An inhibitor of the menin-MLL1 fusion protein interaction
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Isomer(s)
40758SNDX-5613
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Product Type

Biochemicals

Research Area

Cancer
Transcription Factors

VTP-50469

Item No. 40759

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-fluoro-N,N-bis(1-methylethyl)-2-[[4-[7-[[trans-4-[(methylsulfonyl)amino]cyclohexyl]methyl]-2,7-diazaspiro[3.5]non-2-yl]-5-pyrimidinyl]oxy]-benzamide
CAS Number
2169916-18-9
Molecular Formula
C32H47FN6O4S
Formula Weight
630.8
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly soluble: 1-10 mg/ml
SMILES
CC(C)N(C(C)C)C(C(C=C(C=C1)F)=C1OC2=CN=CN=C2N(C3)CC43CCN(C[C@@H]5CC[C@H](CC5)NS(=O)(C)=O)CC4)=O
InChi Code
InChI=1S/C32H47FN6O4S/c1-22(2)39(23(3)4)31(40)27-16-25(33)8-11-28(27)43-29-17-34-21-35-30(29)38-19-32(20-38)12-14-37(15-13-32)18-24-6-9-26(10-7-24)36-44(5,41)42/h8,11,16-17,21-24,26,36H,6-7,9-10,12-15,18-20H2,1-5H3/t24-,26-
InChi Key
ADHHOUXZPBYYSU-YOCNBXQISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $230

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    10 mg

    $414

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    25 mg

    $863

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    50 mg

    $1,036

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    Cayman Chemical
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    Product Description

    VTP-50469 is an inhibitor of the protein-protein interaction between menin and mixed lineage leukemia 1 (MLL1) fusion proteins (Ki = 0.104 nM).1 It selectively inhibits the growth of ten leukemia cell lines expressing MLL1 fusion proteins (IC50s = 13-37 nM) over HL-60 , K562, and Reh leukemia cells expressing wild-type MLL1 (IC50s = >1,000 nM).2 VTP-50469 reduces MLL-AF9-induced increases in the expression of MLL fusion protein target genes, including MEIS1, MEF2C, JMJD1C, and PBX3, in MOLM-13 acute myeloid leukemia (AML) cells. In vivo, VTP-50469 (120 mg/kg twice per day) dramatically increases the survival of mice in a patient-derived xenograft (PDX) mouse model of B cell acute lymphoblastic leukemia (B-ALL).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Krivtsov, A.V., Eschle, B.K., Witkin, M., et al. VTP50469 is a novel, orally available menin-MLL1 inhibitor effective against MLL-rearranged and NPM1-mutant leukemia. Cancer Res. 78(Suppl. 13), 4958 (2018).

    2. Krivtsov, A.V., Evans, K., Gadrey, J.Y., et al. A menin-MLL inhibitor induces specific chromatin changes and eradicates disease in models of MLL-rearranged leukemia. Cancer Cell 36(6), 663-673 (2019).