Uzansertib (INCB053914) phosphate 是一种具有口服活性的，ATP 竞争性泛-PIM 激酶抑制剂，对于 PIM1，PIM2 和 PIM3 的 IC₅₀ 分别为 0.24 nM，30 nM 和 0.12 nM。Uzansertib phosphate 对多种血液肿瘤细胞系具有广泛的抗增殖活性。

Uzansertib (INCB053914) phosphate is an orally active, ATP-competitive pan-PIM kinase inhibitor with IC 50 s of 0.24 nM, 30 nM, 0.12 nM for PIM1, PIM2, PIM3, respectively. Uzansertib phosphate has broad anti-proliferative activity against a variety of hematologic tumor cell lines.

Solid

PIM1 0.24 nM (IC50) PIM2 30 nM (IC50

Uzansertib phosphate inhibits proliferation in all multiple myeloma (MM) cell lines tested, with mean GI50 values ranging from 13.2 nM to 230.0 nM in AML, MM, DLBCL, MCL, and T-ALL cell lines.
Uzansertib phosphate (0.1, 0.3, 1, 3, 10, 30, 100, 300, 1000 nM) inhibits the phosphorylation of downstream PIM kinase substrates (p70S6K/S6 and 4E-BP1) in a dose-dependent manner in MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) cell lines.
PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells is particularly sensitive to inhibition by Uzansertib phosphate (mean IC50, 4 nM and 27 nM, respectively).
has not independently confirmed the accuracy of these methods. They are for reference only.

Uzansertib phosphate (25-100 mg/kg; PO; twice a day; for 15 days) inhibits tumor growth in a dose-dependent manner in mice bearing MOLM-16 (AML) or KMS-12-BM (MM) .
Uzansertib phosphate demonstrates a dose-dependent inhibition of BAD phosphorylation relative to vehicle at 4 hours post dose (MOLM-16 tumors, IC 50 =70 nM; KMS-12-BM tumors, IC 50 =145 nM) .
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Koblish H, et al. Preclinical characterization of INCB053914, a novel pan-PIM kinase inhibitor, alone and in combination with anticancer agents, in models of hematologic malignancies. PLoS One. 2018 Jun 21;13(6):e0199108.

In Vitro: DMSO : 5 mg/mL (8.18 mM; Need ultrasonic and warming)配制储备液