Ponatinib (AP24534) is a novel potent BCR-ABL or BCR-ABLT3151 with an IC50 values of 0.37 and 2.0 nM, respectively. Ponatinib (AP24534) also inhibits other ABL kinase domain mutants at nanomolar potencies. AP24534 exhibits inhibitory activity against PDGFRα, c-Src and c-Kit (IC50 values are 1.1, 5.4 and 12.5 nM respectively) potently inhibits FGFR and VEGFR family kinases.
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
AP24534 purchased from AbMole
Transl Stroke Res. 2017 Nov 4.
Combination of Emricasan with Ponatinib Synergistically Reduces Ischemia/Reperfusion Injury in Rat Brain Through Simultaneous Prevention of Apoptosis and Necroptosis
AP24534 purchased from AbMole
Cell Experiment | |
---|---|
Cell lines | MV4-11, Kasumi-1, KG1, and EOL1 cells |
Preparation method | Cell viability assays. Cell viability was assessed using the Cell Titer 96 Aqueous One Solution Cell Proliferation Assay. Exponentially growing cell lines were plated into 96-well plates and incubated overnight at 37°C. Twenty-four hours after plating, cells were treated with compound or vehicle (dimethyl sulfoxide) for 72 hours. Absorbance was measured using a Wallac Victor microplate reader (PerkinElmer). Data are plotted as percent viability relative to vehicle-treated cells and the IC50 values (the concentration that causes 50% inhibition) are calculated using XLfit version 4.2.2 for Microsoft Excel. Data are shown as mean (±SD) from 3 separate experiments, each tested in triplicate. |
Concentrations | 0~100 nM |
Incubation time | 72 h |
Animal Experiment | |
---|---|
Animal models | MV4-11 human tumor subcutaneous xenograft model |
Formulation | aqueous 25 mmol/L citrate buffer (pH = 2.75) |
Dosages | 1, 2.5, 5, 10, and 25 mg/kg/d once daily for 4 weeks |
Administration | orally |
Molecular Weight | 532.56 |
Formula | C29H27F3N6O |
CAS Number | 943319-70-8 |
Solubility (25°C) | DMSO ≥ 40 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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.
Related Src-bcr-Abl Products |
---|
Asciminib hydrochloride
Asciminib (ABL001) hydrochloride is a potent and selective allosteric BCR-ABL1 inhibitor, which inhibits Ba/F3 cells grown with an IC50 of 0.25 nM. |
Osteogenic Growth Peptide (10-14)
Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. |
Abl Cytosolic Substrate
Abl Cytosolic Substrate is a substrate for Abelson tyrosine kinase (Abl ). |
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH
Ac-Tyr(PO3H2)-Glu-Glu-Ile-Glu-OH is a high-affinity pentapeptide to bind to the src SH2 domain (IC50≈1 µM). |
p60c-src substrate II
p60c-src substrate II is an efficient pentapeptide substrate for the tyrosine kinase pp60c-src. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.