AZD4205 is a novel potent and selective janus kinase 1 (JAK1) inhibitor, with IC50 value of 73 nM. AZD4205 weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM). AZD4205 significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells with an IC50 of 161 nM.
In vivo, AZD4205 (12.5 mg/kg BID, 25 m/kg BID or 50 mg/kg BID, p.o.) alone has increasing antitumor effects, and ehances the antitumor activity of osimertinib, compared to treatment with osimertinib alone in mice bearing NCI-H1975 cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO ≥ 100 mg/mL|
Discovery of (2 R)- N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1 H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor
Qibin Su, et al. J Med Chem. 2020 May 14;63(9):4517-4527. PMID: 32297743.
|Related JAK Products|
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PF-06700841 is a potent dual Janus kinase 1 (JAK1) and TYK2 inhibitor with IC50s of 17 nM and 23 nM, respectively. PF-06700841 also inhibits JAK2 and JAK3 with IC50s of 77 nM and 6.49 μM, respectively.
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PF-06826647, also known as Tyk2-IN-8, is a selective and orally administered tyrosine kinase 2 (TYK2) inhibitor, with IC50 of 17 nM.
PF-06700841 (Brepocitinib) tosylate is a dual inhibitor of JAK1 and TYK2, with IC50 values of 17 nM and 23 nM, respectively.
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