Umbralisib

SKU: orb1302401

Description

Umbralisib (TGR-1202) is a selective small molecule inhibitor of the delta isoform of phosphoinositide 3-kinase (PI3Kδ). It is utilized in preclinical research for studying hematological malignancies, demonstrating activity in both in vitro cellular assays and in vivo models of B-cell lymphomas.

Research Area

Metabolism Research, Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 1532533-67-7
• MW: 571.55
• Purity: 99.56%
• Formula: C₃₁H₂₄F₃N₅O₃
• SMILES: CC(C)Oc1ccc(cc1F)-c1nn([C@@H](C)c2oc3ccc(F)cc3c(=O)c2-c2cccc(F)c2)c2ncnc(N)c12
• Target: Casein Kinase,PI3K
• Solubility: 10% DMSO+90% Corn Oil:3.3 mg/mL (5.77 mM);DMSO:91 mg/mL (159.22 mM)

Bioactivity

• Target IC50:
  PI3Kα:>10000 nM (Kd)|PI3Kβ:>10000 nM (Kd)|PI3Kγ:1400 nM (Kd)|PI3Kδ:22.2 nM|PI3Kδ:6.2 nM (Kd)
• In Vivo:
  In a subcutaneous xenograft model of T-cell acute lymphoblastic leukemia (T-ALL) in NOD/SCID mice using the MOLT-4 cell line, TGR-1202 (150 mg/kg, daily p.o.) significantly shrinks the tumors by day 25.
• In Vitro:
  Umbralisib and carfilzomib synergistically kill blood cancer cells through disrupting the 4E-BP1-eIF4F-c-Myc axis. Umbralisib and carfilzomib in combination synergistically and selectively silence the c-Myc and E2F transcription programs. Umbralisib (15-50 μM) potently represses the expression of c-Myc in the DLBCL cell line LY7, and is uniquely characterized with structural features suitable for targeting CK1ε in lymphoma cells.

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

RP 5264, RP5264, RP-5264, TGR 1202, TGR1202, TGR-1202, PI3Kδ, PI3K, Phosphoinositide 3-kinase, Umbralisib, inhibit, orally active, lymphoma, lymphocytic leukemia, Inhibitor, haematological malignancies, cancer, Casein Kinase, CLL T cells

Compound Identifiers

PubChem CID

72950888