2. Antibody-drug Conjugate/ADC Related Metabolic Enzyme/Protease Apoptosis
  3. ADC Payload Glutathione Peroxidase Ferroptosis
  4. RSL3-NH2 hydrochloride

RSL3-NH2 hydrochloride is a GPX4 inhibitor and ferroptosis inducer. RSL3-NH2 hydrochloride triggers the iron-dependent cell death pathway associated with lipid peroxidation by inhibiting GPX4 activity. RSL3-NH2 hydrochloride exhibits significant cytotoxicity against colorectal cancer cells and effectively induces their ferroptosis. RSL3-NH2 hydrochloride can serve as a ADC payload for synthesizing a ADC and be used in colorectal cancer-related research.

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RSL3-NH2 hydrochloride

RSL3-NH2 hydrochloride Chemical Structure

CAS No. : 3051815-40-5

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Other Forms of RSL3-NH2 hydrochloride:

RSL3-NH2 hydrochloride Related Antibodies

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Description

RSL3-NH2 hydrochloride is a GPX4 inhibitor and ferroptosis inducer. RSL3-NH2 hydrochloride triggers the iron-dependent cell death pathway associated with lipid peroxidation by inhibiting GPX4 activity. RSL3-NH2 hydrochloride exhibits significant cytotoxicity against colorectal cancer cells and effectively induces their ferroptosis. RSL3-NH2 hydrochloride can serve as a ADC payload for synthesizing a ADC and be used in colorectal cancer-related research[1].

IC50 & Target[1]

GPX4

 

In Vitro

The ADC formed by conjugating RSL3-NH2 hydrochloride with a bispecific antibody, namely CDH17 x GUCY2C-RSL3-NH2 hydrochloride 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 hydrochloride 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.

RSL3-NH2 hydrochloride Related Antibodies

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 hydrochloride 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 hydrochloride 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 hydrochloride 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

434.32

Formula

C21H21Cl2N3O3
CAS No.
SMILES

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

DMSO : 100 mg/mL (230.24 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 2.3024 mL 11.5122 mL 23.0245 mL
5 mM 0.4605 mL 2.3024 mL 4.6049 mL
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Purity & Documentation
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Complete Stock Solution Preparation Table

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3024 mL 11.5122 mL 23.0245 mL 57.5612 mL
5 mM 0.4605 mL 2.3024 mL 4.6049 mL 11.5122 mL
10 mM 0.2302 mL 1.1512 mL 2.3024 mL 5.7561 mL
15 mM 0.1535 mL 0.7675 mL 1.5350 mL 3.8374 mL
20 mM 0.1151 mL 0.5756 mL 1.1512 mL 2.8781 mL
25 mM 0.0921 mL 0.4605 mL 0.9210 mL 2.3024 mL
30 mM 0.0767 mL 0.3837 mL 0.7675 mL 1.9187 mL
40 mM 0.0576 mL 0.2878 mL 0.5756 mL 1.4390 mL
50 mM 0.0460 mL 0.2302 mL 0.4605 mL 1.1512 mL
60 mM 0.0384 mL 0.1919 mL 0.3837 mL 0.9594 mL
80 mM 0.0288 mL 0.1439 mL 0.2878 mL 0.7195 mL
100 mM 0.0230 mL 0.1151 mL 0.2302 mL 0.5756 mL
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RSL3-NH2 hydrochloride Related Classifications

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  • 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-NH23051815-40-5ADC PayloadGlutathione PeroxidaseFerroptosisADC Cytotoxinnude miceSW1463 cellsHT-29 cellsGUCY2Ccolorectal cancer cellsGPX4LS1034 cellscolorectal cancerCDH17ferroptosisInhibitorinhibitorinhibit

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