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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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ML-210 (ML210; CID49766530) is a novel, potent, selective RAS inhibitor, and also a covalent inhibitor of glutathione peroxidase 4 (GPX4) with anticancer activity. It inhibits GPX4 with an EC50 of 30 nM. ML-210 binds the GPX4 selenocysteine residue. ML-210 displayed nanomolar potency in the primary screening cell line while maintaining selectivity similar to previously identified probes. The probe is in a novel structural class in the field of RAS synthetically lethal compounds and will, therefore, be highly useful in identifying pathways that can potentially be used for selectively inhibiting cancer cells.
ln Vitro |
In a panel of 821 cancer cells (WM88, LOX-IMVI, CJM, U257, CAKI2, A498, HT1080, MC38, PANC02), ML-210 shown cell-killing ability. One prodrug that needs cells is ML-210. ML-210 has an IC50 of 71 nM, 272 nM, and 107 nM (without HRASV12) against BJeLR (HRASV12), BJeH-LT, and DRD cell lines, respectively [2].
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References |
[1]. John K. Eaton, et al. Targeting a Therapy-Resistant Cancer Cell State Using Masked Electrophiles as GPX4 Inhibitors. Biorxiv. 2018.
[2]. Weïwer M, et al. Development of small-molecule probes that selectively kill cells induced to express mutant RAS. Bioorg Med Chem Lett. 2012 Feb 15;22(4):1822-6. |
Molecular Formula |
C22H20CL2N4O4
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Molecular Weight |
475.326
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Exact Mass |
474.0862
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CAS # |
1360705-96-9
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Related CAS # |
1360705-96-9;
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SMILES |
O=C(N1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=C(Cl)C=C3)CC1)C4=NOC(C)=C4[N+]([O-])=O
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InChi Key |
VIBHJPDPEVVDTB-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H20Cl2N4O4/c1-14-20(28(30)31)19(25-32-14)22(29)27-12-10-26(11-13-27)21(15-2-6-17(23)7-3-15)16-4-8-18(24)9-5-16/h2-9,21H,10-13H2,1H3
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Chemical Name |
[4-[Bis(4-chlorophenyl)methyl]piperazin-1-yl]-(5-methyl-4-nitro-1,2-oxazol-3-yl)methanone
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Synonyms |
CID 49766530 ML-210CID-49766530 ML 210CID49766530 ML210.
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~25 mg/mL (~52.60 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.26 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1038 mL | 10.5190 mL | 21.0380 mL | |
5 mM | 0.4208 mL | 2.1038 mL | 4.2076 mL | |
10 mM | 0.2104 mL | 1.0519 mL | 2.1038 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.