INCB053914 phosphate 是一种可口服的 ATP 竞争性泛-Pim激酶抑制剂，对多种血液肿瘤细胞系具有广泛的抗增殖活性，对 Pim1、Pim2 和 Pim3 的IC50分别为 0.24 、30 和 0.12 nM。

INCB053914 phosphate is an orally active, ATP-competitive inhibitor of pan-PIM kinase(PIM1, PIM2, PIM3 with IC50s of 0.24 nM, 30 nM, 0.12 nM , respectively).

INCB053914, a novel, potent, and selective adenosine triphosphate-competitive pan-PIM kinase inhibitor.?In vitro, INCB053914 inhibited proliferation and the phosphorylation of downstream substrates in cell lines from multiple hematologic malignancies.

Effects were confirmed in primary bone marrow blasts from patients with acute myeloid leukemia treated ex vivo and in blood samples from patients receiving INCB053914 in an ongoing phase 1 dose-escalation study.?In vivo, single-agent INCB053914 inhibited Bcl-2-associated death promoter protein phosphorylation and dose-dependently inhibited tumor growth in acute myeloid leukemia and multiple myeloma xenografts.?Additive or synergistic inhibition of tumor growth was observed when INCB053914 was combined with selective PI3Kδ inhibition, selective JAK1 or JAK1/2 inhibition, or cytarabine.

2088852-47-3

C26H29F3N5O7P

611.51

INCB053914 phosphate

DMSO:5 mg/mL (8.18 mM),Need ultrasonic and warming
Powder: -20°C for 3 years
In solvent: -80°C for 2 years