Dasatinib

Name: Dasatinib
Brand: Tocris Bioscience
SKU: 6793

Tocris Bioscience, part of Bio-Techne | Catalog # 6793

Citations (47)

COA / SDS

Highly potent pan-Src/Bcr-Abl inhibitor

Key Product Details

Description:	Highly potent pan-Src/Bcr-Abl inhibitor
Alternative Names:	BMS-354825
Chemical Name:	N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	488.01

View Full Technical Details for Dasatinib

Technical Data
Citations

Biological Activity for Dasatinib

Dasatinib is a highly potent pan-Src/Bcr-Abl inhibitor (K_i values are 16 and 30 pM, respectively. Inhibits Bcr-Abl, Src, Lck, Fyn, c-kit and Yes with IC₅₀ values in the subnanomolar range. Inhibits proliferation of tumor cells in vitro and exhibits anticancer acivity in vivo in a mouse chronic myelogenous leukemia (CML) xenograft model. Inhibits replication of SARS-CoV and MERS-CoV in vitro (EC₅₀ values are 2.1and 5.5 μM, respectively). Dasatinib also enhances CD3-targeted lentiviral vector-mediated gene transfer by 3 to 10-fold. Targets and eliminates senescent cells. Orally bioavailable.

Compound Libraries for Dasatinib

Dasatinib is also offered as part of the Tocriscreen 2.0 Max, Tocriscreen Kinase Inhibitor Library, Tocriscreen Antiviral Library and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.

Technical Data for Dasatinib

M. Wt	488.01
Formula	C₂₂H₂₆ClN₇O₂S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	302962-49-8
PubChem ID	3062316
InChi Key	ZBNZXTGUTAYRHI-UHFFFAOYSA-N
Smiles	CC1=NC(NC2=NC=C(C(NC3=C(C=CC=C3Cl)C)=O)S2)=CC(N4CCN(CC4)CCO)=N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Dasatinib

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	48.8	100

Preparing Stock Solutions for Dasatinib

The following data is based on the product molecular weight 488.01.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.05 mL	10.25 mL	20.49 mL
5 mM	0.41 mL	2.05 mL	4.10 mL
10 mM	0.20 mL	1.02 mL	2.05 mL
50 mM	0.04 mL	0.20 mL	0.41 mL

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References for Dasatinib

References are publications that support the biological activity of the product.

Braun Dasatinib is a potent enhancer for CAR T cell generation by CD3-targeted lentiviral vectors. Mol.Ther.Methods Clin.Dev. 2022 PMID: 36620073
Lombardo Discovery of N-(2-chloro-6-methyl- phenyl)-2-(6-(4-(2-hydroxyethyl)- piperazin-1-yl)-2-methylpyrimidin-4- ylamino)thiazole-5-carboxamide (BMS-354825), a dual Src/Abl kinase inhibitor with potent antitumor activity in preclinical assays. J.Med.Chem. 2004 PMID: 15615512
Dyall Repurposing of clinically developed drugs for treatment of Middle East Respiratory Syndrome coronavirus infection. Antimicrob.Agents Chemother. 2014 PMID: 24841273
Das 2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide J.Med.Chem. 2006 PMID: 17154512