Dasatinib (BMS354825; Sprycel)

Alias: Trade name: Sprycel; BMS-354825; BMS354825; BMS354825. Dasatinib;
Cat No.:V0629 Purity: ≥98%
Dasatinib (formerly known as BMS-354825; sold under the brand name Sprycel), is a novel, potent and multi-targeted, orally bioavailable synthetic small molecule inhibitor that targets Abl, Src and c-Kitwith potential antitumor activity.
Dasatinib (BMS354825; Sprycel) Chemical Structure CAS No.: 302962-49-8
Product category: Bcr-Abl
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
500mg
1g
5g
10g
Other Sizes

Other Forms of Dasatinib (BMS354825; Sprycel):

  • Dasatinib HCl
  • Dasatinib Monohydrate (BMS354825; Sprycel)
  • Dasatinib D8
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Dasatinib (formerly known as BMS-354825; sold under the brand name Sprycel), is a novel, potent and multi-targeted, orally bioavailable synthetic small molecule inhibitor that targets Abl, Src and c-Kit with potential antitumor activity. It inhibits Abl, Src and c-Kit with IC50s of<1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib is a chemotherapy medication used to treat certain cases of chronic myelogenous leukemia (CML) and acute lymphoblastic leukemia (ALL). Specifically it is used to treat cases that are Philadelphia chromosome-positive (Ph+)Dasatinib binds to and inhibits the growth-promoting activities of these kinases. Apparently because of its less stringent binding affinity for the BCR-ABL kinase, dasatinib has been shown to overcome the resistance to imatinib of chronic myeloid leukemia (CML) cells harboring BCR-ABL kinase domain point mutations.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Against Bcr-Abl, Src, Lck, Yes, c-Kit, PDGFRβ, p38, Her1, Her2, FGFR-1, and MEK, dasatinib exhibits noteworthy action, with IC50 values of less than 1.0, 0.50, 0.40, 0.50, 5.0, 28, 100, 180, 720, 880, and 1700 nM, respectively[1]. With an IC50 of less than 1.0 nM and 9.4 nM, respectively, dasatinib demonstrated antiproliferative action when compared to the K562 chronic myelogenous leukemia (CML), PC3 human prostate tumor, MDA-MB-231 human breast tumor, and WiDr human colon carcinoma cell line. 52 nM and 12 nM[1].
ln Vivo
Dasatinib (10 mg/kg) has a pharmacokinetic profile that is appropriate for further in vivo efficacy research. Dasatinib (5 mg/kg and 50 mg/kg, qd) has modest toxicity at different dose levels and is resolved [1]. When administered intravenously or orally, dasatinib (10 mg/kg) has a good half-life (t1/2s) of 3.3 and 3.1 hours, respectively. In this study, the oral bioavailability (Fpo) was 27% [1].
Animal Protocol
Animal/Disease Models: Nude mice bearing K562 xenografts
Doses: 5 mg/kg and 50 mg/kg
Route of Administration: Oral administration on a 5 day on and 2 day off schedule.
Experimental Results: demonstrated partial tumor regressions after one treatment cycle and complete disappearance of the tumor mass by the end of drug treatment. No toxicity (animal deaths, lack of weight gain) was observed.

Animal/Disease Models: SD (Sprague-Dawley) Rats
Doses: 10 mg/kg (pharmacokinetic/PK Analysis)
Route of Administration: Oral and iv
Experimental Results: Cmax of 13.2 and 0.5 μM for iv and po (oral gavage) respectively.
References
[1]. Lombardo LJ, et al. 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 Dec 30;47(27):6658-61.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H26CLN7O2S
Molecular Weight
488.01
CAS #
302962-49-8
SMILES
O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCO)CC3)=C2)S1)NC4=C(C)C=CC=C4Cl.[H]O[H]
InChi Key
XHXFZZNHDVTMLI-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H26ClN7O2S.H2O/c1-14-4-3-5-16(23)20(14)28-21(32)17-13-24-22(33-17)27-18-12-19(26-15(2)25-18)30-8-6-29(7-9-30)10-11-31;/h3-5,12-13,31H,6-11H2,1-2H3,(H,28,32)(H,24,25,26,27);1H2
Chemical Name
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide monohydrate.
Synonyms
Trade name: Sprycel; BMS-354825; BMS354825; BMS354825. Dasatinib;
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 98 mg/mL (200.8 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
4% DMSO+30% PEG 300+5% Tween 80+ddH2O:5 mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.0491 mL 10.2457 mL 20.4914 mL
5 mM 0.4098 mL 2.0491 mL 4.0983 mL
10 mM 0.2049 mL 1.0246 mL 2.0491 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Dasatinib

  • Dasatinib

    Dasatinib inhibits splenomegaly and lymphadenopathy in Tg6/λ-MYC mice.Antiviral Res.2012 Jul;95(1):49-56.
  • Dasatinib

    Dasatinib inhibits colony formation by bone marrow cells from LMP2A transgenic (TgE) mice.Antiviral Res.2012 Jul;95(1):49-56.
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