An erastin analog with antitumor activity
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PRLX-93936

Item No. 25631

Technical Information
Formal Name
3-(2-ethoxyphenyl)-2-(1-piperazinylmethyl)-4(3H)-quinazolinone
CAS Number
903499-49-0
Molecular Formula
C21H24N4O2
Formula Weight
Purity
≥98%
A solid
SMILES
CCOC1=CC=CC=C1N2C(CN3CCNCC3)=NC(C=CC=C4)=C4C2=O
InChi Code
InChI=1S/C21H24N4O2/c1-2-27-19-10-6-5-9-18(19)25-20(15-24-13-11-22-12-14-24)23-17-8-4-3-7-16(17)21(25)26/h3-10,22H,2,11-15H2,1H3
InChi Key
OBWOSMGNXYUDFB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PRLX-93936 is an analog of erastin (Item No. 17754) that has antitumor activity.1 It inhibits the hypoxia-inducible factor 1 (HIF-1) signaling pathway under hypoxic conditions (IC50 = 0.09 μM in a cell-based reporter assay).2 PRLX-93936 (1 μM) also inhibits hypoxia-induced increases in HIF-1α expression in ME-180 cervical cancer cells. It inhibits the growth of HT-1080 fibrosarcoma, OVCAR-5 ovarian cancer, BJELR tumorigenic primary fibroblast, and PANC-1 pancreatic cancer cells with IC50 values of less than 100 nM.1 PRLX-93936 inhibits tumor growth in PANC-1 and HT-1080 xenograft models when administered at a dose of 50 mg/kg and induces tumor regression when administered at a dose of 100 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stockwell, B.R. Erastin analogs and uses thereof. (2007).

    2. Huang, W., Huang, R., Attene Ramos, M., et alSynthesis and evaluation of quinazolin-4-ones as hypoxia-inducible factor-1α inhibitors. Bioorg. Med. Chem. Lett. 21(18), 5239-5243 (2011).