BAY-985

SKU: orb1219742

Description

BAY-985 is a potent, selective, and orally active ATP-competitive dual inhibitor of TBK1 and IKKε (IC50s: 2/30 and 2 nM for TBK1 (low/high ATP) and IKKε) with antitumor efficacy.BAY-985 inhibits FLT3, RSK4, DRAK1, and ULK1 (IC50s: 123, 276, 311, and 7930 nM). BAY-985 inhibits the cellular phosphorylation of interferon regulatory factor 3 (IRF3, IC50: 74 nM). BAY-985 shows anti-proliferative activity in a few cancer cell lines (IC50s: 900 and 7260 nM for SK-MEL2 (NRAS and TP53 mutated) and ACHN (CDKN2A mutated) cells).BAY-985 (200 mg/kg; p.o.; b.i.d.; 111 days) results in weak antitumor efficacy. BAY-985 shows high clearance (CLb= 4.0 L/h/kg, ca. 95% hepatic extraction), large volume of distribution at steady state (Vss=2.9 L/kg) and a short terminal half-life (t1/2=0.79 h).

Key Properties

• CAS Number: 2409479-29-2
• MW: 553.58
• Purity: >98% (HPLC)
• Formula: C₂₇H₃₀F₃N₉O
• SMILES: C[C@@H](N1CCN(CC1)C(=O)CC(F)(F)F)c1ccnc(Nc2nc3ccc(cc3[nH]2)-c2cc(ncn2)N(C)C)c1
• Target: IκB kinase (IKK)
• Solubility: DMSO:50 mg/mL (90.32 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  Animal model: Female NMRI nude mice bearing SK-MEL-2 human melanoma xenograft model. Dosage: 200 mg/kg. Administration: Applied p.o. ; twice daily (b. i. d.) continuously 111 days. Result: Treatment resulted in weak antitumor efficacy with a T/Ctumor weight ratio of 0.6. The treatment was well tolerated, with a maximum body weight loss of less than 10%.
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• In Vitro:
  Cell Proliferation Assay Cell line: ACHN and SK-MEL-2 cell lines. Concentration: Incubation time: 96 hours. Result: Inhibited proliferation in SK-MEL2 and ACHN cells with IC50s of 900 and 7260 nM, respectively.
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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

IκB kinase (IKK)