AI-10-49

SKU: orb1941001

Description

AI-10-49 is an inhibitor that binds the transcription factor fusion CBFβ-SMMHC. AI-10-49, that selectively binds to CBFβ-SMMHC and disrupts its binding to RUNX1. AI-10-49 restores RUNX1 transcriptional activity, displays favorable pharmacokinetics, and delays leukemia progression in mice. Treatment of primary inv(16) AML patient blasts with AI-10-49 triggers selective cell death. These data suggest that direct inhibition of the oncogenic CBFβ-SMMHC fusion protein may be an effective therapeutic approach for inv(16) AML, and they provide support for transcription factor targeted therapy in other cancers.(In Vitro):AI-10-49 inhibits the binding of CBFβ-SMMHCto theRUNX1 Runt domain with IC50 value of 0.26 μM.AI-10-49 (1 μM; 3, 6, 12 hours) has selectivity for inhibiting CBFβ-SMMHC binding to RUNX1.(In Vivo):AI-10-49 (200 mg/kg; per day) delays leukemia progression in mice.

Key Properties

• CAS Number: 1256094-72-0
• MW: 660.52
• Purity: >98% (HPLC)
• Formula: C₃₀H₂₂F₆N₆O₅
• SMILES: FC(F)(F)OC1=CC=C2NC(=NC2=C1)C1=NC=C(OCCOCCOC2=CN=C(C=C2)C2=NC3=C(N2)C=CC(OC(F)(F)F)=C3)C=C1
• Target: Ephrin Receptor
• Solubility: DMSO : ≥ 34 mg/mL. 51.47 mM

Bioactivity

• In Vivo:
  Animal model: Mice (Cbfb+/MYH11: Ras+/G12D leukemic cells). Dosage: 200 mg/kg. Administration: per day. Result: Reduced leukemia expansion In vivo and survived significantly long.
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• In Vitro:
  Western blot analysis. Cell line: ME-1 cells. Concentration: 1 μM. Incubation time: 3, 6 hours. Result: Effectively dissociated RUNX1 from CBFβ-SMMHC. RT-PCR Cell line: ME-1 and U937 cells. Concentration: 1 μM. Incubation time: 6, 12 hours. Result: Increased expression of RUNX3, CSF1R, and CEBPA.
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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

Alternative Names

AI-10-49 | AI 10-49 | AI10-49

Quick Database Links

Gene Symbol

Ephrin Receptor