Blood Cancer J. 2016 Oct 7;6(10):e481.
Expression of CALR mutants causes mpldependent thrombocytosis in zebrafish
TG101348 purchased from AbMole
Cell Experiment | |
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Cell lines | EpoBa/F3 JAK2V617F, Ba/F3p210, HEL, and K562 cells |
Preparation method | XTT Assay for Cell Proliferation, Apoptosis, and DNA Laddering Assay Approximately 2 3 103 cells were plated into microtiter-plate wells in 100 ml RPMI-1640 growth media with indicated concentrations of inhibitor. Following 72 hr incubation with TG101348, 50 ml of XTT dye (Roche; Basel, Switzerland) were added to each well and incubated for 4 hr in a CO2 incubator. The colored formazan product was measured by spectrophotometry at 450 nm with correction at 650 nm. The concentration in which 50% of the effect (i.e., inhibition of proliferation) is observed (IC50) was determined using the GraphPad Prism 4.0 software. All experiments were performed in triplicate, and the results were normalized to growth of untreated cells. Induction of apoptosis of EpoBa/F3 JAK2V617F, Ba/F3p210, HEL, and K562 cells was determined by DNA fragmentation with DMSO and increasing concentrations of inhibitor. |
Concentrations | 0~30µM |
Incubation time | 72h |
Animal Experiment | |
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Animal models | The murine BM transplant model with C57BL/6 mice |
Formulation | saline |
Dosages | twice daily (b.i.d.) at 60 mg/kg, 120 mg/kg from day 28 on for 42 days |
Administration | oral gavage |
Molecular Weight | 524.68 |
Formula | C27H36N6O3S |
CAS Number | 936091-26-8 |
Solubility (25°C) | DMSO ≥ 100 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.
[1] Geyer HL et al. Hematology. JAK2 inhibitors and their impact in myeloproliferative neoplasms.
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