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.
J Virol. 2020 Feb 14;94(5):e01791-19.
Targeting Kaposi's Sarcoma-Associated Herpesvirus ORF21 Tyrosine Kinase and Viral Lytic Reactivation by Tyrosine Kinase Inhibitors Approved for Clinical Use
Dasatinib purchased from AbMole
Biochim Biophys Acta. 2017 Jan;1864(1):12-22.
Involvement of caveolin-1 in low shear stress-induced breast cancer cell motility and adhesion: Roles of FAK/Src and ROCK/p-MLC pathways.
Dasatinib purchased from AbMole
Cell Experiment | |
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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 | |
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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 |
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.
Molecular Weight | 488.01 |
Formula | C22H26ClN7O2S |
CAS Number | 302962-49-8 |
Purity | 99.91% |
Solubility | DMSO 68 mg/mL |
Storage | at -20°C |
Related Src-bcr-Abl Products |
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1NM-PP1
1NM-PP1 is a cell-permeable and potent Src family kinases inhibitor with IC50 values of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. |
TL02-59
TL02-59 is a selective, orally active Src-family kinase Fgr inhibitor with IC50 of 0.03 nM, it also inhibits Lyn and Hck with IC50s of 0.1 nM and 160 nM, respectively. |
CZC-8004
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase. |
Flumatinib mesylate
Flumatinib mesylate is a selective inhibitor of BCR-ABL/PDGFR/c-Kit with IC50s of 1.2 nM, 307.6 nM and 2662 nM, respectively. |
Asciminib
Asciminib, also known as ABL001, is a potent allosteric inhibitor of BCR-ABL, with a Kd value of 0.5-0.8 nM. |
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