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Tesirine

CAT: 0804-HY-128952-01Size: 1 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-128952-01Size:1 mg
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Description
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 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].
CAS Number
1595275-62-9
Product Name Alternative
SG3249
UNSPSC
12352203
Target
DNA Alkylator/Crosslinker; Drug-Linker Conjugates for ADC
Type
ADC Related
Related Pathways
Antibody-drug Conjugate/ADC Related; Cell Cycle/DNA Damage
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/mp-peg8-va-pabc.html
Purity
98.31
Solubility
DMSO : 200 mg/mL (ultrasonic)
Smiles
O=C(NC1=CC=C(COC(N2[C@@H](O)[C@@](CC(C)=C3)([H])N3C(C4=CC(OC)=C(OCCCCCOC5=C(OC)C=C6C(N7[C@](CC(C)=C7)([H])C=NC6=C5)=O)C=C42)=O)=O)C=C1)[C@H](C)NC([C@H](C(C)C)NC(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(CCN8C(C=CC8=O)=O)=O)=O)=O
Molecular Formula
C75H101N9O23
Molecular Weight
1496.65
References & Citations
[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. |[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.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, protect from light, stored under nitrogen)
Scientific Category
ADC Related
Clinical Information
Phase 3
Isoform
Pyrrolobenzodiazepines

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