Belizatinib (TSR-011)

"Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). "

Belizatinib (TSR-011) Chemical Structure

Belizatinib (TSR-011) Chemical Structure

CAS No. 1357920-84-3

Purity & Quality Control

Belizatinib (TSR-011) Related Products

Signaling Pathway

Biological Activity

Description "Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). "
Targets
TrkA [1] TrkB [1] TrkC [1] TrkA [1] TrkB [1] Click to View More Targets
In vitro
In vitro TSR-011 has high affinity for wild-type recombinant ALK kinase activity, with an IC50 value of 0.7 nM and inhibits tropomyosin receptor kinase (TRK) A, B, and C (IC50 < 3nM)[1].
In Vivo
In vivo TSR-011 exerts sustained potent inhibition of ALK-dependent tumour growth in mouse models. It is well-tolerated[1].

Chemical Information & Solubility

Molecular Weight 577.73 Formula

C33H44FN5O3

CAS No. 1357920-84-3 SDF Download Belizatinib (TSR-011) SDF
Smiles CC(C)NC(=O)C1CCC(CC1)N2C3=C(C=CC(=C3)CN4CCC(CC4)C(C)(C)O)N=C2NC(=O)C5=CC=C(C=C5)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (173.09 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

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In vivo Formulation Calculator (Clear solution)

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

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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