An inhibitor of the menin-MLL1 protein-protein interaction
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Product Type

Biochemicals

Research Area

Cancer

Enzomenib

Item No. 44271

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-fluoro-2-[[4-[7-[[(1S,3S,4R)-5-methylene-2-azabicyclo[2.2.2]oct-3-yl]carbonyl]-2,7-diazaspiro[3.5]non-2-yl]-5-pyrimidinyl]oxy]-N,N-bis(1-methylethyl)-benzamide
CAS Number
2412555-70-3
Synonyms
  • DSP-5336
Molecular Formula
C33H43FN6O3
Formula Weight
590.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlDMSO: Slightly Soluble: 0.1-1 mg/ml
SMILES
O=C([C@@H]1[C@@]2([H])C(C[C@@](CC2)([H])N1)=C)N3CCC4(CC3)CN(C4)C5=NC=NC=C5OC6=C(C(N(C(C)C)C(C)C)=O)C=C(F)C=C6
InChi Code
InChI=1S/C33H43FN6O3/c1-20(2)40(21(3)4)31(41)26-15-23(34)6-9-27(26)43-28-16-35-19-36-30(28)39-17-33(18-39)10-12-38(13-11-33)32(42)29-25-8-7-24(37-29)14-22(25)5/h6,9,15-16,19-21,24-25,29,37H,5,7-8,10-14,17-18H2,1-4H3/t24-,25+,29-/m0/s1
InChi Key
JQHJEDMMWUIYCE-FVVBACEJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $138

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    5 mg

    $585

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    10 mg

    $963

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    25 mg

    $1,891

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    Cayman Chemical
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    Product Description

    Enzomenib is an inhibitor of the protein-protein interaction between menin and mixed-lineage leukemia 1 (MLL1).1 It binds to menin (Kd = 6 nM) and inhibits the menin-MLL1 interaction with an IC50 value of 1.4 nM. Enzomenib selectively inhibits the growth of MV4-11, MOLM-13, KOPN-8, and OCI-AML-3 leukemia cells (IC50s = 10, 15, 31, and 15 nM, respectively), which contain MLL rearrangement (MLL-r) or NPM1 mutations, over HL-60, MOLT-4, and Reh leukemia cells (IC50s = >10 µM for all), which do not have MLL-r or NPM1 mutations. In vivo, enzomenib (25 and 50 mg/kg) has antitumor activity in a mouse xenograft model using MV4-11 cells, which express an MLL-AF4 gene fusion.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Eguchi, K., Shimizu, T., Kato, D., et al. Preclinical evaluation of a novel orally bioavailable menin-MLL interaction inhibitor, DSP-5336, for the treatment of acute leukemia patients with MLL-rearrangement or NPM1 mutation. Blood 138(Suppl. 1), 3339 (2021).