GDC-0339 是可口服的、耐受性良好的泛 Pim 激酶高效抑制剂，具有研究多发性骨髓瘤的潜力，对 Pim1、Pim2 和 Pim3 作用的Ki值分别为 0.03、0.1 和 0.02 nM。

GDC-0339 is discovered as a potential treatment of multiple myeloma. GDC-0339 is an orally bioavailable and well-tolerated inhibitor of the pan-Pim kinase (Kis: 0.03 nM, 0.1 nM, and 0.02 nM for Pim1, Pim2, and Pim3, respectively).

GDC-0339 is cytostatic (IC50 of 0.1 μM for MM.1S cells). GDC-0339 treatment shows a constellation of Pim downstream signaling events. Which is consistent with inhibition of Pim kinases[2].

GDC-0339 has a half-life of t1/2=0.9 h. GDC-0339 (1-300 mg/kg; p.o; daily; for 21 days) is potently in RPMI8226 and MM.1S human multiple myeloma xenograft mouse models [2].

1428569-85-0

C20H22F3N7OS

465.5

DMSO:50 mg/mL (107.41 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years