An inhibitor of the ATPase p97/VCP
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CB-5339

Item No. 46233

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-methyl-1-[5,6,7,8-tetrahydro-4-[(phenylmethyl)amino]pyrido[2,3-d]pyrimidin-2-yl]-1H-indole-4-carboxamide
CAS Number
1863952-15-1
Molecular Formula
C24H24N6O
Formula Weight
412.5
Purity
≥95%
Formulation (Request formulation change)
A solid
SMILES
CC1=CC2=C(C=CC=C2C(N)=O)N1C3=NC(NCC4=CC=CC=C4)=C5C(N3)=NCCC5
InChi Code
InChI=1S/C24H24N6O/c1-15-13-19-17(21(25)31)9-5-11-20(19)30(15)24-28-22-18(10-6-12-26-22)23(29-24)27-14-16-7-3-2-4-8-16/h2-5,7-9,11,13H,6,10,12,14H2,1H3,(H2,25,31)(H2,26,27,28,29)
InChi Key
XDHFSLWWYBVSLN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $75

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    10 mg

    $128

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    25 mg

    $225

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    50 mg

    $375

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    Cayman Chemical
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    Product Description

    CB-5339 is an inhibitor of the AAA-ATPase p97, also known as valosin-containing protein (VCP; IC50 = 9 nM), and a derivative of CB-5083 (Item No. 19311).1 It inhibits phosphodiesterase 6C (PDE6C) and accumulates in rat retina to a lesser extent than CB-5083. CB-5339 inhibits the growth of 16 primary acute myeloid leukemia (AML) cell lines (median IC50 = 375 nM) and induces polyubiquitin protein accumulation and endoplasmic reticulum (ER) stress in MV4-11 AML cells. It decreases tumor cell bone marrow infiltration and increases survival in an MLL-AF9-driven patient-derived xenograft (PDX) mouse model of AML at 90 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Roux, B., Vaganay, C., Vargas, J.D., et al. Targeting acute myeloid leukemia dependency on VCP-mediated DNA repair through a selective second-generation small-molecule inhibitor. Sci. Transl Med. 13(587), eabg1168 (2021).