Alternate TextTo enhance service speed and avoid tariff delays, we've opened a US warehouse. All US orders ship directly from our US facility.
Home > Products > Novel inhibitors

AZD 4205

  Cat. No.:  DC20726   Featured
Chemical Structure
2091134-68-6
For research use only. We do not sell to patients.
We match the best price and quality on market.
Email:order@dcchemicals.com  sales@dcchemicals.com
Tel:+86-021-58447131
Get Quotation Now
We are official vendor of:
  • 20
  • 19
  • 18
  • 17
  • 16
  • 15
  • 14
  • 12
  • 11
  • 10
  • 9
  • 8
  • 13
  • 6
  • 5
  • 4
  • 3
  • 2
  • 1
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
Cat. No. Product name Field of application
DC31074 Isopropyl myristate Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC75868 AZ14133346 AZ14133346 (compound 36) is a potent and selective inhibitor of EGFR Exon20 insertions, with the IC50 of 85 nM. AZ14133346 plays an important role in cancer research.
DC75865 TI17 ​​TI17​​ represents a novel class of targeted anticancer agents that specifically disrupt DNA damage repair mechanisms in malignant cells.
DC75816 Nisoxetine Nisoxetine acts as a highly selective and potent noradrenaline transporter (NET) antagonist, exhibiting a binding affinity (Kd) of 0.76 nM. In addition to its antidepressant properties, nisoxetine functions as a local anesthetic by inhibiting voltage-gated sodium channels. This dual pharmacological activity makes it a compound of interest for both neurological and pain management research.
DC75641 GENZ-644282 TFA salt Genz-644282, also known as SAR402674, is a non-camptothecin inhibitor of topoisomerase I with potential antineoplastic activity. Topoisomerase I inhibitor Genz-644282 binds to and inhibits the enzyme topoisomerase I, which may result in the inhibition of repair of single-strand DNA breaks, DNA replication, and tumor cell growth in susceptible tumor cell populations.
DC75325 PSMA-617 TFA PSMA-617, also know as vipivotide tetraxetan, is a ligand used to make 177Lu-PSMA-617, which is a radioactive molecule to fight cancer. PSMA617 possesses a small peptide, which was designed to target prostate-specific membrane antigen (PSMA). PSMA617 demonstrates high radiolytic stability for at least 72 h. PSMA617 has high inhibition potency (equilibrium dissociation constant Ki=2.34±2.94 nM on LNCaP; Ki=0.37±0.21 nM enzymatically determined). 177 Lu-PSMA-617 offers a potential additional life-prolonging treatment option for men with mCRPC.
DC75202 Fosaprepitant free acid Fosaprepitant, also known as MK0517, is an antiemetic drug, administered intravenously. It is a prodrug of aprepitant. Fosaprepitant was developed by Merck & Co. and was approved. It is a prodrug of Aprepitant. It aids in the prevention of acute and delayed nausea and vomiting associated with chemotherapy treatment. Fosaprepitant is a weak inhibitor of CYP3A4, and aprepitant, the active moiety, is a substrate, inhibitor, and inducer of CYP3A4
DC74748 O4I4 O4I4 (compound 23) is a OCT4-inducing compound with metabolical stability.
DC74684 ZH8667 ZH8667 is a trace amine-associated receptor 1 (TAAR1)–Gs agonist.
DC74646 EB-PSMA-617 EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer.
X
Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.
Site Map|Privacy PolicyCopyright © 2018-2020 All Rights Reserved. Technical Support:KuuJia