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[CAS NO. 1219810-16-8] RSL3

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Catalog:	HY-100218A
Brand:	MCE
CAS:	1219810-16-8

Overview

MDL	MFCD30187526
Molecular Weight	440.88
Molecular Formula	C23H21ClN2O5
SMILES	O=C([C@H]1CC2=C([C@H](C3=CC=C(C(OC)=O)C=C3)N1C(CCl)=O)NC4=C2C=CC=C4)OC

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

92 Publications Citing Use of MCE

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Summary

RSL3 ((1S,3R)-RSL3) is an inhibitor of glutathione peroxidase 4 (GPX4) ( ferroptosis activator), reduces the expression of GPX4 protein, and induces ferroptotic death of head and neck cancer cell. RSL3 increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells ^[1] .

IC50 & Target

Glutathione peroxidase 4 ^[1]

In Vitro

RSL3 (0-8 μM, 72 hours) potently reduces the viability of HN3 cells, with IC ₅₀ s of 0.48 µM in HN3 and 5.8 µM in HN3-rslR cells, respectively ^[1] .
RSL3 (0-8 μM, 24 hours) reduces the expression of GPX4 protein, increases the expression of p62 and Nrf2 and inactivates Keap1 in HN3-rslR cells ^[1] .

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

Cell Viability Assay ^[1]

Cell Line:	HN3 cells, HN3-rslR cells
Concentration:	0-8 μM
Incubation Time:	72 hours
Result:	Showed IC ₅₀ s of 0.48 µM in HN3 and 5.8 µM in HN3-rslR cells, respectively ^[1] .

Western Blot Analysis ^[1]

Cell Line:	HN3-rslR cells
Concentration:	0-8 μM
Incubation Time:	24 hours
Result:	Inhibited GPX4 expression, increased p62 and Nrf2 levels, and decreased Keap1 levels.

In Vivo

RSL3 (100 mg/kg, Intratumorally twice per week for 20 days) significantly inhibits the growth of tumor in combination with trigonelline in mice bearing HN3R cells.

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

Animal Model:	Ten-week-old athymic BALB/c male nude mice (nu/nu) bearing HN3R cells ^[1]
Dosage:	100 mg/kg in combination with trigonelline (50 mg/kg)
Administration:	Intratumorally twice per week for 20 days
Result:	Significantly reduced the volume of tumor combined with trigonelline in mice.

Appearance

Solid

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 ( 226.82 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.2682 mL	11.3410 mL	22.6819 mL
5 mM	0.4536 mL	2.2682 mL	4.5364 mL
10 mM	0.2268 mL	1.1341 mL	2.2682 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 50% PEG300 >> 50% saline

Solubility: 20 mg/mL (45.36 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: 5 mg/mL (11.34 mM); Suspended solution; Need ultrasonic
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.67 mM); Clear solution
4.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.08 mg/mL (4.72 mM); Clear solution
5.

Add each solvent one by one: 10% DMF >> 90% corn oil

Solubility: ≥ 0.56 mg/mL (1.27 mM); Clear solution

* All of the co-solvents are available by MCE.

References

[1] Shin D, et al. Nrf2 inhibition reverses resistance to GPX4 inhibitor-induced ferroptosis in head and neck cancer. Free Radic Biol Med. 2018 Dec;129:454-462.

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