Ro 5-3335

SKU: orb1223159

Description

Ro 5-3335 is core binding factor (CBF) inhibitor; preferentially kills human leukemia cell lines with CBF fusion proteins (IC50 = 1.1 μM). It represses RUNX1/CBFβ-dependent transactivation in reporter assays and inhibits transcriptional regulation by RUNX1 and CBFβ. It also reduces the leukemia burden in a mouse model. Attenuates RUNX1-dependent hematopoiesis in zebrafish embryos. It also is a Tat antagonist and inhibits HIV-1 replication in vitro.

Key Properties

• CAS Number: 30195-30-3
• MW: 259.69
• Purity: >98% (HPLC)
• Formula: C₁₃H₁₀ClN₃O
• SMILES: Clc1ccc2NC(=O)CN=C(c2c1)c3cccn3
• Target: CETP
• Solubility: In Vitro: DMSO : 100 mg/mL (385.07 mM)

Bioactivity

• In Vivo:
  Ro5-3335 is identified as an inhibitor of RUNX1–CBFβ function in zebrafish models. Ro5-3335 rescues preleukemic phenotype in a RUNX1-ETO transgenic zebrafish. Ro5-3335 (300 mg/kg/d; p. o; for 30 days) reduces leukemia burden in a mouse CBFB-MYH11 leukemia model. Animal model: C57BL/6 mice (leukemic model). Dosage: 300 mg/kg. Administration: Oral administration; daily; for 30 days. Result: Reduced the number of c-kit+ cells in the transplanted mice and leukemic cell infiltration in the livers, bone marrow and spleen.
• In Vitro:
  Ro5-3335 has antiproliferative activity against human CBF leukemia cell lines, with IC50s of 1.1 μM, 21.7 μM and 17.3 μM for ME-1, Kasumi-1 and REH, respectively. Ro5-3335 inhibits definitive hematopoiesis in zebrafish embryos. Ro5-3335 does not completely break apart RUNX1-CBFβ interaction, but changes the conformation of their complex or increases the distance between RUNX1 and CBFβ in the complex.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

CETP