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  3. MI-463

MI-463 

Cat. No.: HY-19809 Purity: 99.57%
Handling Instructions

MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

For research use only. We do not sell to patients.

MI-463 Chemical Structure

MI-463 Chemical Structure

CAS No. : 1628317-18-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 192 In-stock
Estimated Time of Arrival: December 31
1 mg USD 84 In-stock
Estimated Time of Arrival: December 31
5 mg USD 180 In-stock
Estimated Time of Arrival: December 31
10 mg USD 252 In-stock
Estimated Time of Arrival: December 31
50 mg USD 564 In-stock
Estimated Time of Arrival: December 31
100 mg USD 804 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

MI-463 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

In Vitro

MI-463 can reach the target protein in mammalian cells and effectively inhibit the menin-mLL-AF9 interaction at sub-micromolar concentrations. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-463 results in substantial growth inhibition, with GI50 of 0.23 μM[1].

In Vivo

MI-463 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (45%). Pharmacologic inhibition of the menin-mLL interaction substantially delays progression of mLL leukemia in murine models through on-target activity without causing toxicity. MI-463 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. The expression of mLL fusion protein target genes, HOXA9 and MEIS1, are significant reduced upon treatment with MI-463. 20 days treatment of MV4;11 xenograft recipient mice with MI-463 also results in a substantial delay in leukemia progression as manifested by a marked decrease in the bioluminescence level which is associated with a significant decrease in the population of leukemic cells in the peripheral blood, spleen and bone marrow samples[1].

Molecular Weight

484.54

Formula

C₂₄H₂₃F₃N₆S

CAS No.

1628317-18-9

SMILES

FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(NC(C#N)=C5)C5=C4C)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (257.98 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0638 mL 10.3191 mL 20.6381 mL
5 mM 0.4128 mL 2.0638 mL 4.1276 mL
10 mM 0.2064 mL 1.0319 mL 2.0638 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.29 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.29 mM); Suspended solution; Need ultrasonic

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.29 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Leukemia cells are treated with MI-463 or 0.25% DMSO and cultured at 37 °C for 7 days. Media is changed at day 4, viable cell numbers are restored to the original concentration and MI-463 are re-supplied. MTT cell proliferation assay kit is then employed, and plates are read for absorbance at 570 nm using a microplate reader[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: For efficacy studies in MV4;11 subcutaneous xenograft mice model, 5×106 cells are injected into the 4-6 week old female BALB/c nude mice. Treatment is started when the tumor size reached ~100 mm3. 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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.57%

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Keywords:

MI-463MI463MI 463Epigenetic Reader DomainInhibitorinhibitorinhibit

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Product Name:
MI-463
Cat. No.:
HY-19809
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