A BRM and BRG1 inhibitor
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FHD-286

Item No. 41864

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-2-[[4-[6-[(2R,6S)-2,6-dimethyl-4-morpholinyl]-2-pyridinyl]-2-thiazolyl]amino]-1-(methoxymethyl)-2-oxoethyl]-1-(methylsulfonyl)-1H-pyrrole-3-carboxamide
CAS Number
2671128-05-3
Molecular Formula
C24H30N6O6S2
Formula Weight
562.7
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/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(NC1=NC(C2=CC=CC(N3C[C@@H](C)O[C@@H](C)C3)=N2)=CS1)[C@@H](NC(C4=CN(S(C)(=O)=O)C=C4)=O)COC
InChi Code
InChI=1S/C24H30N6O6S2/c1-15-10-29(11-16(2)36-15)21-7-5-6-18(25-21)20-14-37-24(27-20)28-23(32)19(13-35-3)26-22(31)17-8-9-30(12-17)38(4,33)34/h5-9,12,14-16,19H,10-11,13H2,1-4H3,(H,26,31)(H,27,28,32)/t15-,16+,19-/m0/s1
InChi Key
JBLQNFBXKOAIHG-FCEWJHQRSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $69

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    5 mg

    $325

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    10 mg

    $614

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    25 mg

    $1,023

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    Product Description

    FHD-286 is an inhibitor of Brahma homolog (BRM), also known as SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), and Brahma-related gene 1 (BRG1), also known as SMARCA4.1 It induces differentiation of, and reduces viability in, MV4-11 and MOLM-13 acute myeloid leukemia (AML) cells, which express mixed-lineage leukemia 1 (MLL1) rearrangements, and OCI-AML-3 AML cells, which express mutant nucleophosmin 1 (NPM1), when used at a concentration of 30 nM. FHD-286 (100 nM) decreases BRG1-chromatin and BRM-chromatin associations in MOLM-13 cells. In vivo, FHD-286 (1.5 mg/kg) decreases tumor burden and increases survival in patient-derived xenograft (PDX) mouse models of AML when used alone or in combination with venetoclax (ABT-199; Item No. 16233), OTX015 (Item No. 15947), SNDX-5613 (Item No. 40758), or decitabine (Item No. 11166).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fiskus, W., Piel, J., Collins, M., et al. BRG1/BRM inhibitor targets AML stem cells and exerts superior preclinical efficacy combined with BET or menin inhibitor. Blood 143(20), 2059-2072 (2024).