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Golidocitinib (AZD4205) is a novel potent and selective janus kinase 1 (JAK1) inhibitor, with IC50 value of 73 nM. Golidocitinib (AZD4205) weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM). Golidocitinib (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.
| Molecular Weight | 489.57 |
| Formula | C25H31N9O2 |
| CAS Number | 2091134-68-6 |
| 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 |
| Related JAK Products |
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| iJak-381
iJak-381 is a JAK1/2 inhibitor with anti-inflammatory activity. |
| Ritlecitinib (malonate)
Ritlecitinib (PF-06651600) malonate is an orally active and selective JAK3 inhibitor with an IC50 of 33.1 nM. |
| Deuruxolitinib
Deuruxolitinib is a deuterated Ruxolitinib (INCB18424), which modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research of hair loss disorders. |
| A-005
A-005 is a potentially first-in-class, brain-penetrating TYK2 allosteric inhibitor for studies related to neuroinflammatory and neurodegenerative diseases. |
| Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9)
Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide corresponding to amino acids 475 to 491 of mouse JAK2. |
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