[CAS NO. 143664-11-3] Elacridar
PRODUCTS SPECIFICATIONS [143664-11-3]
DESCRIPTION [143664-11-3]
Overview
| MDL | MFCD00912604 |
|---|---|
| Molecular Weight | 563.64 |
| Molecular Formula | C34H33N3O5 |
| SMILES | O=C1C2=CC=CC(C(NC(C=C3)=CC=C3CCN4CC(C=C(C(OC)=C5)OC)=C5CC4)=O)=C2NC6=C1C=CC=C6OC |
19 Publications Citing Use of MCE
- [1]Clin Cancer Res. 2018 Jan 15;24(2):383-394.
- [2]Cell Rep. 2020 Jun 23;31(12):107782.
- [3]Cell Death Dis. 2021 Jul 27;12(8):742.
- [4]Cell Death Dis. 2019 May 24;10(6):400.
- [5]J Mater Chem B. 2018 Dec 7;6(45):7521-7529.
- [6]Food Chem Toxicol. 2021, 112381.
- [7]Crit Rev Anal Chem. 2021 Mar 10;1-15.
- [8]Int J Mol Sci. 2019 Mar 5;20(5). pii: E1125.
- [9]Biomed Pharmacother. 2020 Sep;129:110506.
- [10]J Biol Chem. 2022 Aug 6;102353.
- [11]J Agric Food Chem. 2022 Feb 3.
- [12]J Agric Food Chem. 2019 Feb 27;67(8):2350-2360.
- [13]Antiviral Res. 2021 Jun 28;105124.
- [14]Sci Rep. 2021 Jul 22;11(1):14948.
- [15]J Drug Target. 2016;24(5):441-9.
- [16]Molecules. 2019 Apr 27;24(9):1661.
- [17]EJNMMI Res. 2015 Mar 17;5:11.
- [18]Biomed Res Int. 2020 Nov 29;2020:8878158.
- [19]Hong Kong Polytechnic University. Department of Applied Biology and Chemical Technology. 2022 Oct.
Summary
Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on drug distribution to brain and the research of cancer [1] [2] .
IC50 & Target
P-glycoprotein (Pgp), BCRP [1]
In Vitro
Elacridar (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells
[2]
.
Elacridar (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines
[2]
.
Elacridar (5 μM; 24 h) affects
99m
Tc-MIBI intracellular accumulation in MCF-7 and 786-O cells
[2]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Viability Assay [2]
| Cell Line: | 786-O cells |
| Concentration: | 2.5 and 5 μM |
| Incubation Time: | 2 hours |
| Result: | Dose-dependently inhibited cell viability of 786-O cells and showed better inhibitory effect with sunitnib adding |
Western Blot Analysis [2]
| Cell Line: | MCF-7, Caki-1, and 786-O cell lines |
| Concentration: | 5 μM |
| Incubation Time: | 24 hours |
| Result: | Dreased P-glycoprotein protein expression level in 786-O cells and increased ABCG2 protein expression level in Caki-1 cells. |
Cell Viability Assay [2]
| Cell Line: | MCF-7 and 786-O cell lines |
| Concentration: | 5 μM |
| Incubation Time: | 24 hours |
| Result: | Dose-dependently increased 99m Tc-MIBI intracellular accumulation in MCF-7 and 786-O cells. |
In Vivo
Elacridar (100 mg/kg; i.p. once) shows different distribution in brain and plasma
[1]
.
|
Mice
PO 100 mg/kg |
Mice
IP 100 mg/kg |
Mice
IV 2.5 mg/kg |
|
| CL/F (ml/min) | 2.05 | 33.2 | 0.46 |
| Vd/F (liter) | 3.5 | 12.3 | 0.17 |
| t 1/2 (h) | 20 | 4.3 | 4.4 |
| AUC 0-inf (μg•min/ml) | 1460 | 90.3 | 161.4 |
| F | 0.22 | 0.013 | 1 |
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | FVB wild-type mice [1] . |
| Dosage: | 100 mg/kg |
| Administration: | Intraperitoneal injection; 100 mg/kg once |
| Result: | Showd a higher concertration in brain than plasma except at 4 h after the dose. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 5 mg/mL ( 8.87 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7742 mL | 8.8709 mL | 17.7418 mL |
| 5 mM | 0.3548 mL | 1.7742 mL | 3.5484 mL |
| 10 mM | --- | --- | --- |
-
1.
Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: 1.67 mg/mL (2.96 mM); Suspended solution; Need ultrasonic
-
2.
-
3.
-
4.
Add each solvent one by one: 5% DMSO >> 95% (20% SBE-β-CD in saline)
Solubility: 0.25 mg/mL (0.44 mM); Suspended solution; Need ultrasonic
-
5.
Add each solvent one by one: 1% DMSO >> 99% saline
Solubility: 0.05 mg/mL (0.09 mM); Suspended solution; Need ultrasonic
References
- [1] Sane R, et al. Brain distribution and bioavailability of elacridar after different routes of administration in the mouse. Drug Metab Dispos. 2012 Aug;40(8):1612-9.
- [2] Sato H, et al. Elacridar enhances the cytotoxic effects of sunitinib and prevents multidrug resistance in renal carcinoma cells. Eur J Pharmacol. 2015 Jan 5;746:258-66.
Synonyms
