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Uzansertib phosphate

Catalog No. T12477 CAS 2088852-47-3

Synonyms: INCB053914 phosphate

Uzansertib phosphate (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).

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Uzansertib phosphate, CAS 2088852-47-3

Pack Size	Availability	Price/USD
1 mg	In stock	$ 97.00
5 mg	In stock	$ 296.00
10 mg	In stock	$ 441.00
25 mg	In stock	$ 729.00
50 mg	In stock	$ 987.00
100 mg	In stock	$ 1,390.00

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Purity: 99.75%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Uzansertib phosphate (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).
Targets&IC50	Pim1:0.24 nM, Pim3:0.12 nM, Pim2:30 nM
In vitro	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.
In vivo	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.

Synonyms	INCB053914 phosphate
Molecular Weight	611.51
Formula	C26H29F3N5O7P
CAS No.	2088852-47-3

Storage

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

Solubility Information

DMSO: 5 mg/mL (8.18 mM), Sonication and heating are recommended.

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.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Active Compound Library Anti-Cancer Clinical Compound Library Anti-Pancreatic Cancer Compound Library Reprogramming Compound Library Anti-Liver Cancer Compound Library Bioactive Compound Library Anti-Prostate Cancer Compound Library

Related Products

Related compounds with same targets

GDC-0339 BRD7389 M-110 CX-6258 CX-6258 hydrochloride Pim-1 kinase inhibitor 8 GNE-955 Quercetagetin

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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 phosphate 2088852-47-3 Chromatin/Epigenetic JAK/STAT signaling Pim cell inhibit malignancies INCB 053914 INCB-053914 INCB053914 phosphate Inhibitor orally Uzansertib Phosphate INCB053914 ATP-competitive tumor Pim kinases Uzansertib hematologic lines broad INCB-053914 Phosphate activity anti-proliferative INCB 053914 Phosphate INCB053914 Phosphate inhibitor

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