Name: Tasisulam
Brand: Selleck Chemicals
SKU: S7326
Availability: InStock
Rating: 5 (1 reviews)

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Quality Control

Batch: S732601 DMSO]83 mg/mL]false]Ethanol]83 mg/mL]false]Water]Insoluble]false Purity: 99.93%

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COA
NMR
SDS
Datasheet

99.93

Related Targets	Bcl-2 PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha Ras KRas
Other Caspase Inhibitors	Emricasan (IDN-6556) Z-VAD-FMK Q-VD-Oph Z-DEVD-FMK Belnacasan (VX-765) Z-IETD-FMK Ac-DEVD-CHO Z-LEHD-FMK TFA Z-VAD(OH)-FMK PAC-1

Solubility

In vitro
Batch:

DMSO : 83 mg/mL (199.94 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 83 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	415.11	Formula	C₁₁H₆BrCl₂NO₃S₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	519055-62-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LY573636			Smiles	C1=CC(=C(C=C1Cl)Cl)C(=O)NS(=O)(=O)C2=CC=C(S2)Br

Mechanism of Action

Targets/IC₅₀/Ki	Caspase
In vitro	Tasisulam inhibits growth of various human leukemia and lymphoma cell lines with ED50 ranging from 7 to 40 μM. This compound also induces apoptosis in HL60, Reh, and MD901 cells, mainly by loss of mitochondrial membrane potential and induction of reactive oxygen species. In addition, this chemical also produce antiproliferative activities in more than 70% of the 120 cell lines tested with EC50 of less than 50 μM. It induces G2–M accumulation and subsequent apoptosis in Calu-6 and A-375 cells. In vitro, this agent also inhibits VEGF-, FGF- and EGF-induced endothelial cord formation with EC50 of 47, 103, and 34 nM, respectively.
In vivo	Tasisulam induces morphologic features of vascular normalization, including increased pericyte coverage and decreased hypoxia in vivo. This compound (25 or 50 mg/kg, i.v.) displays dose-dependent antitumor activity, induces apoptosis, and normalizes tumor-associated vasculature in the Calu-6 non–small cell lung xenograft model. Besides, it displays potent antitumor activity across a range of in vivo xenografts, including colorectal (HCT-116), melanoma (A-375), gastric (NUGC-3), leukemia (MV-4-11), and pancreatic (QGP-1).
References	[1] https://pubmed.ncbi.nlm.nih.gov/18949427/ [2] https://pubmed.ncbi.nlm.nih.gov/21903607/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT01209832	Terminated	Advanced Cancer	Eli Lilly and Company	September 2010	Phase 1
NCT01214668	Completed	Solid Tumors	Eli Lilly and Company	January 2009	Phase 1
NCT00718159	Completed	Acute Myeloid Leukemia\|Essential Thrombocythemia	Eli Lilly and Company	August 2008	Phase 1
NCT01258348	Completed	Metastatic Renal Cell Cancer	Eli Lilly and Company	July 2008	Phase 1
NCT01215916	Completed	Solid Tumors	Eli Lilly and Company	February 2008	Phase 1
NCT00490451	Completed	Sarcoma Soft Tissue	Eli Lilly and Company	August 2007	Phase 2

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Tasisulam Caspase activator

Chemical Structure

Molecular Weight: 415.11