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GDC-0339

Names

[ CAS No. ]:
1428569-85-0

[ Name ]:
GDC-0339

[Synonym ]:
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)-
5-Amino-N-{5-[(4R,5R)-4-amino-5-fluoro-1-azepanyl]-1-methyl-1H-pyrazol-4-yl}-2-(2,6-difluorophenyl)-1,3-thiazole-4-carboxamide

Biological Activity

[Description]:

GDC-0339 is a Pim kinase inhibitor with IC50 of 43.6 nM for BaF3 PIM1.IC50 value: 43.6 nM (for BaF3 PIM1), 0.04 nM (Ki, for PIM1 LC-3K)Target: Pim

[Related Catalog]:

Signaling Pathways >> JAK/STAT Signaling >> Pim
Research Areas >> Cancer

[Cell Assay]

BaF3, a murine interleukin-3 dependent pro-B cell line, parental cells, BaF3 PIM 1 cells, BaF3 PIM2 cells, and MM1.S (multiple myeloma) cells are seeded at 2 k/well, 5 k/well, 5k/well, 10 k/well, respectively, in a 384-well plate, at 45 μL/well. GDC-0339 is added at 5 μL/well. BaF3 cells (parental and transfected) are incubated over night, while MM1.S cells are incubated for 72 hours at 37°C, 5% CO2, CELL TITER GLO Reagent is added at 50 μL/well, the plates are incubated for 30 minutes, and their luminescence read on an HT Analyst. IC50/EC50 values for GDC-0339 is calculated[1].

[Related Small Molecules]

AZD1208 | PIM-447 dihydrochloride | Pim1/AKK1-IN-1 | SGI-1776 free base | CX-6258 | TP-3654 | Hispidulin | TCS PIM-1 1 | TCS-PIM-1-4a | SMI-16a | M-110 | INCB053914 phosphate | 3,3',4',5,6,7-HEXAHYDROXYFLAVONE

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C20H22F3N7OS

[ Molecular Weight ]:
465.495

[ Exact Mass ]:
465.155853

[ LogP ]:
0.43

[ Index of Refraction ]:
1.715

[ Storage condition ]:
2-8℃

Related Compounds