Molecular structure of Elacridar, CAS Number: 143664-11-3
Elacridar (CAS 143664-11-3)
See product citations (19)
Alternate Names:
GG 918; GF 120918
Application:
Elacridar is a prototypical BCRP (ABCG2) inhibitor
CAS Number:
143664-11-3
Purity:
≥98%
Molecular Weight:
563.64
Molecular Formula:
C34H33N3O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
Elacridar is a potent inhibitor of P-glycoprotein. Elacridar function by binding to the ATP-binding site of P-glycoprotein, preventing the hydrolysis of ATP and the subsequent efflux of chemotherapeutic agents from cancer cells.Elacridar′s mechanism of action involves blocking the transport of chemotherapeutic agents out of cancer cells, leading to increased drug retention.
Elacridar (CAS 143664-11-3) References
- Plasma and cerebrospinal fluid pharmacokinetics of imatinib after administration to nonhuman primates. | Neville, K., et al. 2004. Clin Cancer Res. 10: 2525-9. PMID: 15073132
- Phase II study of imatinib mesylate plus hydroxyurea in adults with recurrent glioblastoma multiforme. | Reardon, DA., et al. 2005. J Clin Oncol. 23: 9359-68. PMID: 16361636
- Abcg2/Bcrp1 mediates the polarized transport of antiretroviral nucleosides abacavir and zidovudine. | Pan, G., et al. 2007. Drug Metab Dispos. 35: 1165-73. PMID: 17437964
- P-glycoprotein and breast cancer resistance protein restrict brigatinib brain accumulation and toxicity, and, alongside CYP3A, limit its oral availability. | Li, W., et al. 2018. Pharmacol Res. 137: 47-55. PMID: 30253203
- β-Casein micelles for oral delivery of SN-38 and elacridar to overcome BCRP-mediated multidrug resistance in gastric cancer. | Bar-Zeev, M., et al. 2018. Eur J Pharm Biopharm. 133: 240-249. PMID: 30367935
- Physical blood-brain barrier disruption induced by focused ultrasound does not overcome the transporter-mediated efflux of erlotinib. | Goutal, S., et al. 2018. J Control Release. 292: 210-220. PMID: 30415015
- Codelivery of doxorubicin and elacridar to target both liver cancer cells and stem cells by polylactide-co-glycolide/d-alpha-tocopherol polyethylene glycol 1000 succinate nanoparticles. | Chen, D., et al. 2018. Int J Nanomedicine. 13: 6855-6870. PMID: 30498347
- Oral coadministration of elacridar and ritonavir enhances brain accumulation and oral availability of the novel ALK/ROS1 inhibitor lorlatinib. | Li, W., et al. 2019. Eur J Pharm Biopharm. 136: 120-130. PMID: 30660696
- The influence of the coadministration of the p-glycoprotein modulator elacridar on the pharmacokinetics of lapatinib and its distribution in the brain and cerebrospinal fluid. | Karbownik, A., et al. 2020. Invest New Drugs. 38: 574-583. PMID: 31177402
- Evaluation of the Role of P-glycoprotein (P-gp)-Mediated Efflux in the Intestinal Absorption of Common Substrates with Elacridar, a P-gp Inhibitor, in Rats. | Suzuki, K., et al. 2020. Eur J Drug Metab Pharmacokinet. 45: 385-392. PMID: 32078103
- Blood-Brain Barrier Disruption Increases Amyloid-Related Pathology in TgSwDI Mice. | Abdallah, IM., et al. 2021. Int J Mol Sci. 22: PMID: 33513818
- The effect of ivermectin alone and in combination with cobicistat or elacridar in experimental Schistosoma mansoni infection in mice. | Vicente, B., et al. 2021. Sci Rep. 11: 4476. PMID: 33627744
- Optimization of dose and route of administration of the P-glycoprotein inhibitor, valspodar (PSC-833) and the P-glycoprotein and breast cancer resistance protein dual-inhibitor, elacridar (GF120918) as dual infusion in rats. | Rowbottom, C., et al. 2021. Pharmacol Res Perspect. 9: e00740. PMID: 33660938
- Rifampin and ritonavir increase oral availability and elacridar enhances overall exposure and brain accumulation of the NTRK inhibitor larotrectinib. | Wang, Y., et al. 2022. Eur J Pharm Biopharm. 170: 197-207. PMID: 34952136
- Investigations with Drugs and Pesticides Revealed New Species- and Substrate-Dependent Inhibition by Elacridar and Imazalil in Human and Mouse Organic Cation Transporter OCT2. | Kuehne, A., et al. 2022. Int J Mol Sci. 23: PMID: 36555439
Inhibitor of:
ABC-1, ABC-me, ABCA14, ABCA15, ABCA16, ABCA17, Abca8a, ABCB6, ABCC11, ABCD2, ABCF3, ABCG2, Abcg3, ABCG4, ATP-binding cassette (ABC) transporter, GlnP, Mdr-1, PGP, SLC25A3, SLC25A45, Solute carrier family 25 (SLC25A), TAP2, and TMEM41B.Activator of:
ABCD4, and TAP1.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
Elacridar, 5 mg | sc-207613A | 5 mg | $96.00 | |||
Elacridar, 10 mg | sc-207613 | 10 mg | $111.00 | |||
Elacridar, 50 mg | sc-207613B | 50 mg | $403.00 | |||
Elacridar, 100 mg | sc-207613C | 100 mg | $515.00 | |||
Elacridar, 1 g | sc-207613D | 1 g | $2555.00 |