Free shipping on all orders over $ 500

Dasatinib

Cat. No. M1701
Dasatinib Structure
Synonym:

BMS-354825

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 40  USD50 In stock
10mg USD 16.8  USD21 In stock
50mg USD 52.8  USD66 In stock
100mg USD 72  USD90 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

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.

Product Citations
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).
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 488.01
Formula C22H26ClN7O2S
CAS Number 302962-49-8
Purity 99.91%
Solubility DMSO 68 mg/mL
Storage at -20°C
References

[1] Sano et al. Intern Med. Pulmonary arterial hypertension caused by treatment with dasatinib for chronic myeloid leukemia critical alert.

[2] Yang et al. Blood. Anti-tumor T cell responses contribute to the effects of dasatinib on c-KIT mutant murine mastocytoma and are potentiated by anti-OX40.

[3] Radich et al. Blood. A randomized trial of dasatinib 100 mg vs imatinib 400 mg in newly diagnosed chronic phase chromic myeloid leukemia.

[4] Sharma et al. Asia Pac J Clin Oncol. Dasatinib in chronic myeloid leukemia: A limited Indian experience.

[5] Agarwal et al. Mol Cancer Ther. Active efflux of dasatinib from the brain limits efficacy against murine glioblastoma: broad implications for the clinical use of molecularly-targeted agents.

[6] Birch et al. Biomed Chromatogr. Simple methodology for the therapeutic drug monitoring of the tyrosine kinase inhibitors dasatinib and imatinib.

[7] Noy et al. Leuk Res. Dasatinib inhibits leukaemic cell survival by decreasing PRH/Hhex phosphorylation resulting in increased repression of VEGF signalling genes.

[8] Kralj et al. J Chromatogr B Analyt Technol Biomed Life Sci. Simultaneous measurement of imatinib, nilotinib and dasatinib in dried blood spot by ultra high performance liquid chromatography tandem mass spectrometry.

[9] Kuckertz et al. Onkologie. Comparison of the effects of two kinase inhibitors, sorafenib and dasatinib, on chronic lymphocytic leukemia cells.

Related Src-bcr-Abl Products
Vodobatinib (K0706)

Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively.

DGY-06-116

DGY-06-116 is an irreversible covalent and selective inhibitor of Src with IC50 of 2.6 nM.

RK 24466

RK-24466 (KIN 001-51) is a potent and selective inhibitor of Lck that inhibits two constructs of the human lck kinase, lck (64-509) and lckcd with IC50 of < 0.001 μM and 0.002 μM, respectively.

UM-164

UM-164 is a highly potent, dual c-Src/p38inhibitor of c-Src with a binding constant Kd of 2.7 nM for c-Src and inhibits both p38α and p38β.

TP0427736 HCl

TP0427736 is a potent inhibitor of ALK5 kinase activity with an IC50 of 2.72 nM and this effect is 300-fold higher than the inhibitory effect on ALK3 (IC50 = 836 nM for ALK3). It also inhibits Smad2/3 phosphorylation in A549 cells induced by TGF-β1 with an IC50 value of 8.68 nM.

  Catalog
Abmole Inhibitor Catalog




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.