2. Epigenetics
  3. Epigenetic Reader Domain
  4. MI-3454

MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis.

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MI-3454 Chemical Structure

MI-3454 Chemical Structure

CAS No. : 2134169-43-8

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Based on 2 publication(s) in Google Scholar

MI-3454 Related Antibodies

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Description

MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis[1].

IC50 & Target

IC50: 0.51 nM (menin-MLL1 interaction)[1]
In Vitro

MI-3454 (0.001-10 μM; 7 days) strongly reduces murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1 proliferation[1].
MI-3454 (50 nM; 6 days) leads to downregulated expression of HOXA9 and MEIS1 in Human leukemic cell lines MV-4-11 cells or MOLM13[1].
MI-3454 markedly reduces the viability of leukemic cells harboring various MLL fusion proteins (MLL-AF9, MLL-AF4, MLL-ENL), with GI50 values ranging from 7 to 27 nM. MI-3454 blocks the interaction of menin with an MLL14–43 fragment encompassing the entire menin binding motif[1].
MI-3454 does not potently inhibit cytochromes P450 (<50% inhibition at 10 μM)[1].

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

MI-3454 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1
Concentration: 0.001, 0.01, 0.1, 1, 10 μM
Incubation Time: 7 days
Result: Demonstrated strong reduction of cell proliferation.

RT-PCR[1]

Cell Line: Human leukemic cell lines MV-4-11 cells or MOLM13
Concentration: 50 nM
Incubation Time: 6 days
Result: Led to downregulated expression of HOXA9 and MEIS1 and expression level of other MLL fusion target genes, including MEF2C, DLX2, HOXA10, PBX3, and FLT3.
In Vivo

MI-3454 induces complete remission or regression of leukemia in mouse models of mixed lineage leukemia 1 (MLL1)-rearranged or nucleophosmin 1 (NPM1)-mutated leukemia[1].
MI-3454 (p.o.; 120 mg/kg; one or twice daily for 7 consecutive days) sufficiently blocks leukemia progression by a once-daily treatment[1].
MI-3454 (p.o.; 100 mg/kg; b.i.d.; for 19 consecutive days) effectively blocks leukemia progression during the treatment period and markedly prolongs survival of MOLM13 xenotransplantation model mice. MI-3454 induces complete remission or blocks leukemia progression in patient-derived xenograft (PDX) models of MLL leukemia[1].
MI-3454 (100 mg/kg of PO or 15 mg/kg of IV) has a T1/2 of 3.2 hours, a Cmax of 4698 mg/mL for PO[1].
MI-3454 exhibits favorable stability in murine and human liver microsomes (t1/2=20.4 minutes and 37.1 minutes, respectively)[1].
MI-3454 demonstrates lower levels in brain and cerebrospinal fluid, suggesting limited ability to cross the blood-brain barrier[1].

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

Animal Model: 8- to 10-week-old female NSG mice (MV-4-11 xenotransplantation model of MLL leukemia)[1]
Dosage: 120 mg/kg
Administration: Orally; one or twice daily for 7 consecutive days
Result: A once-daily treatment was sufficient to block leukemia progression.
Animal Model: Female CD-1 mice[1]
Dosage: 100 mg/kg (PO) or 15 mg/kg (IV) (Pharmacokinetic Analysis)
Administration: PO or IV
Result: Had a T1/2 of 3.2 hours, a Cmax of 4698 mg/mL for PO.
Had a T1/2 of 2.4 hours, a CL of 2375 mL/hours•kg, and a Vss of 5358 mL/kg for IV.
Molecular Weight

636.73

Formula

C32H35F3N8OS
CAS No.
Appearance

Solid

Color

Light brown to brown

SMILES

O=CNC1(C2)CC2(CN3C(C#N)=CC4=C3C=CC(CN5CCC(NC6=C(C=C(CC(F)(F)F)S7)C7=NC(NC)=N6)CC5)=C4C)C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, stored under nitrogen

*In solvent : -80°C, 2 years; -20°C, 1 year (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 31.25 mg/mL (49.08 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5705 mL 7.8526 mL 15.7052 mL
5 mM 0.3141 mL 1.5705 mL 3.1410 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  20% HP-β-CD    5% Cremophor EL

    Solubility: 5 mg/mL (7.85 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (stored under nitrogen). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5705 mL 7.8526 mL 15.7052 mL 39.2631 mL
5 mM 0.3141 mL 1.5705 mL 3.1410 mL 7.8526 mL
10 mM 0.1571 mL 0.7853 mL 1.5705 mL 3.9263 mL
15 mM 0.1047 mL 0.5235 mL 1.0470 mL 2.6175 mL
20 mM 0.0785 mL 0.3926 mL 0.7853 mL 1.9632 mL
25 mM 0.0628 mL 0.3141 mL 0.6282 mL 1.5705 mL
30 mM 0.0524 mL 0.2618 mL 0.5235 mL 1.3088 mL
40 mM 0.0393 mL 0.1963 mL 0.3926 mL 0.9816 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MI-34542134169-43-8MI3454MI 3454Epigenetic Reader Domainorallymenin-MLL1interactionproliferationdifferentiationleukemiaMLL1NPM1leukemogenesisMV-4-11MOLM13Inhibitorinhibitorinhibit

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