Endoxifen Z-isomer hydrochloride

Name: Endoxifen Z-isomer hydrochloride
Brand: MedChemExpress
SKU: HY-18719A
Rating: 5.0 (3 reviews)

Cat. No.: HY-18719A Purity: 99.67%: Data Sheet
COA

SDS
Handling Instructions
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Endoxifen Z-isomer hydrochloride, an orally active Tamoxifen (HY-13757A) metabolite, is a selective estrogen receptor modulator with 100-fold more potency than its parent agent, Tamoxifen. Endoxifen Z-isomer hydrochloride inhibits PKCβ1 kinase activity. Endoxifen Z-isomer hydrochloride attenuates PKCβ1-activated AKT^Ser473 phosphorylation, diminishes AKT substrate phosphorylation, and induces Apoptosis. Endoxifen Z-isomer hydrochloride exhibits anticancer activity against hormone-resistant metastatic breast cancer.

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

Endoxifen Z-isomer hydrochloride Chemical Structure

CAS No. : 1032008-74-4

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

Other Forms of Endoxifen Z-isomer hydrochloride:

Endoxifen hydrochloride In-stock
Endoxifen E-isomer hydrochloride In-stock
Endoxifen (E-isomer) In-stock
Endoxifen In-stock
Endoxifen (Z-isomer) In-stock
Endoxifen-d₅ (Z-isomer) Get quote

3 Publications Citing Use of MCE Endoxifen Z-isomer hydrochloride

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Estrogen Receptor/ERR Isoform Specific Products:

View All Isoforms

Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

View All PKC Isoform Specific Products:

View All Isoforms

PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

View All Akt Isoform Specific Products:

View All Isoforms

Akt Akt1 Akt2 Akt3

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]^[2]^[3]^[4]

PKC-βI

In Vitro

Endoxifen Z-isomer (2.5-10 µM; 48 h) hydrochloride inhibits growth and induces apoptosis in estrogen deprived ERα⁺ /HER2^- MCF7AC1 cells^[2].
Endoxifen Z-isomer (0.1-5 μM, 7 days) hydrochloride exhibits potent antiproliferative activity against MCF7AC1 and MCF7LR cell lines^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[2]

Cell Line:	MCF7AC1 cells
Concentration:	0.01, 0.1, 5 µM
Incubation Time:	2 h (pretreatment)
Result:	Blocked AKTSer473, AKTThr308 phosphorylation at 5 µM. Diminished Insulin-stimulated phosphorylation of AKT substrates at 5 µM.

In Vivo

Endoxifen Z-isomer (50 mg/kg, p.o., 5 times a week for 4 weeks) hydrochloride shows better antitumor efficacy in the MCF7LR resistant mouse model^[4].
Endoxifen Z-isomer (75 mg/kg, p.o., once daily for 4 weeks) hydrochloride shows strong antitumor activity in the MCF7AC1 mouse breast cancer model^[4].
Endoxifen Z-isomer (5 mg/kg/day, s.c., gradual agent release every 30 days, pellets replaced every 90 days) hydrochloride effectively prevents breast cancer in the C3(1)-TAg mouse model^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C3(1)-TAg mouse mammary tumorigenesis model, developed by breeding FVB/NJ females with FVB/C3(1)-TAg males (8 weeks), resulting in SV40 T-antigen expression in mammary gland cells and tamoxifen resistance^[3]
Dosage:	5 mg/kg/day
Administration:	Subcutaneously implanted pellets, replaced every 90 days, with each pellet designed to release the drug gradually over 30 days.
Result:	Significantly increased tumor latency and reduced tumor growth.

Animal Model:	MCF7LR mouse breast cancer model, simulating endocrine-resistant breast cancer, developed by prolonged exposure to Letrozole^[4]
Dosage:	Z-Endoxifen: 50 mg/kg (Tamoxifen (HY-13757A): 500 μg/day, Exemestane (HY-13632): 250 μg/day, Everolimus (HY-10218): 2.5 mg/day)
Administration:	Z-Endoxifen: oral gavage (p.o.), the others administered subcutaneously, 5 times a week for 4 weeks
Result:	Significantly reduced tumor volume in the MCF7LR resistant model compared to Tamoxifen and Exemestane.

Molecular Weight

409.95

Formula

C₂₅H₂₈ClNO₂

CAS No.

1032008-74-4

Appearance

Solid

Color

White to off-white

SMILES

OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (243.93 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	2.4393 mL	12.1966 mL	24.3932 mL
5 mM	0.4879 mL	2.4393 mL	4.8786 mL
10 mM	0.2439 mL	1.2197 mL	2.4393 mL

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, 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.

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 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.10 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 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 (25.0 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 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (6.10 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 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 (25.0 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 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 1.25 mg/mL (3.05 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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: 99.67%

Select Batch:

Data Sheet (282 KB) SDS (562 KB)

COA (251 KB) HNMR (553 KB) LCMS (99 KB)

Handling Instructions (2659 KB)

References

[1]. Goetz MP, et al. First-in-Human Phase I Study of the Tamoxifen Metabolite Z-Endoxifen in Women With Endocrine-Refractory Metastatic Breast Cancer. J Clin Oncol. 2017 Oct 20;35(30):3391-3400. [Content Brief]

[2]. Jayaraman S, et al. Endoxifen downregulates AKT phosphorylation through protein kinase C beta 1 inhibition in ERα+ breast cancer. NPJ Breast Cancer. 2023 Dec 19;9(1):101. [Content Brief]

[3]. Lee O, et al. Z-Endoxifen prevents aggressive mammary cancers in mice by inhibiting cell proliferation and creating a tumor suppressive microenvironment. Biomed Pharmacother. 2023 Jun;162:114607. [Content Brief]

[4]. Jayaraman S, et al. Antitumor activity of Z-endoxifen in aromatase inhibitor-sensitive and aromatase inhibitor-resistant estrogen receptor-positive breast cancer. Breast Cancer Res. 2020 May 19;22(1):51. [Content Brief]

Complete Stock Solution Preparation Table

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

DMSO	1 mM	2.4393 mL	12.1966 mL	24.3932 mL	60.9830 mL
	5 mM	0.4879 mL	2.4393 mL	4.8786 mL	12.1966 mL
	10 mM	0.2439 mL	1.2197 mL	2.4393 mL	6.0983 mL
	15 mM	0.1626 mL	0.8131 mL	1.6262 mL	4.0655 mL
	20 mM	0.1220 mL	0.6098 mL	1.2197 mL	3.0492 mL
	25 mM	0.0976 mL	0.4879 mL	0.9757 mL	2.4393 mL
	30 mM	0.0813 mL	0.4066 mL	0.8131 mL	2.0328 mL
	40 mM	0.0610 mL	0.3049 mL	0.6098 mL	1.5246 mL
	50 mM	0.0488 mL	0.2439 mL	0.4879 mL	1.2197 mL
	60 mM	0.0407 mL	0.2033 mL	0.4066 mL	1.0164 mL
	80 mM	0.0305 mL	0.1525 mL	0.3049 mL	0.7623 mL
	100 mM	0.0244 mL	0.1220 mL	0.2439 mL	0.6098 mL