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AZD4205

Cat. No. M10377
AZD4205 Structure
Synonym:

AZD-4205; Golidocitinib

Size Price Availability Quantity
10mM*1mL in DMSO USD 180  USD200 In stock
5mg USD 175.5  USD195 In stock
10mg USD 297  USD330 In stock
50mg USD 783  USD870 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

AZD4205 is a novel potent and selective janus kinase 1 (JAK1) inhibitor, with IC50 value of 73 nM. AZD4205 weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM). 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 489.57
Formula C25H31N9O2
CAS Number 2091134-68-6
Purity >99%
Solubility DMSO ≥ 100 mg/mL
Storage at -20°C
References

Discovery of (2 R)- N-[3-[2-[(3-Methoxy-1-methyl-pyrazol-4-yl)amino]pyrimidin-4-yl]-1 H-indol-7-yl]-2-(4-methylpiperazin-1-yl)propenamide (AZD4205) as a Potent and Selective Janus Kinase 1 Inhibitor
Qibin Su, et al. J Med Chem. 2020 May 14;63(9):4517-4527. PMID: 32297743.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: AZD4205, AZD-4205; Golidocitinib supplier, JAK, inhibitors

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