Tesirine
Tesirine Basic information
- Product Name:
- Tesirine
- Synonyms:
-
- 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-...
- Tesirine (SG3249, MP-PEG8-VA-PABC-PBD DIMER)
- Tesirine
- 4-((2S,5S)-37-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)-5-isopropyl-2-methyl-4,7,35-trioxo-10,13,16,19,22,25,28,31-octaoxa-3,6,34-triazaheptatriacontanamido)benzyl (11S,11aS)-11-hydroxy-7-methoxy-8-((5-(((S)-7-methoxy-2-methyl-5-oxo-5,11a-dihydro-1H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-8-yl)oxy)pentyl)oxy)-2-methyl-5-oxo-11,11a-dihydro-1H-benzo[e]pyrrolo[1,2-a][1,4]diazepine-10(5H)-carboxylate
- {4-[(2S)-2-[(2S)-2-{1-[3-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)propanamido]-3,6,9,12,15,18,21,24-octaoxaheptacosan-27-amido}-3-methylbutanamido]propanamido]phenyl}methyl (7S,8S)-8-hydroxy-13-methoxy-12-[(5-{[(7S)-13-methoxy-5-methyl-2-oxo-3,9-diazatricyclo[8.4.0.03,?]tetradeca-1(14),4,8,10,12-pentaen-12-yl]oxy}pentyl)oxy]-5-methyl-2-oxo-3,9-diazatricyclo[8.4.0.03,?]tetradeca-1(14),4,10,12-tetraene-9-carboxylate
- Tesirine（SG3249）
- MP-PEG8-VA-PABC-PBD Dimer
- SG3249
- CAS:
- 1595275-62-9
- MF:
- C75H101N9O23
- MW:
- 1496.67
- Mol File:
- 1595275-62-9.mol
Tesirine Chemical Properties
- 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)
- pka
- 12.42±0.40(Predicted)
- form
- Solid
- color
- White to light yellow
- InChIKey
- HKGATZAPXCCEJR-HNGGPZSVNA-N
Tesirine Usage And Synthesis
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
TesirineSupplier
- Tel
- 0512-81877925 051281877925
- info@levena.cn
- Tel
- 021-52996696，15000506266 15000506266
- Tel
- 021-021-58111628 15800915896
- sales@twochem.com
- Tel
- 177-54423994 17754423994
- 2853530910@QQ.com
- Tel
- 010-60605840 18892239720
- psaitong@jm-bio.com