Elacridar (Synonyms: GF120918; GW0918; GG918; GW120918)

Name: Elacridar
Brand: MedChemExpress
SKU: HY-50879
Rating: 5.0 (27 reviews)

Cat. No.: HY-50879 Purity: 99.94%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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 agent distribution to brain and the research of cancer.

For research use only. We do not sell to patients.

Elacridar Chemical Structure

CAS No. : 143664-11-3

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 46	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 72	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 252	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 372	In-stock	Estimated Time of Arrival: December 31
200 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 1200	In-stock	Estimated Time of Arrival: December 31
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Based on 27 publication(s) in Google Scholar

Other Forms of Elacridar:

Elacridar hydrochloride In-stock

26 Publications Citing Use of MCE Elacridar

Proliferation Assay

: Elacridar 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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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

P-glycoprotein (Pgp), BCRP^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.41 μM Compound: GF-120918	Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry Inhibition of ABCG2 expressed in HEK293 cells assessed as mitoxantrone-mediated efflux by flow cytometry	[PMID: 17317193]
MCF7	IC₅₀	0.4 μM Compound: GF-120918	Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining Inhibition of BCRP expressed in MCF7 MX cells by Hoechst 33342 staining	[PMID: 19932960]
MDCK	IC₅₀	0.43 μM Compound: GF-120918	Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay Inhibition of BCRP expressed in MDCK cells by pheophorbide A assay	[PMID: 19932960]
MDCK-II	IC₅₀	0.4 μM Compound: 1	Inhibition of human Pgp overexpressed in human MDCK2-MDR1 cells assessed as inhibition of R123 efflux after 60 mins Inhibition of human Pgp overexpressed in human MDCK2-MDR1 cells assessed as inhibition of R123 efflux after 60 mins	[PMID: 21419632]

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 ^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.

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 ^99mTc-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].
1.19 Plasma Pharmacokinetic Parameters of Elacridar in mice^[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

MedChemExpress (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.

Molecular Weight

563.64

Formula

C₃₄H₃₃N₃O₅

CAS No.

143664-11-3

Appearance

Solid

Color

Light yellow to brown

SMILES

O=C1C2=CC=CC(C(NC(C=C3)=CC=C3CCN4CC(C=C(C(OC)=C5)OC)=C5CC4)=O)=C2NC6=C1C=CC=C6OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 5 mg/mL (8.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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	---	---	---

View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 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

This protocol yields a suspended solution of 1.67 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 (16.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.5 mg/mL (0.89 mM); Clear solution

This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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.
Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 0.25 mg/mL (0.44 mM); Clear solution
Protocol 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
Protocol 5

Add each solvent one by one: 1% DMSO 99% Saline
Solubility: 0.05 mg/mL (0.09 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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

Purity: 99.94%

Select Batch:

Data Sheet (281 KB) SDS (393 KB)

COA (251 KB) LCMS (93 KB)

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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7742 mL	8.8709 mL	17.7418 mL	44.3546 mL
DMSO	5 mM	0.3548 mL	1.7742 mL	3.5484 mL	8.8709 mL

Elacridar Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Elacridar (Synonyms: GF120918; GW0918; GG918; GW120918)

Customer Review

Other Forms of Elacridar:

Elacridar Related Antibodies

26 Publications Citing Use of MCE Elacridar

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References

Customer Review

Elacridar Related Antibodies

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Complete Stock Solution Preparation Table

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