GDC-0339

Research use only, not for human use.

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

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

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.

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.

GDC-0339 | GDC 0339 | GDC0339

JAK/STAT Signaling

Pim

Pim

Cancer

Blood cancer

1428569-85-0

465.4952

C20H22F3N7OS

>98% (HPLC)

DMSO: ≥ 52 mg/mL

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

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)-

(-20℃)

With Ice Pack

≥ 2 years