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  3. MI-503

MI-503 

Cat. No.: HY-16925 Purity: 99.77%
Handling Instructions

MI-503 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-503 Chemical Structure

MI-503 Chemical Structure

CAS No. : 1857417-13-0

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2 mg USD 140 In-stock
Estimated Time of Arrival: December 31
5 mg USD 240 In-stock
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10 mg USD 400 In-stock
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25 mg USD 790 In-stock
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50 mg USD 1130 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

MI-503 is a highly potent and orally bioavailable small molecule inhibitor of the menin-mLL interaction.

In Vitro

MI-503 occupies the F9 and P13 pockets on menin, forming a hydrogen bond with Tyr276, and also extends beyond the P13 pocket to form hydrogen bonds with Trp341 and Glu366. Treatment of murine bone marrow cells (BMC) transformed with the mLL-AF9 oncogene with MI-503 results in substantial growth inhibition, with GI50 of 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[1].

In Vivo

MI-503 achieves high level in peripheral blood following a single intravenous or oral dose, while also showing high oral bioavailability (75%). MI-503 induces strong inhibition of tumor growth with once daily intraperitoneal (i.p.) administration. Treatment with MI-503 results in an over 80% reduction in MV4;11 tumor volume and complete tumor regression in two mice. Ten consecutive days of treatment with MI-503 results in a marked delay in progression of mLL leukemia in mice and significantly reduces leukemia tumor burden. Treatment with MI-503 and MI-463 leads to markedly reduced expression of Hoxa9 and Meis1, downstream targets of mLL fusion proteins substantially upregulated in mLL leukemias[1].

Molecular Weight

564.63

Formula

C₂₈H₂₇F₃N₈S

CAS No.

1857417-13-0

SMILES

FC(F)(F)CC(S1)=CC2=C1N=CN=C2NC3CCN(CC4=CC=C(N(CC5=CNN=C5)C(C#N)=C6)C6=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 : 25 mg/mL (44.28 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7711 mL 8.8554 mL 17.7107 mL
5 mM 0.3542 mL 1.7711 mL 3.5421 mL
10 mM 0.1771 mL 0.8855 mL 1.7711 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 (3.68 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (3.68 mM); Clear solution

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

Leukemia cells are treated with MI-503 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-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[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: 99.77%

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Keywords:

MI-503MI503MI 503Epigenetic Reader DomainInhibitorinhibitorinhibit

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