibody-drug conjugate (ADC) payload tesirine. Sci Rep. 2018;8(1):10479. Published 2018 Jul 11. DOI:10.1038/s41598-018-28533-4 |
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Twochem Co.Ltd
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