Size | Price | Stock | Qty |
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100mg |
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500mg |
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1g |
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5g |
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10g |
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Other Sizes |
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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-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.
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].
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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].
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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.
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Molecular Formula |
C22H26CLN7O2S
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Molecular Weight |
488.01
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CAS # |
302962-49-8
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SMILES |
O=C(C1=CN=C(NC2=NC(C)=NC(N3CCN(CCO)CC3)=C2)S1)NC4=C(C)C=CC=C4Cl.[H]O[H]
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InChi Key |
XHXFZZNHDVTMLI-UHFFFAOYSA-N
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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
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Chemical Name |
N-(2-chloro-6-methylphenyl)-2-((6-(4-(2-hydroxyethyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide monohydrate.
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Synonyms |
Trade name: Sprycel; BMS-354825; BMS354825; BMS354825. Dasatinib;
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.
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