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AZD 4205

Chemical Structure : AZD 4205

CAS No.: 2091134-68-6

AZD 4205 (AZD4205, Golidocitinib)

Catalog No.: PC-61986Not For Human Use, Lab Use Only.

Golidocitinib (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Golidocitinib (AZD4205) is a potent, selective JAK1 inhibitor IC50 of 73 nM and Ki of 2.8 nM, shows high selectivity against JAK2 and JAK3 with IC50 of 13,233 nM and >30,000 nM respectively.
Golidocitinib (AZD4205) shows potent inhibition of p-STAT3 in a cell based assay of JAK1 activity with an IC50 of 128 nM and excellent selectivity across the kinome.
Golidocitinib (AZD4205) reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.

Physicochemical Properties

M.Wt 521.601
Formula C25H31N9O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(R)-N-(3-(2-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-1H-indol-7-yl)-2-(4-methylpiperazin-1-yl)propanamide

References

1. Jason G. Kettle, et al. AACR Abstract 979: Discovery of the JAK1 selective kinase inhibitor AZD4205.

2.  Patent: WO 2017050938 A1 20170330, Example 32.

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