I-BET567

SKU: orb2900253

Description

I-BET567 is a potent and orally active inhibitor of pan-BET candidate with pIC50s of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. I-BET567 has been demonstrated efficacy in mouse models of oncology and inflammation.

Key Properties

• CAS Number: 1887237-54-8
• MW: 359.81
• Purity: >98% (HPLC)
• Formula: C₁₇H₁₈ClN₅O₂
• SMILES: C[C@H]1C[C@@H](Nc2ncc(Cl)cn2)c2cc(ccc2N1C(C)=O)C(N)=O
• Solubility: In Vitro: DMSO : 100 mg/mL (277.92 mM; Ultrasonic )

Bioactivity

• In Vivo:
  I-BET567 (compound 27) (3, 10, and 30 mg/kg; p.o. ; once daily for 20 days) leads to a significant reduction in tumor growth compared with vehicle controls at both 10 and 30 mg/kg. Assessment of Pharmacokinetics (PK) profile of I-BET567 following intravenous infusion and oral administration in male wistar han rat and beagle doga. a: Values are mean, n = 3 unless otherwise stated. b: IV dose 1h infusion in DMSO and (10%, w/v) Kleptose HPB in saline (2%: 98% (v/v)). c: PO dose vehicle: 1%(w/v) methycellulose (400 cps) (aq). d: Mean n = 2. Animal model: NMC 11060 xenograft mouse model (NOD/SCID mouse; bearing NMC 11060 cells). Dosage: 3, 10, and 30 mg/kg. Administration: p.o. (once daily for 20 days. Result: Led to a significant reduction in tumor growth compared to vehicle controls at both 10 and 30 mg/kg.
  Read more...
• In Vitro:
  I-BET567 (compound 27) (72 hours; 1.5 nM-30 μM) effectively inhibites the proliferation of human NMC cell line 11060 in vitro with a mean gpIC50 6.2 (0.63 μM). Cell Viability Assay Cell line: NMC line 11060 cells. Concentration: 1.5 nM-30 μM Incubation time: 72 hours. Result: Significantly reduced cell growth.
  Read more...

Storage & Handling

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