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).
FASEB J. 2023 Feb;37(2):e22693.
ANGPTL4 inhibits granulosa cell proliferation in polycystic ovary syndrome by EGFR/JAK1/STAT3‐mediated induction of p21
INCB18424 purchased from AbMole
Front Immunol. 2022 May 23;13:866638.
A Novel STAT3 Gain-of-Function Mutation in Fatal Infancy-Onset Interstitial Lung Disease
INCB18424 purchased from AbMole
BMC Biol. 2021 May 20;19(1):108.
Very long intergenic non-coding (vlinc) RNAs directly regulate multiple genes in cis and trans
INCB18424 purchased from AbMole
Blood Adv. 2020 Jul 14;4(13):3000-3010.
Inflammation-driven activation of JAK/STAT signaling reversibly accelerates acute myeloid leukemia in vitro
INCB18424 purchased from AbMole
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
INCB18424 purchased from AbMole
Cell Experiment | |
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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 | |
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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 |
Molecular Weight | 306.37 |
Formula | C17H18N6 |
CAS Number | 941678-49-5 |
Solubility (25°C) | DMSO 60 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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GDC046
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RO495
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