RSL3-NH2

Name: RSL3-NH2
Brand: MedChemExpress
SKU: HY-175615

Cat. No.: HY-175615: Data Sheet Handling Instructions
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RSL3-NH2 is a GPX4 inhibitor and ferroptosis inducer. RSL3-NH2 triggers the iron-dependent cell death pathway associated with lipid peroxidation by inhibiting GPX4 activity. RSL3-NH2 exhibits significant cytotoxicity against colorectal cancer cells and effectively induces their ferroptosis. RSL3-NH2 can serve as a ADC payload for synthesizing antibody-drug conjugates (ADC) and be used in colorectal cancer-related research.

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

RSL3-NH2 Chemical Structure

CAS No. : 3051815-39-2

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GPX1 GPX4

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

GPX4

In Vitro

The ADC formed by conjugating RSL3-NH2 with a bispecific antibody, namely CDH17 x GUCY2C-RSL3-NH2 ADC, potently inhibits the proliferation of SW1463 and LS1034 cells and induces significant MDA and lipid ROS accumulation, with IC₅₀ values of 4.97 μg/mL and 2.249 μg/mL at 72 h, respectively^[1].
CDH17 x GUCY2C-RSL3-NH2 ADC (5 μg/mL; 72 h) exhibits bystander cytotoxicity against CDH17/GUCY2C-negative HT-29 cells when co-cultured with CDH17/GUCY2C-positive SW1463 or LS1034 cells^[1].

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

Cell Cytotoxicity Assay^[1]

Cell Line:	SW1463/HT-29 co-cultures, LS1034/HT-29 co-cultures
Concentration:	5 μg/mL
Incubation Time:	72 h
Result:	Increased bystander killing of CDH17/GUCY2C-negative HT-29 cells in co-culture with positive cells, compared to the control group.

In Vivo

ADC Conjugated from RSL3-NH2 and Bispecific Antibody: CDH17 x GUCY2C-RSL3-NH2 ADC (1 mg/kg; intravenous injection; once every 5 days; 7 doses total) induces significant regression of SW1463 colorectal cancer tumors and robust ferroptosis (elevated levels of MDA and 4-HNE) in nude mice^[1].
CDH17 x GUCY2C-RSL3-NH2 ADC (1 mg/kg; intravenous injection; once every 5 days; 7 injections in total) induces significant regression of LS1034 colorectal tumors in nude mice and triggers strong ferroptosis (elevated levels of MDA and 4-HNE)^[1].
CDH17 x GUCY2C-RSL3-NH2 ADC (1 mg/kg; intravenous injection; once every 5 days; 7 injections total) exhibits favorable safety in double-humanized BALB/c mice, with no hepatotoxicity or organ damage detected^[1].

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

Animal Model:	hCDH17/hGUCY2 double-humanized BALB/c (7-week-old female)^[1]
Dosage:	1 mg/kg
Administration:	i.v.; once every 5 days; 7 injections total
Result:	Maintained serum levels of alanine aminotransferase (ALT) and aspartate aminotransferase (AST) within the normal range, not significantly different from PBS control. Showed no histopathological signs of toxicity in the heart, liver, spleen, lungs, or kidneys.

Molecular Weight

397.85

Formula

C₂₁H₂₀ClN₃O₃

CAS No.

3051815-39-2

SMILES

NC(C=C1)=CC=C1[C@H](N2C(CCl)=O)C(NC3=C4C=CC=C3)=C4C[C@@H]2C(OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility

In Vitro:

Ethanol : 100 mg/mL (251.35 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5135 mL	12.5676 mL	25.1351 mL
5 mM	0.5027 mL	2.5135 mL	5.0270 mL
10 mM	0.2514 mL	1.2568 mL	2.5135 mL

View the Complete Stock Solution Preparation Table

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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH 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% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.28 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL EtOH 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% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.28 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 EtOH stock solution (25.0 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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Zhang Y, et al. Development of a bispecific CDH17-GUCY2C ADC bearing the ferroptosis inducer RSL3 for the treatment of colorectal cancer. Cell Death Discov. 2025;11(1):347. Published 2025 Jul 28. [Content Brief]

Complete Stock Solution Preparation Table

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

Ethanol	1 mM	2.5135 mL	12.5676 mL	25.1351 mL	62.8378 mL
	5 mM	0.5027 mL	2.5135 mL	5.0270 mL	12.5676 mL
	10 mM	0.2514 mL	1.2568 mL	2.5135 mL	6.2838 mL
	15 mM	0.1676 mL	0.8378 mL	1.6757 mL	4.1892 mL
	20 mM	0.1257 mL	0.6284 mL	1.2568 mL	3.1419 mL
	25 mM	0.1005 mL	0.5027 mL	1.0054 mL	2.5135 mL
	30 mM	0.0838 mL	0.4189 mL	0.8378 mL	2.0946 mL
	40 mM	0.0628 mL	0.3142 mL	0.6284 mL	1.5709 mL
	50 mM	0.0503 mL	0.2514 mL	0.5027 mL	1.2568 mL
	60 mM	0.0419 mL	0.2095 mL	0.4189 mL	1.0473 mL
	80 mM	0.0314 mL	0.1571 mL	0.3142 mL	0.7855 mL
	100 mM	0.0251 mL	0.1257 mL	0.2514 mL	0.6284 mL

RSL3-NH2 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.

Keywords:

RSL3-NH23051815-39-2ADC PayloadGlutathione PeroxidaseFerroptosisADC Cytotoxinnude miceSW1463 cellsHT-29 cellsGUCY2Ccolorectal cancer cellsGPX4LS1034 cellscolorectal cancerCDH17ferroptosisInhibitorinhibitorinhibit

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