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Dasatinib

Cat. No. M1701
Dasatinib Structure
Synonym:

BMS-354825

Size Price Availability Quantity
100mg USD 80 In stock
500mg USD 140 In stock
1g USD 200 In stock
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Quality Control
Biological Activity

Dasatinib (BMS-354825) is a small molecule inhibitor of both the SRC and BCR/ABL tyrosine kinases, with IC50's for the isolated kinases of 0.55 and 3.0 nM, respectively. Dasatinib also inhibits Lyn (IC50 = 8.5 nM) and Src (IC50 = 3.0 nM) kinase activities in vitro using 0.1 mg/mL poly (Glu4-Tyr) as the substrate. Dasatinib has greater potency than imatinib mesylate and has activity against the majority of kinase mutations in imatinib-resistant chronic myeloid leukemia.

Protocol
Cell Experiment
Cell lines Ba/F3 cell lines
Preparation method Cellular proliferation assays. Ba/F3 cell lines were plated in triplicate and incubated with escalating concentrations of imatinib, AMN107, or BMS-354825 for 72 hours. Proliferation was measured using a methanethiosulfonate-based viability assay (CellTiter96 Aqueous One Solution Reagent; Promega). IC50 and IC90 values are reported as the mean of three independent experiments done in quadruplicate. The inhibitor concentration ranges for IC50 and IC90 determinations were 0 to 2,000 nmol/L (imatinib and AMN107) or 0 to 32 nmol/L (BMS-354825). The imatinib concentration range was extended to 6,400 nmol/L for mutants with IC50 >2,000 nmol/L. The BMS-354825 concentration range was extended to 200 nmol/L for mutant T315I.
Concentrations 0~2000nM
Incubation time 72 h
Animal Experiment
Animal models primary human Ph+ B-ALL xenografts
Formulation dissolved in a mixture of polypropylene glycol (Sigma-Aldrich) diluted in water (50:50)
Dosages 5 mg/kg/day for two weeks
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 488.01
Formula C22H26ClN7O2S
CAS Number 302962-49-8
Purity 99.71%
Solubility DMSO
Storage at -20°C
Customer Product Validations & Biological Datas
Source Biochimica et Biophysica Acta (2017) . Figure 7. Dasatinib was supplied from Abmole Bioscience (Houston, TX, USA).
Method Flow cytometry
Cell Lines MDA-MB-231 cells
Concentrations 20 μM
Incubation Time 24 h
Results Apoptosis analysis by flow cytometry showed that shCtrl- and shCav-1-transfected MDA-MB-231 cells treated with Dasatinib for 24 h maintained high cell viability (N80%), with no disparity in apoptosis (Fig. 7B).
Rating
Product Citations
References

Pulmonary arterial hypertension caused by treatment with dasatinib for chronic myeloid leukemia critical alert.
Sano et al. Intern Med. 2012;51(17):2337-40. PMID: 22975544.

Anti-tumor T cell responses contribute to the effects of dasatinib on c-KIT mutant murine mastocytoma and are potentiated by anti-OX40.
Yang et al. Blood. 2012 Aug 30. PMID: 22936666.

A randomized trial of dasatinib 100 mg vs imatinib 400 mg in newly diagnosed chronic phase chromic myeloid leukemia.
Radich et al. Blood. 2012 Aug 28. PMID: 22915637.

Dasatinib in chronic myeloid leukemia: A limited Indian experience.
Sharma et al. Asia Pac J Clin Oncol. 2012 Jul 6. PMID: 22897916.

Active efflux of dasatinib from the brain limits efficacy against murine glioblastoma: broad implications for the clinical use of molecularly-targeted agents.
Agarwal et al. Mol Cancer Ther. 2012 Aug 13. PMID: 22891038.

Simple methodology for the therapeutic drug monitoring of the tyrosine kinase inhibitors dasatinib and imatinib.
Birch et al. Biomed Chromatogr. 2012 Aug 6. PMID: 22886846.

Dasatinib inhibits leukaemic cell survival by decreasing PRH/Hhex phosphorylation resulting in increased repression of VEGF signalling genes.
Noy et al. Leuk Res. 2012 Aug 5. PMID: 22874537.

Simultaneous measurement of imatinib, nilotinib and dasatinib in dried blood spot by ultra high performance liquid chromatography tandem mass spectrometry.
Kralj et al. J Chromatogr B Analyt Technol Biomed Life Sci. 2012 Aug 15;903:150-6. PMID: 22857863.

Comparison of the effects of two kinase inhibitors, sorafenib and dasatinib, on chronic lymphocytic leukemia cells.
Kuckertz et al. Onkologie. 2012;35(7-8):420-6. PMID: 22846973.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Dasatinib, BMS-354825 supplier, Src-bcr-Abl, inhibitors

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