CX-6258

SKU: orb1307354

Description

CX-6258 is a potent and selective oral inhibitor of Pim kinases (Pim-1, -2, -3) with IC50 values of 5 nM, 25 nM, and 16 nM, respectively. It is used in preclinical research to investigate Pim kinase function in cancer cell proliferation and survival, both in vitro and in vivo.

Research Area

Epigenetics & Chromatin, Signal Transduction

Key Properties

• CAS Number: 1202916-90-2
• MW: 461.94
• Purity: 97.46% (May vary between batches)
• Formula: C₂₆H₂₄ClN₃O₃
• SMILES: CN1CCCN(CC1)C(=O)c1cccc(c1)-c1ccc(\C=C2\C(=O)Nc3ccc(Cl)cc23)o1
• Target: Pim
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.33 mM);DMSO:22.5 mg/mL (48.71 mM)

Bioactivity

• Target IC50:
  Pim2:25 nM|Pim1:5 nM|Pim3:16 nM
• In Vitro:
  CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively.

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

inhibit, Inhibitor, Bad, 4E-BP1, CX 6258, CX6258, CX-6258, Pim2, Pim, Pim1, Pim kinases, Pim3

Compound Identifiers

PubChem CID

44545852