MI-503

SKU: orb1296227

Description

MI-503 is a potent and selective Menin-MLL interaction inhibitor exhibiting an IC50 of 14.7 nM. It demonstrates significant anti-proliferative activity in human MLL-rearranged leukemia cell lines with GI values ranging from 250 to 570 nM, supporting its use in both in vitro and in vivo cancer research.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1857417-13-0
• MW: 564.63
• Purity: 99.99% (May vary between batches)
• Formula: C₂₈H₂₇F₃N₈S
• SMILES: Cc1c(CN2CCC(CC2)Nc2ncnc3sc(CC(F)(F)F)cc23)ccc2n(Cc3cn[nH]c3)c(cc12)C#N
• Target: Epigenetic Reader Domain,Histone Methyltransferase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.54 mM);DMSO:45 mg/mL (79.7 mM);H2O:Insoluble

Bioactivity

• Target IC50:
  Menin-MLL:4.7 nM (cell free)
• In Vivo:
  Following a single intravenous or oral administration, MI-503 rapidly attains high concentrations in peripheral blood and demonstrates significant oral bioavailability (75%). This compound effectively suppresses tumor growth through daily intraperitoneal (i.p.) doses, leading to an over 80% decrease in MV4;11 tumor volume, including complete regression in two mice. Continuous treatment over ten days notably delays the progression of mLL leukemia and substantially lowers the leukemia tumor burden in mice. Additionally, combined use of MI-503 and MI-463 significantly diminishes the expression of Hoxa9 and Meis1, indicating a potent antitumor activity.
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• In Vitro:
  Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-503 results in substantial growth inhibition (GI50: 0.22 μM). The cell growth inhibitory effect of MI-503 is time-dependent, with a pronounced effect achieved after 7-10 days of treatment.
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• Cell Research:
  Leukemia cells are treated with MI-503 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed on day 4, viable cell numbers are restored to the original concentration and MI-503 are re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader.
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• Animal Research:
  For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×10^6 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm^3. Vehicle (25% DMSO, 25% PEG400, 50% PBS) or compounds (MI-463 or MI-503) are administrated once daily at designated doses using i.p. injections.
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Storage & Handling

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

Alternative Names

MI 503, MI503, MI-503, Inhibitor, inhibit, Epigenetic Reader Domain, EpigeneticReaderDomain, Menin-MLL, Histone Methyltransferase, HistoneMethyltransferase

Compound Identifiers

PubChem CID

91667931