ML-210 (Synonyms: DPI10) |
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Catalog No.GC18705
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ML-210 is a prodrug that selectively inhibits GPX4 covalently with an EC50 of 30nM.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1360705-96-9
Sample solution is provided at 25 µL, 10mM.
ML-210 is a prodrug that selectively inhibits GPX4 covalently with an EC50 of 30nM[1]. ML-210 has been widely used as a target or model compound to develop a range of GPX4 degraders[2].
In vitro, ML-210 treatment at 10μM for 2 hours induced rapid accumulation of lipid radicals in clear-cell renal cell carcinoma cells and caused ferroptosis[3]. Treatment of PANC-1 cells with 3μM ML-210 for 48 hours significantly inhibited cell viability, strongly decreased N-cadherin expression, increased lipid peroxides on the cell membrane, and inhibited cell migration[4]. ML-210 treatment (10μM) for 24h significantly induced cell cycle arrest in ABCB1 overexpressing colorectal cancer cells without altering ABCB1 protein expression[5]. In OCI-AML3 cells, treatment with 0.5µM of ML-210 for 48h simultaneously increased the proportion of annexin V-positive and DAPI-positive cells, resulting in an increased number of apoptotic cells[6].
In vivo, ML-210 treatment (5mg/kg; administered intraperitoneally every other day for 20 days) inhibited ovarian cancer progression and modestly reduced body weight in mice[7].
References:
[1] Eaton J K, Furst L, Ruberto R A, et al. Selective covalent targeting of GPX4 using masked nitrile-oxide electrophiles[J]. Nature chemical biology, 2020, 16(5): 497-506.
[2] Wang H, Wang C, Li B, et al. Discovery of ML210-Based glutathione peroxidase 4 (GPX4) degrader inducing ferroptosis of human cancer cells[J]. European Journal of Medicinal Chemistry, 2023, 254: 115343.
[3] Zou Y, Palte M J, Deik A A, et al. A GPX4-dependent cancer cell state underlies the clear-cell morphology and confers sensitivity to ferroptosis[J]. Nature communications, 2019, 10(1): 1617.
[4] Takemura K, Ikeda K, Miyake H, et al. Epithelial–Mesenchymal Transition Suppression by ML210 Enhances Gemcitabine Anti-Tumor Effects on PDAC Cells[J]. Biomolecules, 2025, 15(1): 70.
[5] Li Y C, Xiong Y M, Long Z P, et al. ML210 Antagonizes ABCB1-Not ABCG2-Mediated Multidrug Resistance in Colorectal Cancer[J]. Biomedicines, 2025, 13(5): 1245.
[6] Akiyama H, Zhao R, Ostermann L B, et al. Mitochondrial regulation of GPX4 inhibition–mediated ferroptosis in acute myeloid leukemia[J]. Leukemia, 2024, 38(4): 729-740.
[7] Li N, Jiang X, Zhang Q, et al. Synergistic suppression of ovarian cancer by combining NRF2 and GPX4 inhibitors: in vitro and in vivo evidence[J]. Journal of Ovarian Research, 2024, 17(1): 49.
| Cell experiment [1]: | |
Cell lines | PANC-1 cells |
Preparation Method | 2×105 PANC-1 cells were seeded in a 6-well dish plates and incubated for 24h. The cells were treated with 0, 0.025, 0.05, 0.1, 0.3μM ML-210 for 24h. The cells were then trypsinized and suspended in FBS (−) medium and seeded into the culture inserts with a filter membrane (8.0µm). The culture inserts were then put on the bottom of the chambers with 750μL of FBS (+) medium. The filter membranes were fixed with cold methanol and stained with crystal violet after 24h of incubation. The cells on the upper surface of filter membranes were wiped away by using a cotton swab and the cells on the lower surface of the membranes were evaluated under a microscope with the imaging system. Each experiment was done in triplicate. |
Reaction Conditions | 0, 0.025, 0.05, 0.1, 0.3μM; 24h |
Applications | ML-210 treatment inhibited the migration of PANC-1 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/6 mice |
Preparation Method | 5-week-old female C57BL/6 mice were bred and raised in SPF laboratory at a temperature of 26℃ with free access to water and food. Mice were inoculated with 5×106 ID8-Luc-puro cells by intraperitoneal injection in 200μL PBS. On the seventh day after cell inoculation, mice were treated with 1mg/kg trigonelline, 30mg/kg ML385, 0.5mg/kg clobetasol propionate, 3mg/kg RSL3, 5mg/kg ML-210, and 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline were given as a control. ML-210 was intraperitoneally administered every other day for a total of 10 administrations. Body weight was measured every 5 days. After treatment, mice were injected with pentobarbitone (1mg/mice) and D-luciferin (3mg/mice) in succession, and luminescence signals were observed within 15min using the In-vivo Xtreme live imaging system. Illuminance intensity was normalized and analyzed by the related software. |
Dosage form | 5mg/kg, every other day for 20 days; i.p. |
Applications | ML-210 treatment inhibited the spread of ID8-Luc-puro cells in mice and modestly reduced body weight in mice. |
References: | |
| Cas No. | 1360705-96-9 | SDF | |
| Synonyms | DPI10 | ||
| Chemical Name | [4-[bis(4-chlorophenyl)methyl]-1-piperazinyl](5-methyl-4-nitro-3-isoxazolyl)-methanone | ||
| Canonical SMILES | ClC1=CC=C(C(C2=CC=C(Cl)C=C2)N3CCN(C(C4=NOC(C)=C4[N+]([O-])=O)=O)CC3)C=C1 | ||
| Formula | C22H20Cl2N4O4 | M.Wt | 475.3 |
| Solubility | 25mg/mL in DMSO (Need ultrasonic), 10mg/mL in DMF, slightly soluble in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1039 mL | 10.5197 mL | 21.0393 mL |
| 5 mM | 420.8 μL | 2.1039 mL | 4.2079 mL |
| 10 mM | 210.4 μL | 1.052 mL | 2.1039 mL |
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
