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GDC-0339

CAS No. 1428569-85-0

GDC-0339( GDC-0339 | GDC 0339 | GDC0339 )

Catalog No. M11806 CAS No. 1428569-85-0

GDC-0339 is a novel small molecule pan-Pim kinase inhibitor that was discovered as a potential treatment for multiple myeloma.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    GDC-0339
  • Note
    Research use only, not for human use.
  • Brief Description
    GDC-0339 is a novel small molecule pan-Pim kinase inhibitor that was discovered as a potential treatment for multiple myeloma.
  • Description
    GDC-0339 is a novel small molecule pan-Pim kinase inhibitor that was discovered as a potential treatment for multiple myeloma.Blood Cancer Preclinical.
  • In Vitro
    GDC-0339 is cytostatic, with an IC50 of 0.1 μM for MM.1S cells.GDC-0339 treatment reveals a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases. Cell Viability Assay Cell Line:MM.1S cells Concentration:Incubation Time:3 days Result:Inhibited cell viability.Western Blot Analysis Cell Line:MM.1S cells Concentration:0.01 μM, 0.03 μM, 0.09 μM,0.27 μM, 0.83 μM, 2.5 μM Incubation Time:4 hours Result:Induced a constellation of Pim downstream signaling events consistent with inhibition of Pim kinases.
  • In Vivo
    GDC-0339 (1-300 mg/kg; p.o; daily; for 21 days) is efficacious in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models.GDC-0339 has a half-life of t1/2=0.9 h. Animal Model:Female C.B-17 SCID mice, RPMI8226 human multiple myeloma xenograft mouse model Dosage:1mg/kg, 10 mg/kg, 50 mg/kg, 100 mg/kg, 200 mg/kg, 300 mg/kg Administration:Oral administration; once daily; for 21 days Result:Showed dose-dependent tumor growth inhibition.
  • Synonyms
    GDC-0339 | GDC 0339 | GDC0339
  • Pathway
    JAK/STAT Signaling
  • Target
    Pim
  • Recptor
    Pim
  • Research Area
    Cancer
  • Indication
    Blood cancer

Chemical Information

  • CAS Number
    1428569-85-0
  • Formula Weight
    465.4952
  • Molecular Formula
    C20H22F3N7OS
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO: ≥ 52 mg/mL
  • SMILES
    O=C(C1=C(N)SC(C2=C(F)C=CC=C2F)=N1)NC3=C(N4CC[C@@H](N)[C@H](F)CC4)N(C)N=C3
  • Chemical Name
    4-Thiazolecarboxamide, 5-amino-N-[5-[(4R,5R)-4-amino-5-fluorohexahydro-1H-azepin-1-yl]-1-methyl-1H-pyrazol-4-yl]-2-(2,6-difluorophenyl)-

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Takahashi RH, et al. Drug Metab Dispos. 2017 Aug 8. pii: dmd.117.076786.
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