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Tesirine

SKU: orb2655870

Description

Tesirine ( SG3249) is a cathepsin B-cleavable valine-alanine pyrrolobenzodiazepine (PBD) dimer as antibody-drug conjugate (ADC) payload; Tesirine (SG3249) was designed to combine potent antitumor activity with desirable physicochemical properties such as favorable hydrophobicity and improved conjugation characteristics; Rovalpituzumab tesirine is a first-in-class antibody-drug conjugate directed against delta-like protein 3 (DLL3), a novel target identified in tumour-initiating cells and expressed in small-cell lung cancer.

Images & Validation

Key Properties

CAS Number1595275-62-9
MW1496.673
Purity>98% (HPLC)
FormulaC75H101N9O23
SMILESCC1=CN2C(C1)C=NC3=CC(=C(C=C3C2=O)OC)OCCCCCOC4=C(C=C5C(=C4)N(C(C6CC(=CN6C5=O)C)O)C(=O)OCC7=CC=C(C=C7)NC(=O)C(C)NC(=O)C(C(C)C)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCN8C(=O)C=CC8=O)OC
TargetDrug-Linker Conjugates
SolubilityIn Vitro: DMSO : 200 mg/mL (133.63 mM)

Bioactivity

In Vitro
Tesirine (SG3199) is the released warhead component of the ADC payload Tesirine. Tesirine inhibits K562, NCIN87, BT474, and SKBR3 cancer cells with IC50s of 150 pM, 20 pM, 1 nM and 320 pM.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SG3249 | SG-3249

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Tesirine (orb2655870)

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