Uzansertib phosphate

SKU: orb1309243

Description

Uzansertib phosphate (INCB053914 phosphate) is an orally bioavailable, ATP-competitive pan-PIM kinase inhibitor, demonstrating potent activity against PIM1, PIM2, and PIM3. It is a research tool used in vitro and in vivo to study oncology, hematological malignancies, and signaling pathways involving PIM kinases.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 2088852-47-3
• MW: 611.51
• Purity: 99.85% (May vary between batches)
• Formula: C₂₆H₂₉F₃N₅O₇P
• SMILES: O=C(C1=NC(C2=C(F)C=CC=C2F)=C(F)C=C1)NC3=CN=C4C(CC[C@H]4O)=C3N5C[C@@H](N)[C@H](O)[C@@H](C)C5.O=P(O)(O)O
• Target: Pim
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (1.64 mM);DMSO:5 mg/mL (8.18 mM)

Bioactivity

• Target IC50:
  Pim2:30 nM|Pim3:0.12 nM|Pim1:0.24 nM
• 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.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Pim, Pim kinases, PIM3, PIM2, PIM1, Uzansertib, Uzansertib Phosphate, Uzansertib phosphate, tumor, lines, inhibit, INCB 053914, INCB 053914 Phosphate, INCB053914 phosphate, INCB053914 Phosphate, INCB-053914 Phosphate, INCB053914, INCB-053914, orally, Inhibitor, hematologic, malignancies, cell, activity, ATP-competitive, anti-proliferative, broad

Compound Identifiers

PubChem CID

126673672