A JAK1 inhibitor
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AZD 4205

Item No. 36622

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(αR)-N-[3-[2-[(3-methoxy-1-methyl-1H-pyrazol-4-yl)amino]-4-pyrimidinyl]-1H-indol-7-yl]-α,4-dimethyl-1-piperazineacetamide
CAS Number
2091134-68-6
Synonyms
  • Golidocitinib
Molecular Formula
C25H31N9O2
Formula Weight
489.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble
λmax
331 nm
SMILES
C[C@@H](N1CCN(CC1)C)C(NC2=C3C(C(C4=NC(NC5=CN(C)N=C5OC)=NC=C4)=CN3)=CC=C2)=O
InChi Code
InChI=1S/C25H31N9O2/c1-16(34-12-10-32(2)11-13-34)23(35)28-20-7-5-6-17-18(14-27-22(17)20)19-8-9-26-25(29-19)30-21-15-33(3)31-24(21)36-4/h5-9,14-16,27H,10-13H2,1-4H3,(H,28,35)(H,26,29,30)/t16-/m1/s1
InChi Key
CVCVOSPZEVINRM-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $44

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    5 mg

    $153

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    10 mg

    $283

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    25 mg

    $649

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    Product Description

    AZD 4205 is a JAK1 inhibitor (IC50 = 0.07 µM).1 It is selective for JAK1 over JAK2 (IC50 = >15 µM). AZD 4205 inhibits the phosphorylation of STAT3 in H1975 non-small cell lung cancer (NSCLC) cells (IC50 = 0.13 µM). It enhances the antitumor activity of osimertinib (AZD 9291; Item No. 16237) in an H1975 mouse xenograft model when administered at a dose of 50 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Su, Q., Banks, E., Bebernitz, G., et al. Discovery of (2R)- 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. J. Med. Chem. 63(9), 4517-4527 (2020).