1. Antibody-drug Conjugate/ADC Related
    Cell Cycle/DNA Damage
  2. Drug-Linker Conjugates for ADC
    DNA Alkylator/Crosslinker
  3. Tesirine

Tesirine (Synonyms: SG3249)

Cat. No.: HY-128952 Purity: 97.96%
Handling Instructions

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.

For research use only. We do not sell to patients.

Tesirine Chemical Structure

Tesirine Chemical Structure

CAS No. : 1595275-62-9

Size Price Stock Quantity
1 mg USD 2850 In-stock
Estimated Time of Arrival: December 31
5 mg USD 9500 In-stock
Estimated Time of Arrival: December 31
10 mg USD 15500 In-stock
Estimated Time of Arrival: December 31
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

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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 (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].

IC50 & Target

Pyrrolobenzodiazepines

 

In Vitro

SG3199 (HY-101161) is the released warhead component of the ADC payload Tesirine. SG3199 inhibits K562, NCIN87, BT474, and SKBR3 cancer cells with IC50s of 150 pM, 20 pM, 1 nM and 320 pM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

1496.65

Formula

C75H101N9O23

CAS No.
SMILES

O=C(NC1=CC=C(COC(N2[[email protected]@H](O)[[email protected]@](CC(C)=C3)([H])N3C(C4=CC(OC)=C(OCCCCCOC5=C(OC)C=C6C(N7[[email protected]](CC(C)=C7)([H])C=NC6=C5)=O)C=C42)=O)=O)C=C1)[[email protected]](C)NC([[email protected]](C(C)C)NC(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(CCN8C(C=CC8=O)=O)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (133.63 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6682 mL 3.3408 mL 6.6816 mL
5 mM 0.1336 mL 0.6682 mL 1.3363 mL
10 mM 0.0668 mL 0.3341 mL 0.6682 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (3.34 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (3.34 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (3.34 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 97.96%

References
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Product Name:
Tesirine
Cat. No.:
HY-128952
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