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AZD 4205

  Cat. No.:  DC20726   Featured
Chemical Structure
2091134-68-6
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More than 5000 active chemicals with high quality for research!
Field of application
AZD 4205 (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; 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; reduces residual disease and prolongs the benefit of Osimertinib in lung cancer patients with EGFR activating mutations both in vitro and in vivo.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2091134-68-6
Chemical Name: (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
Synonyms: AZD4205,AZD-4205
SMILES: O=C([C@@H](C)N1CCN(C)[C@H](C)C1)NC2=CC=CC3=C2NC=C3C4=C(F)C=NC(NC5=CN(C)N=C5OC)=N4
Formula: C25H31N9O2
M.Wt: 521.601
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 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.
Description: AZD-4205 is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively).
Target: JAK1:73 nM (IC50)
In Vivo: AZD-4205 (12.5 mg/kg BID (twice daily), 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[1].
In Vitro: AZD-4205 (Example 32) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2, and shows little inhibition on JAK3 (IC50, >14.7, >30 μM, respectively). AZD-4205 significantly inhibits STAT3 phosphorylation in NCI-H 1975 cells with an IC50 of 161 nM[1].
References: [1]. Annika Birgitta Margareta ÅSTRAND, et al. Compounds and methods for inhibiting jak
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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