Elacridar hydrochloride
Based on 31 publication(s) in Google Scholar
Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer.
For research use only. We do not sell to patients.
- Purity: 99.81%
- CAS No.: 143851-98-3
- Formula: C34H34ClN3O5
- Molecular Weight:600.10
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Elacridar hydrochloride
More- Cell Metab. 2024 Mar 5;36(3):498-510.e11. [Abstract]
- Sci Adv. 2023 Oct 20;9(42):eabp9530. [Abstract]
- Cell Death Dis. 2021 Jul 27;12(8):742. [Abstract]
- Cell Death Dis. 2019 May 24;10(6):400. [Abstract]
- Cancer Lett. 2024 Nov 25:217355. [Abstract]
- Arch Toxicol. 2025 Jun 7. [Abstract]
- Clin Cancer Res. 2018 Jan 15;24(2):383-394. [Abstract]
- Mol Psychiatry. 2023 Sep;28(9):3930-3942. [Abstract]
- Int J Biol Macromol. 2024 Feb 21;264(Pt 1):130377. [Abstract]
- Crit Rev Anal Chem. 2022;52(7):1557-1571. [Abstract]
- Cell Rep. 2020 Jun 23;31(12):107782. [Abstract]
- J Agric Food Chem. 2026 Feb 11;74(5):4823-4836. [Abstract]
- Eur J Med Chem. 2023 Nov 15:260:115721. [Abstract]
- J Agric Food Chem. 2022 Feb 16;70(6):1923-1933. [Abstract]
- J Agric Food Chem. 2019 Feb 27;67(8):2350-2360. [Abstract]
- J Mater Chem B. 2018 Dec 7;6(45):7521-7529. [Abstract]
- Int J Mol Sci. 2019 Mar 5;20(5). pii: E1125. [Abstract]
- Eur J Pharm Sci. 2025 Sep 1:212:107194. [Abstract]
- Molecules. 2019 Apr 27;24(9):1661. [Abstract]
- Sci Rep. 2021 Jul 22;11(1):14948. [Abstract]
- J Drug Target. 2016;24(5):441-9. [Abstract]
- Antiviral Res. 2021 Sep:193:105124. [Abstract]
- Chem Res Toxicol. 2025 Aug 12. [Abstract]
- J Biol Chem. 2022 Sep;298(9):102353. [Abstract]
- Food Chem Toxicol. 2021 Sep:155:112381. [Abstract]
- Biomed Res Int. 2020 Nov 29;2020:8878158. [Abstract]
- EJNMMI Res. 2015 Mar 17:5:11. [Abstract]
- Xenobiotica. 2024 Aug 10:1-15. [Abstract]
- Preprints. 2024 Jun 19.
- Hong Kong Polytechnic University. 2022 Oct.
- Biomed Pharmacother. 2020 Sep;129:110506. [Abstract]
Customer Validation & Images
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Cell Proliferation/Viability Assay
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IF
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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Cell Proliferation/Viability Assay
Biological Activity
Elacridar hydrochloride (0.001-1 μM; 2 h) inhibits cell viability of 786-O cells[2]. Elacridar hydrochloride (5 μM; 24 h) affects P-glycoprotein and ABCG2 protein expression levels in MCF-7 and 786-O cell lines[2]. Elacridar hydrochloride (5 μM; 24 h) affects 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:786-O cells
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Concentration:2.5 and 5 μM
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Incubation Time:2 hours
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Result:Dose-dependently inhibited cell viability of 786-O cells and showed better inhibitory effect with sunitnib adding.
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Cell Line:MCF-7, Caki-1, and 786-O cell lines
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Concentration:5 μM
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Incubation Time:24 hours
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Result:Dreased P-glycoprotein protein expression level in 786-O cells and increased ABCG2 protein expression level in Caki-1 cells.
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Cell Line:MCF-7 and 786-O cell lines
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Concentration:5 μM
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Incubation Time:24 hours
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Result:Dose-dependently increased 99mTc-MIBI intracellular accumulation in MCF-7 and 786-O cells.
| Mice PO 100 mg/kg |
Mice IP 100 mg/kg |
Mice IV 2.5 mg/kg |
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| CL/F (ml/min) | 2.05 | 33.2 | 0.46 |
| Vd/F (liter) | 3.5 | 12.3 | 0.17 |
| t1/2 (h) | 20 | 4.3 | 4.4 |
| AUC0-inf (μg·min/ml) | 1460 | 90.3 | 161.4 |
| F | 0.22 | 0.013 | 1 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:FVB wild-type mice[1]
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Dosage:100 mg/kg
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Administration:Intraperitoneal injection; 100 mg/kg once
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Result:Showd a higher concertration in brain than plasma except at 4 h after administration.
Chemical Information
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CAS No. 143851-98-3
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Appearance Solid
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Molecular Weight 600.10
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Formula C34H34ClN3O5
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Color Light yellow to yellow
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SMILES
O=C1C2=CC=CC(C(NC(C=C3)=CC=C3CCN4CC(C=C(C(OC)=C5)OC)=C5CC4)=O)=C2NC6=C1C=CC=C6OC.[H]Cl
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Synonyms
GF120918A
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (31)
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Journal Impact Factor
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Most Recent
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Cell Metab
ABCG2 is an itaconate exporter that limits antibacterial innate immunity by alleviating TFEB-dependent lysosomal biogenesis. [Abstract]2024 Mar 5;36(3):498-510.e11. PMID: 38181789 -
Sci Adv
BCRP drives intrinsic chemoresistance in chemotherapy-naïve breast cancer brain metastasis. [Abstract]2023 Oct 20;9(42):eabp9530. PMID: 37851804
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: Sci Adv. 2023 Oct 20;9(42):eabp9530. [Abstract]
Elacridar (200 nM) increased the sensitivity of BCBM organoids to doxorubicin by immunofluorescent staining.
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Cell Death Dis
2021 Jul 27;12(8):742. PMID: 34315857 -
Cell Death Dis
Targeting HDAC/OAZ1 axis with a novel inhibitor effectively reverses cisplatin resistance in non-small cell lung cancer. [Abstract]2019 May 24;10(6):400. PMID: 31127087 -
Cancer Lett
PAF1-mediated transcriptional reprogramming confers docetaxel resistance in advanced prostate cancer. [Abstract]2024 Nov 25:217355. PMID: 39603380
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2024 Nov 25:217355. [Abstract]
ABCB1 inhibition significantly reduced the number of 22Rv1-DR PCa cell-derived colonies compared to docetaxel treatment alone. Treatment with 2 μM Elacridar as a single agent did not impact colony growth in DR cells.
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Arch Toxicol
Daunorubicin and its hydroxy metabolite in cardiomyocytes: insights into cellular kinetics, toxicity, DNA damage, and dexrazoxane-induced cardioprotection. [Abstract]2025 Jun 7. PMID: 40481868 -
Clin Cancer Res
Inhibition of ID1-BMPR2 Intrinsic Signaling Sensitizes Glioma Stem Cells to Differentiation Therapy. [Abstract]2018 Jan 15;24(2):383-394. PMID: 29208670 -
Mol Psychiatry
cAMP-mediated upregulation of HCN channels in VTA dopamine neurons promotes cocaine reinforcement. [Abstract]2023 Sep;28(9):3930-3942. PMID: 37845497
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: Mol Psychiatry. 2023 Sep;28(9):3930-3942. [Abstract]
Systemic ivabradine administration (0,3,10 mg/kg; i.p.) following Elacridar hydrochloride (5 mg/kg; i.v.; single dose), dose-dependently decreased the mean number of active lever presses and cocaine infusions under an FR2 reinforcement schedule.
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Int J Biol Macromol
2024 Feb 21;264(Pt 1):130377. PMID: 38395279 -
Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566 -
Cell Rep
2020 Jun 23;31(12):107782. PMID: 32579914 -
J Agric Food Chem
Improvement of the Intestinal Absorption of Dihydroquercetin (DHQ) by Flavonoids via Inhibiting P-Glycoprotein (P-gp)-Mediated Efflux in P-gp Overexpressed KB/MDR1 Cells and Caco-2 Monolayers. [Abstract]2026 Feb 11;74(5):4823-4836. PMID: 41592218 -
Eur J Med Chem
Discovery of highly potent covalent SARS-CoV-2 3CLpro inhibitors bearing 2-sulfoxyl-1,3,4-oxadiazole scaffold for combating COVID-19. [Abstract]2023 Nov 15:260:115721. PMID: 37598484 -
J Agric Food Chem
Transport and Interactions of Co-incubated Bi-functional Flavonoids through Inhibiting the Function of P-Glycoprotein (P-gp) Using KB/Multidrug-Resistant (MDR) Cells and Rat Everted Gut Sacs. [Abstract]2022 Feb 16;70(6):1923-1933. PMID: 35112564 -
J Agric Food Chem
Establishment and Use of Human Mouth Epidermal Carcinoma (KB) Cells Overexpressing P-Glycoprotein To Characterize Structure Requirements for Flavonoids Transported by the Efflux Transporter. [Abstract]2019 Feb 27;67(8):2350-2360. PMID: 30688455 -
J Mater Chem B
Polymeric nanovesicles as simultaneous delivery platforms with doxorubicin conjugation and elacridar encapsulation for enhanced treatment of multidrug-resistant breast cancer. [Abstract]2018 Dec 7;6(45):7521-7529. PMID: 32254754
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: J Mater Chem B. 2018 Dec 7;6(45):7521-7529. [Abstract]
Elacridar hydrochloride (0.25 mg/kg; i.v.; every two days for a total of five doses). Ex vivo histological analyses of tumor sections excised from mice bearing MCF-7/ADR tumors after treatment. Nuclei were stained blue, and the extracellular matrix and cytoplasm were stained red through respectively. H&E staining images of the heart of MCF-7/ADR tumor-bearing mice after treatment. Scale bars represent 50 μM.
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: J Mater Chem B. 2018 Dec 7;6(45):7521-7529. [Abstract]
Bioactivity inhibition of the P-gp protein in MCF-7/ADR cells using the immunofluorescence assay after incubation with different samples. Green fluorescence: P-gp proteins labelled with FITC-antibody; blue fluorescence: nuclei stained with DAPI. The scale bars represent 20 mm. DOX concentration if applied: 10 mg/mL; Elacridar hydrochloride concentration if applied: 0.5 mg/mL.
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: J Mater Chem B. 2018 Dec 7;6(45):7521-7529. [Abstract]
Elacridar hydrochloride (0.25 mg/kg; i.v.; every two days for a total of five doses) co-delivered with DOX, exhibited a synergistic anticancer effect on multidrug-resistant MCF-7/ADR tumors in xenograft mouse models.
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Int J Mol Sci
Cisplatin Synergistically Enhances Antitumor Potency of Conditionally Replicating Adenovirus via p53 Dependent or Independent Pathways in Human Lung Carcinoma. [Abstract]2019 Mar 5;20(5). pii: E1125. PMID: 30841620
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2019 Mar 5;20(5). pii: E1125. [Abstract]
Sensitization of resistant cells to chemotherapy by Elacridar (5 μM) treatment.
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Eur J Pharm Sci
2025 Sep 1:212:107194. PMID: 40639493 -
Molecules
Quantitative Structure⁻Activity Relationships for the Flavonoid-Mediated Inhibition of P-Glycoprotein in KB/MDR1 Cells. [Abstract]2019 Apr 27;24(9):1661. PMID: 31035631 -
Sci Rep
Cannabis constituents interact at the drug efflux pump BCRP to markedly increase plasma cannabidiolic acid concentrations. [Abstract]2021 Jul 22;11(1):14948. PMID: 34294753 -
J Drug Target
2016;24(5):441-9. PMID: 26373825
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: J Drug Target. 2016;24(5):441-9. [Abstract]
Cells are co-treated with 5 μM of free LY139481 or an equivalent dose of SMA-LY139481 and either vehicle control (0.01% DMSO), Elacridar (1 μM), KO143 (5 μM), Valspodar (1 μM) or a combination of efflux inhibitors for 6 h.
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Antiviral Res
2021 Sep:193:105124. PMID: 34197862
Elacridar hydrochloride purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2021 Sep:193:105124. [Abstract]
Elacridar (0-33.34 μM, 72 h) do not induce cell toxicity by MTT assay.
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Chem Res Toxicol
Inhibitory Effects of Alkaloids on BCRP Implicated in Reversing Multidrug Resistance: A Case Example of Enhancing Temozolomide Cytotoxicity. [Abstract]2025 Aug 12. PMID: 40793827 -
J Biol Chem
p38 MAPK-dependent phosphorylation of transcription factor SOX2 promotes an adaptive response to BRAF inhibitors in melanoma cells. [Abstract]2022 Sep;298(9):102353. PMID: 35944584 -
Food Chem Toxicol
Structure-activity relationship and mechanism of flavonoids on the inhibitory activity of P-glycoprotein (P-gp)-mediated transport of rhodamine123 and daunorubicin in P-gp overexpressed human mouth epidermal carcinoma (KB/MDR) cells. [Abstract]2021 Sep:155:112381. PMID: 34217736 -
Biomed Res Int
A Novel Cryptococcal Meningitis Therapy: The Combination of Amphotericin B and Posaconazole Promotes the Distribution of Amphotericin B in the Brain Tissue. [Abstract]2020 Nov 29;2020:8878158. PMID: 33313322 -
EJNMMI Res
The effect of radiation exposure on multidrug resistance: in vitro and in vivo studies using non-small lung cancer cells. [Abstract]2015 Mar 17:5:11. PMID: 25853017 -
Xenobiotica
The metabolic activation of and platelet response to vicagrel vary with P-glycoprotein deficiency, rather than P-glycoprotein inhibition, in mice. [Abstract]2024 Aug 10:1-15. PMID: 39126503 -
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Biomed Pharmacother
Interplay of drug transporters P-glycoprotein (MDR1), MRP1, OATP1A2 and OATP1B3 in passage of maraviroc across human placenta. [Abstract]2020 Sep;129:110506. PMID: 32768979
Solvent & Solubility
DMSO : 5.83 mg/mL (9.72 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (3.47 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6664 mL | 8.3319 mL | 16.6639 mL | 41.6597 mL |
| 5 mM | 0.3333 mL | 1.6664 mL | 3.3328 mL | 8.3319 mL |
Elacridar hydrochloride Related Classifications
HY-50880 Related Classifications
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