Tesirine intermediate-2

Cat. No.: HY-24144 Purity: 98.82%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Tesirine intermediate-2 is the intermediate of Tesirine (HY-128952). Tesirine (SG3249), a pyrrole benzodiazepine (PBD) dimer, is a DNA small channel crosslinker with strong cytotoxicity. Tesirine can be used to synthesize Antibody-Drug Conjugates (ADCs), the warhead component of the payload is SG3199 (HY-101161), which has strong anticancer cell activity.

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

Tesirine intermediate-2 Chemical Structure

CAS No. : 1430738-34-3

Size	Price	Stock	Quantity
1 mg	USD 286	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 659	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 1055	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 2220	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 3560	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 5700	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Purity & Documentation
References
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Description

Molecular Weight

793.98

Formula

C₄₀H₅₅N₅O₁₀Si

CAS No.

1430738-34-3

Appearance

Solid

Color

White to off-white

SMILES

CC(C)(C)[Si](C)(C)O[C@@H]1N(C2=CC(O)=C(OC)C=C2C(N3[C@@]1([H])CC(C)=C3)=O)C(OCC4=CC=C(C=C4)NC([C@H](C)NC([C@H](C(C)C)NC(OCC=C)=O)=O)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 200 mg/mL (251.90 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	1.2595 mL	6.2974 mL	12.5948 mL
5 mM	0.2519 mL	1.2595 mL	2.5190 mL
10 mM	0.1259 mL	0.6297 mL	1.2595 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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

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 90% Corn Oil
Solubility: ≥ 5 mg/mL (6.30 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).

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: 98.82%

Select Batch:

Data Sheet (273 KB) SDS (251 KB)

COA (251 KB) HNMR (260 KB) LCMS (104 KB)

Handling Instructions (2659 KB)

References

[1]. Howard, et al. Process for the preparation of intermediates useful for the synthesis of pyrrolobenzodiazepine dimers. World Intellectual Property Organization, WO2013053872 A1. 2013-04-18.

[2]. 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]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.2595 mL	6.2974 mL	12.5948 mL	31.4869 mL
	5 mM	0.2519 mL	1.2595 mL	2.5190 mL	6.2974 mL
	10 mM	0.1259 mL	0.6297 mL	1.2595 mL	3.1487 mL
	15 mM	0.0840 mL	0.4198 mL	0.8397 mL	2.0991 mL
	20 mM	0.0630 mL	0.3149 mL	0.6297 mL	1.5743 mL
	25 mM	0.0504 mL	0.2519 mL	0.5038 mL	1.2595 mL
	30 mM	0.0420 mL	0.2099 mL	0.4198 mL	1.0496 mL
	40 mM	0.0315 mL	0.1574 mL	0.3149 mL	0.7872 mL
	50 mM	0.0252 mL	0.1259 mL	0.2519 mL	0.6297 mL
	60 mM	0.0210 mL	0.1050 mL	0.2099 mL	0.5248 mL
	80 mM	0.0157 mL	0.0787 mL	0.1574 mL	0.3936 mL
	100 mM	0.0126 mL	0.0630 mL	0.1259 mL	0.3149 mL