A non-peptidomimetic inhibitor of IAP protein-peptide interactions
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Product Categories

Product Type

Biochemicals

Research Area

Cancer
Cell Death
Apoptosis

ASTX660

Item No. 36619

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[6-[(4-fluorophenyl)methyl]-2,3-dihydro-5-(hydroxymethyl)-3,3-dimethyl-1H-pyrrolo[3,2-b]pyridin-1-yl]-2-[(2R,5R)-5-methyl-2-[[(3R)-3-methyl-4-morpholinyl]methyl]-1-piperazinyl]-ethanone
CAS Number
1799328-86-1
Synonyms
  • Tolinapant
Molecular Formula
C30H42FN5O3
Formula Weight
539.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
258, 301 nm
SMILES
C[C@H](COCC1)N1C[C@@H](CN[C@@H](C2)C)N2CC(N3C4=CC(CC5=CC=C(C=C5)F)=C(CO)N=C4C(C)(C3)C)=O
InChi Code
InChI=1S/C30H42FN5O3/c1-20-14-35(25(13-32-20)15-34-9-10-39-18-21(34)2)16-28(38)36-19-30(3,4)29-27(36)12-23(26(17-37)33-29)11-22-5-7-24(31)8-6-22/h5-8,12,20-21,25,32,37H,9-11,13-19H2,1-4H3/t20-,21-,25-/m1/s1
InChi Key
YCXOHEXZVKOGEV-DNRQZRRGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $218

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    10 mg

    $363

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    25 mg

    $603

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    Product Description

    ASTX660 is an inhibitor of inhibitor of apoptosis (IAP) protein-peptide interactions.1 It inhibits the protein-peptide interaction between the IAP1 and XIAP BIR3 domains with a Smac-derived peptide in cell-free assays (IC50s = <40 and 12 nM, respectively). ASTX660 inhibits the protein-protein interaction between XIAP and caspase-9 in HEK293 cells (EC50 = 2.8 nM) and induces displacement of Smac from XIAP in A375 melanoma cells. It induces apoptosis in MDA-MB-231, A375, and SK-MEL-28 cells in a TNF-α-dependent manner. In vivo, ASTX660 (20 mg/kg) reduces tumor growth in MDA-MB-231 breast cancer and A375 melanoma mouse xenograft models.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ward, G.A., Lewis, E.J., Ahn, J.S., et al. ASTX660, a novel non-peptidomimetic antagonist of cIAP1/2 and XIAP, potently induces TNFα-dependent apoptosis in cancer cell lines and inhibits tumor growth. Mol. Cancer Ther. 17(7), 1381-1391 (2018).