A selective P-glycoprotein inhibitor
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PGP-4008

Item No. 20901

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2,3-dihydro-1-(phenylmethyl)-1H-pyrrolo[2,3-b]quinolin-4-yl]-benzeneacetamide
CAS Number
365565-02-2
Molecular Formula
C26H23N3O
Formula Weight
393.5
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 50mMEthanol: 5mM
λmax
210, 256, 347 nm
SMILES
O=C(CC1=CC=CC=C1)NC2=C(CCN3CC4=CC=CC=C4)C3=NC5=C2C=CC=C5
InChi Code
InChI=1S/C26H23N3O/c30-24(17-19-9-3-1-4-10-19)28-25-21-13-7-8-14-23(21)27-26-22(25)15-16-29(26)18-20-11-5-2-6-12-20/h1-14H,15-18H2,(H,27,28,30)
InChi Key
HVIAKQBMYMKWII-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    500 µg

    $54

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    1 mg

    $99

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    Cayman Chemical
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    Product Description

    PGP-4008 is a selective inhibitor of P-glycoprotein (P-gp) that does not affect the activity of multidrug resistance-related protein 1 (MRP1).1,2 It is effective in vitro and, when delivered intraperitoneally, in vivo, inhibiting tumor growth when given with doxorubicin (Item No. 15007).1,2 PGP-4008 also enhances the ability of docetaxel (Item No. 11637) to inhibit growth and drive apoptosis in ovarian cancer cells.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lee, B.D., French, K.J., Zhuang, Y., et al. Development of a syngeneic in vivo tumor model and its use in evaluating a novel P-glycoprotein modulator, PGP-4008. Onocl. Res. 14(1), 49-60 (2003).

    2. Lee, B.D., Li, Z., French, K.J., et al. Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J. Med. Chem. 47(6), 1413-1422 (2004).

    3. Miettinen, S., Grènman, S., and Ylikomi, T. Inhibition of P-glycoprotein-mediated docetaxel efflux sensitizes ovarian cancer cells to concomitant docetaxel and SN-38 exposure. Anticancer Drugs 20(4), 267-276 (2009).