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INCB18424

Cat. No. M1787
INCB18424 Structure
Synonym:

Ruxolitinib

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 55  USD55 In stock
5mg USD 55  USD55 In stock
10mg USD 80  USD80 In stock
50mg USD 180  USD180 In stock
100mg USD 300  USD300 In stock
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Quality Control
Biological Activity

INCB18424 (Ruxolitinib), the most advanced JAK-1 and JAK-2 inhibitor, is in Phase III testing to treat myelofibrosis. INCB18424 demonstrated potent in vitro cellular activity (100-130 nM) in an engineered Ba/F3 cell line harboring the JAK2V617F mutation and EPO-independent erythroid colony growth of precursor cells from PV patients (IC50 of 67 nM) while showing lesser effect on normal colony formation from healthy donors (IC50 > 400 nM).

Product Citations
Customer Product Validations & Biological Datas
Source Leukemia (2013). Figure 2. INCB18424
Method MTS assay
Cell Lines leukemia cells
Concentrations 1 μM
Incubation Time 48 h
Results INCB18424 showed a significantly better inhibitory effect than TG101209 at concentrations below 1 μM. Both inhibitors also promoted apoptosis (Figure 2b) and delayed cell cycle progression (Figure 2c) of the AEtr leukemia cell line.
Source Leukemia (2013). Figure 1. INCB18424
Method CFU assays
Cell Lines AML1–ETO- and AE9a-transformed cells
Concentrations 150, 300, 600, 1200 nM
Incubation Time 36 h
Results Similar to the shRNA results, both inhibitors reduced the colony-forming ability of the transformed cells in a dose-dependent manner
Protocol
Cell Experiment
Cell lines Ba/F3-EpoR-JAK2V617F and HEL cell lines
Preparation method Cell proliferation assay. 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 0~10 µ M
Incubation time 48 h
Animal Experiment
Animal models myeloproliferative neoplasm mouse model
Formulation 5% dimethyl acetamide, 0.5% methocellulose
Dosages 180mg/kg began within 24 hours of cell inoculation, twice daily
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 306.37
Formula C17H18N6
CAS Number 941678-49-5
Purity 99.35%
Solubility DMSO 60 mg/mL
Storage at -20°C
References

[1] Chase A, et al. Haematologica. Ruxolitinib as potential targeted therapy for patients with JAK2 rearrangements.

[2] Mascarenhas J, et al. Curr Med Chem. Biology and Clinical Management of Myeloproliferative Neoplasms and Development of the JAK Inhibitor Ruxolitinib.

[3] Eghtedar A, et al. Blood. Phase 2 study of the JAK kinase inhibitor ruxolitinib in patients with refractory leukemias, including postmyeloproliferative neoplasm acute myeloid leukemia.

[4] Harrison C, et al. N Engl J Med. JAK inhibition with ruxolitinib versus best available therapy for myelofibrosis.

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Keywords: INCB18424, Ruxolitinib supplier, JAK, inhibitors

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