Tesirine (Synonyms: SG3249)

Name: Tesirine
Brand: MedChemExpress
SKU: HY-128952
Rating: 5.0 (3 reviews)

Cat. No.: HY-128952 Purity: 98.10%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 1595275-62-9

Size	Price	Stock	Quantity
1 mg	USD 2850	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 7200	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 10800	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE Tesirine

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

Pyrrolobenzodiazepines

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^[1].

MedChemExpress (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.

1595275-62-9

Appearance

Solid

Color

White to light yellow

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

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 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

This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 5 mg/mL (3.34 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 98.10%

Select Batch:

Data Sheet (278 KB) SDS (252 KB)

COA (256 KB) RP-HPLC (275 KB) LCMS (105 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	0.6682 mL	3.3408 mL	6.6816 mL	16.7040 mL
	5 mM	0.1336 mL	0.6682 mL	1.3363 mL	3.3408 mL
	10 mM	0.0668 mL	0.3341 mL	0.6682 mL	1.6704 mL
	15 mM	0.0445 mL	0.2227 mL	0.4454 mL	1.1136 mL
	20 mM	0.0334 mL	0.1670 mL	0.3341 mL	0.8352 mL
	25 mM	0.0267 mL	0.1336 mL	0.2673 mL	0.6682 mL
	30 mM	0.0223 mL	0.1114 mL	0.2227 mL	0.5568 mL
	40 mM	0.0167 mL	0.0835 mL	0.1670 mL	0.4176 mL
	50 mM	0.0134 mL	0.0668 mL	0.1336 mL	0.3341 mL
	60 mM	0.0111 mL	0.0557 mL	0.1114 mL	0.2784 mL
	80 mM	0.0084 mL	0.0418 mL	0.0835 mL	0.2088 mL
	100 mM	0.0067 mL	0.0334 mL	0.0668 mL	0.1670 mL

Tesirine Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tesirine1595275-62-9SG3249SG 3249SG-3249Drug-Linker Conjugates for ADCDNA Alkylator/Crosslinkercross-linkingPBDdimercytotoxicityantitumorDNAcancercellsInhibitorinhibitorinhibit

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Tesirine (Synonyms: SG3249)

Customer Review

Tesirine Related Antibodies

3 Publications Citing Use of MCE Tesirine

Featured Recommendations

•Related Small Molecules:

•Related Proteins:

View All Drug-Linker Conjugates for ADC Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Tesirine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Tesirine Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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