Synonym
PGP-4008; PGP 4008; PGP4008.
IUPAC/Chemical Name
N-[2,3-dihydro-1-(phenylmethyl)-1H-pyrrolo[2,3-b]quinolin-4-yl]-benzeneacetamide
InChi Key
HVIAKQBMYMKWII-UHFFFAOYSA-N
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)
SMILES Code
O=C(NC1=C2C(N(CC3=CC=CC=C3)CC2)=NC4=CC=CC=C14)CC5=CC=CC=C5
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
393.49
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Huang L, Wang J, Chen WC, Li HY, Liu JS, Tao Jiang, Yang WD. P-glycoprotein expression in Perna viridis after exposure to Prorocentrum lima, a dinoflagellate producing DSP toxins. Fish Shellfish Immunol. 2014 Aug;39(2):254-62. doi: 10.1016/j.fsi.2014.04.020. PubMed PMID: 24811006.
2: Yoshino Y, Yuan B, Kaise T, Takeichi M, Tanaka S, Hirano T, Kroetz DL, Toyoda H. Contribution of aquaporin 9 and multidrug resistance-associated protein 2 to differential sensitivity to arsenite between primary cultured chorion and amnion cells prepared from human fetal membranes. Toxicol Appl Pharmacol. 2011 Dec 1;257(2):198-208. doi: 10.1016/j.taap.2011.09.006. PubMed PMID: 21945491; PubMed Central PMCID: PMC3470788.
3: Miettinen S, Grènman S, Ylikomi T. Inhibition of P-glycoprotein-mediated docetaxel efflux sensitizes ovarian cancer cells to concomitant docetaxel and SN-38 exposure. Anticancer Drugs. 2009 Apr;20(4):267-76. doi: 10.1097/CAD.0b013e328329977f. PubMed PMID: 19262372.
4: Karla PK, Earla R, Boddu SH, Johnston TP, Pal D, Mitra A. Molecular expression and functional evidence of a drug efflux pump (BCRP) in human corneal epithelial cells. Curr Eye Res. 2009 Jan;34(1):1-9. doi: 10.1080/02713680802518251. PubMed PMID: 19172464; PubMed Central PMCID: PMC4406241.
5: Anglicheau D, Pallet N, Rabant M, Marquet P, Cassinat B, Méria P, Beaune P, Legendre C, Thervet E. Role of P-glycoprotein in cyclosporine cytotoxicity in the cyclosporine-sirolimus interaction. Kidney Int. 2006 Sep;70(6):1019-25. PubMed PMID: 16837925.
6: Maines LW, Antonetti DA, Wolpert EB, Smith CD. Evaluation of the role of P-glycoprotein in the uptake of paroxetine, clozapine, phenytoin and carbamazapine by bovine retinal endothelial cells. Neuropharmacology. 2005 Oct;49(5):610-7. PubMed PMID: 15961125.
7: Lee BD, Li Z, French KJ, Zhuang Y, Xia Z, Smith CD. Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11;47(6):1413-22. PubMed PMID: 14998330.
8: Lee BD, French KJ, Zhuang Y, Smith CD. Development of a syngeneic in vivo tumor model and its use in evaluating a novel P-glycoprotein modulator, PGP-4008. Oncol Res. 2003;14(1):49-60. PubMed PMID: 14552591.
