S-Ruxolitinib is the chirality of INCB018424, which is the first potent, selective, JAK1/2 inhibitor to enter the clinic with IC50 of 3.3 nM/2.8 nM, >130-fold selectivity for JAK1/2 versus JAK3.
Blood Cancer J. 2016 Oct 7;6(10):e481.
Expression of CALR mutants causes mpl-dependent thrombocytosis in zebrafish.
S-Ruxolitinib purchased from AbMole
Nature. 2014 Aug 7;512(7512):78-81.
Neuropathy of haematopoietic stem cell niche is essential for myeloproliferative neoplasms.
S-Ruxolitinib purchased from AbMole
Cell Experiment | |
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Cell lines | Ba/F3-EpoR-JAK2V617F or HEL cells |
Preparation method | Cells were seeded at 2000/well of white bottom 96-well plates, treated with compounds from DMSO stocks (0.2% final DMSO concentration), and incubated for 48 hours at 37°C with 5% CO2. Viability was measured by cellular ATP determination using the Cell-Titer Glo (Promega) luciferase reagent or viable cell counting. Values were transformed to percent inhibition relative to vehicle control, and IC50 curves were fitted according to nonlinear regression analysis of the data using PRISM GraphPad. |
Concentrations | 0~10µM |
Incubation time | 48h |
Animal Experiment | |
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Animal models | 6- to 8-week-old female BALB/c mice Ba/F3-JAK2V617F cells model |
Formulation | 5% dimethyl acetamide, 0.5% methocellulose |
Dosages | 180mg/kg, twice a day |
Administration | orally |
Molecular Weight | 306.37 |
Formula | C17H18N6 |
CAS Number | 941685-37-6 |
Solubility (25°C) | DMSO 51 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.
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