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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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| AG490
AG490 (Tyrphostin AG490) is a selective inhibitor of EGF receptor tyrosine kinase (IC50 values are 2 and 13.5 μM for EGFR and ErbB2 respectively). |
| AZ 960
AZ 960 is a novel and specific inhibitor of the JAK2 kinase with a Ki of 0.45nM in vitro. |
| Momelotinib (CYT387)
Momelotinib (CYT387) is a small-molecule, ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 and 18 nM respectively. |
| TG101348
TG101348 is a selective small-molecule Janus kinase 2 (JAK2) inhibitor with IC50 of 3 nM. |
| WP1130
Degrasyn (WP1130) is a small molecular deubiquitinase (DUB) inhibitor and suppresses JAK-Stat signaling pathway. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
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