[CAS NO. 1595275-62-9] Tesirine

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PRODUCTS SPECIFICATIONS [1595275-62-9]

Catalog

HY-128952

Brand

MCE

CAS

1595275-62-9

DESCRIPTION [1595275-62-9]

Overview

MDL	-
Molecular Weight	1496.65
Molecular Formula	C75H101N9O23
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

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

Summary

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 IC ₅₀ s 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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02819999	AbbVie	Small Cell Lung Cancer	October 2016	Phase 1
NCT05190705	Shayna Sarosiek, MD\|ADC Therapeutics S.A.\|Dana-Farber Cancer Institute	Waldenstrom Macroglobulinemia	February 17, 2022	Phase 2
NCT03033511	AbbVie	Small Cell Lung Cancer	February 7, 2017	Phase 3
NCT04705454	ADC Therapeutics S.A.	Relapsed or Refractory Diffuse Large B-Cell Lymphoma (R+R DLBCL)
NCT05270057	Medical College of Wisconsin	B-cell Lymphoma\|Burkitt Lymphoma	December 2022	Phase 1
NCT02674568	AbbVie	Small Cell Lung Cancer	January 25, 2016	Phase 2
NCT03543358	AbbVie	Cancer	September 10, 2018	Phase 2
NCT01901653	Stemcentrx	Recurrent Small Cell Lung Cancer	July 2013	Phase 1\|Phase 2
NCT04970901	ADC Therapeutics S.A.	B-Cell Non-Hodgkin Lymphoma\|Relapsed B-Cell Non-Hodgkin Lymphoma\|Refractory B-Cell Non-Hodgkin Lymphoma	June 17, 2022	Phase 1
NCT02874664	Stemcentrx	Small Cell Lung Carcinoma	September 2016	Phase 1
NCT03061812	AbbVie	Small Cell Lung Cancer	April 11, 2017	Phase 3
NCT04384484	ADC Therapeutics S.A.	Relapsed Diffuse Large B-Cell Lymphoma\|Refractory Diffuse Large B-Cell Lymphoma	September 16, 2020	Phase 3
NCT02432235	ADC Therapeutics S.A.	Hodgkin Lymphoma\|Non-Hodgkin Lymphoma	October 5, 2015	Phase 1
NCT05296070	University of Miami\|ADC Therapeutics S.A.	Marginal Zone Lymphoma	June 21, 2022	Phase 2
NCT04998669	Juan P. Alderuccio, MD\|ADC Therapeutics S.A.\|University of Miami	Follicular Lymphoma	February 11, 2022	Phase 2
NCT05053659	Brian Hill, MD, PhD\|Case Comprehensive Cancer Center	Relapsed Non Hodgkin Lymphoma\|Refractory Non-Hodgkin Lymphoma	September 2022	Phase 1
NCT03000257	AbbVie	Advanced Solid Tumors	December 14, 2016	Phase 1
NCT04052997	ADC Therapeutics S.A.	Relapsed Hodgkin Lymphoma\|Refractory Hodgkin Lymphoma	September 13, 2019	Phase 2
NCT05222438	Barbara Ann Karmanos Cancer Institute	Relapsed Diffuse Large B-cell Lymphoma	April 8, 2022	Phase 2
NCT04699461	ADC Therapeutics S.A.	Relapsed Follicular Lymphoma\|Refractory Follicular Lymphoma	November 4, 2021	Phase 2
NCT03334487	AbbVie	Small Cell Lung Cancer	March 15, 2018	Phase 3
NCT03503890	AbbVie	Small Cell Lung Cancer
NCT05453396	University of Washington	Post-Transplant Lymphoproliferative Disorder\|Recurrent B-Cell Non-Hodgkin Lymphoma\|Recurrent Diffuse Large B-Cell Lymphoma\|Recurrent Follicular Lymphoma\|Recurrent Mantle Cell Lymphoma\|Recurrent Neoplastic Post-Transplant Lymphoproliferative Disorder\|Refractory B-Cell Non-Hodgkin Lymphoma\|Refractory Diffuse Large B-Cell Lymphoma\|Refractory Follicular Lymphoma\|Refractory Mantle Cell Lymphoma\|Refractory Neoplastic Post-Transplant Lymphoproliferative Disorder	January 1, 2023	Phase 2
NCT03589469	ADC Therapeutics S.A.	Diffuse Large B-Cell Lymphoma Refractory\|Diffuse Large B-cell Lymphoma Recurrent	August 1, 2018	Phase 2
NCT02709889	AbbVie	Malignant Melanoma\|Medullary Thyroid Cancer\|Glioblastoma\|Large-Cell Neuroendocrine Carcinoma\|Neuroendocrine Prostate Cancer\|High Grade Gastroenteropancreatic Neuroendocrine Carcinoma\|Other Neuroendocrine Carcinoma\|Other Solid Tumors	September 23, 2016	Phase 1\|Phase 2
NCT03086239	AbbVie	Small Cell Lung Cancer	April 28, 2017	Phase 1
NCT05144009	ADC Therapeutics S.A.	Diffuse Large B-cell Lymphoma	June 21, 2022	Phase 2
NCT05600686	Joseph Tuscano\|National Cancer Institute (NCI)\|ADC Therapeutics\|University of California, Davis	Double-Expressor Lymphoma\|High Grade B-Cell Lymphoma With MYC and BCL2 and+or BCL6 Rearrangements\|High Grade B-Cell Lymphoma With MYC and BCL2 or BCL6 Rearrangements\|High Grade B-Cell Lymphoma With MYC, BCL2, and BCL6 Rearrangements	December 1, 2022	Phase 2
NCT03685344	ADC Therapeutics S.A.	Diffuse Large B-Cell Lymphoma\|Mantle Cell Lymphoma\|Follicular Lymphoma	February 4, 2019	Phase 1
NCT05228249	Fred Hutchinson Cancer Center\|ADC Therapeutics	Recurrent Diffuse Large B-Cell Lymphoma\|Recurrent Diffuse Large B-Cell Lymphoma, Not Otherwise Specified\|Recurrent High Grade B-Cell Lymphoma With MYC and BCL2 or BCL6 Rearrangements\|Recurrent Primary Mediastinal (Thymic) Large B-Cell Lymphoma\|Recurrent Transformed Follicular Lymphoma to Diffuse Large B-Cell Lymphoma\|Refractory Diffuse Large B-Cell Lymphoma\|Refractory Diffuse Large B-Cell Lymphoma, Not Otherwise Specified\|Refractory High Grade B-Cell Lymphoma With MYC and BCL2 or BCL6 Rearrangements\|Refractory Primary Mediastinal (Thymic) Large B-Cell Lymphoma\|Refractory Transformed Follicular Lymphoma to Diffuse Large B-Cell Lymphoma	December 7, 2022	Phase 1
NCT03684694	ADC Therapeutics S.A.	Diffuse Large B-Cell Lymphoma\|Mantle Cell Lymphoma	December 1, 2018	Phase 1\|Phase 2
NCT04974996	ADC Therapeutics S.A.	Diffuse Large B-Cell Lymphoma	February 1, 2022	Phase 1
NCT05464719	M.D. Anderson Cancer Center	Large B-cell Lymphoma\|Lymphoma	September 23, 2022	Phase 2
NCT03026166	AbbVie\|Bristol-Myers Squibb	Small Cell Lung Cancer	March 30, 2017	Phase 1\|Phase 2

Appearance

Solid

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.