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.
For research use only. We do not sell to patients.
- CAS No.: 3051815-40-5
- Formula: C21H21Cl2N3O3
- Molecular Weight:434.32
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Storage:
-20°C, protect from light, stored under argon
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under argon)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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GPX4 |
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.
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Cell Line:SW1463/HT-29 co-cultures, LS1034/HT-29 co-cultures
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Concentration:5 μg/mL
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Incubation Time:72 h
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Result:Increased bystander killing of CDH17/GUCY2C-negative HT-29 cells in co-culture with positive cells, compared to the control group.
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.
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Animal Model:hCDH17/hGUCY2 double-humanized BALB/c (7-week-old female)[1]
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Dosage:1 mg/kg
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Administration:i.v.; once every 5 days; 7 injections total
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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.
Chemical Information
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CAS No. 3051815-40-5
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Appearance Solid
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Molecular Weight 434.32
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Formula C21H21Cl2N3O3
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SMILES
NC(C=C1)=CC=C1[C@H](N2C(CCl)=O)C(NC3=C4C=CC=C3)=C4C[C@@H]2C(OC)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, protect from light, stored under argon
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under argon)
Solvent & Solubility
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)
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 (protect from light, stored under argon). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light, stored under argon). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
References
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 (protect from light, stored under argon). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| 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 |
RSL3-NH2 hydrochloride Related Classifications
HY-175615A Related Classifications
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