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Uzansertib

Catalog No. T39090 CAS 1620012-39-6

Synonyms: INCB053914

Uzansertib (INCB053914) is a potent ATP-competitive pan-PIM kinase inhibitor. It exhibits exceptional inhibitory activity against PIM1, PIM2, and PIM3 with IC50 values of 0.24 nM, 30 nM, and 0.12 nM, respectively. Furthermore, Uzansertib demonstrates significant anti-proliferative effects against an assorted range of hematologic tumor cell lines.

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Uzansertib, CAS 1620012-39-6

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Description	Uzansertib (INCB053914) is a potent ATP-competitive pan-PIM kinase inhibitor. It exhibits exceptional inhibitory activity against PIM1, PIM2, and PIM3 with IC50 values of 0.24 nM, 30 nM, and 0.12 nM, respectively. Furthermore, Uzansertib demonstrates significant anti-proliferative effects against an assorted range of hematologic tumor cell lines.
Targets&IC50	Pim1:0.24 nM (IC50), Pim3:0.12 nM (IC50), Pim2:30 nM (IC50)
In vitro	Uzansertib effectively hampers the growth of multiple myeloma (MM) and other cancer cell lines, including AML, DLBCL, MCL, and T-ALL, demonstrating a significant range in potency with mean GI50 values between 13.2 nM and 230.0 nM[1]. This compound also dose-dependently blocks the phosphorylation of key PIM kinase targets (p70S6K/S6 and 4E-BP1) across various cell lines like MOLM-16 (AML), Pfeiffer (DLBCL), and KMS-12-PE/BM (MM) at concentrations from 0.1 to 1000 nM[1]. Notably, Uzansertib shows heightened efficacy in inhibiting PIM kinase-mediated phosphorylation of BAD in MOLM-16 and KMS-12-BM cells, with mean IC50 values standing at 4 nM and 27 nM, respectively[1].
In vivo	Administered orally at doses ranging from 25 to 100 mg/kg twice daily for 15 days, Uzansertib effectively suppresses tumor growth in a dose-dependent manner in immunocompromised (severe combined immunodeficiency [SCID]) female mice aged 5-9 weeks with either MOLM-16 (acute myeloid leukemia [AML]) or KMS-12-BM (multiple myeloma [MM]) tumors[1]. Moreover, Uzansertib exhibits dose-dependent inhibition of BAD phosphorylation compared to the control group, achieving half-maximal inhibitory concentrations (IC50) of 70 nM and 145 nM for MOLM-16 and KMS-12-BM tumors, respectively, at 4 hours post-administration[1].

Synonyms	INCB053914
Molecular Weight	513.521
Formula	C26H26F3N5O3
CAS No.	1620012-39-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

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.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Uzansertib 1620012-39-6 INCB053914 INCB 053914 INCB-053914 inhibitor inhibit

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