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Golidocitinib (AZD4205) is a selective JAK1 inhibitor with an IC50 of 73 nM, while it weakly inhibits JAK2 and JAK3 with IC50 values greater than 14.7 μM and 30 μM, respectively.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $97 | In Stock | |
5 mg | $166 | In Stock | |
10 mg | $282 | In Stock | |
25 mg | $489 | In Stock | |
50 mg | $651 | In Stock | |
100 mg | $927 | In Stock | |
1 mL x 10 mM (in DMSO) | $178 | In Stock |
Description | Golidocitinib (AZD4205) is a selective JAK1 inhibitor with an IC50 of 73 nM, while it weakly inhibits JAK2 and JAK3 with IC50 values greater than 14.7 μM and 30 μM, respectively. |
Targets&IC50 | JAK1:73 nM |
In vitro | AZD4205 significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50: 161 nM). |
In vivo | AZD4205, administered orally at doses of 12.5 mg/kg, 25 mg/kg, or 50 mg/kg twice daily (BID), exhibits dose-dependent antitumor effects when used alone. Additionally, it boosts the antitumor efficacy of osimertinib when compared to the administration of osimertinib alone in mice implanted with NCI-H1975 cells. |
Alias | AZD4205 |
Molecular Weight | 489.57 |
Formula | C25H31N9O2 |
Cas No. | 2091134-68-6 |
Smiles | COc1nn(C)cc1Nc1nccc(n1)-c1c[nH]c2c(NC(=O)[C@@H](C)N3CCN(C)CC3)cccc12 |
Relative Density. | 1.38 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 250 mg/mL (510.65 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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