| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
MYLS22 targets optic atrophy 1 (OPA1), a mitochondrial protein involved in mitochondrial fusion and cristae organization. By inhibiting OPA1, MYLS22 affects NF-κB activity and angiogenic gene expression, thereby inhibiting angiogenesis. This reduces tumor development and metastasis.
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| ln Vitro |
By blocking OPA1, MYLS22 inhibits vascular tumorization and associated vascular angiogenesis, hence reducing tumor development and metastasis and successfully returning vascular tumor morphology to normal [2]. Acute myeloid leukocyte (AML) cell clonal development is inhibited by MYLS22 (10-30 μM; 7-10 days) with an IC50 of 12.5 μM [1]. In AML cells, MYLS22 (10-30 μM; 7-10 days) can effectively prevent mitochondrial fusion, lowering ROS levels and blocking the cell cycle during the G0/G1 transition phase [1].
In vitro, MYLS22 (10-30 μM; 7-10 days) inhibits acute myeloid leukemia (AML) cell clonal development with an IC50 of 12.5 μM. It downregulates angiogenic factors (FGFR, FGF, EGF, and PDGF) used by tumors escaping from VEGF inhibitors. The compound reduces tumor vascularization and successfully returns vascular tumor morphology to normal. |
| ln Vivo |
MYLS22 (30 mg/kg; intraperitoneal injection; once daily for 7 days) significantly reduced the total tumor burden in mice [1]. MYLS22 (10 mg/kg; i.p.; once daily for six days) suppresses tumor growth in subcutaneous B16F10 melanoma mice by targeting OPA1 [3].
In vivo, MYLS22 (10 mg/kg/die; peritumoral injection; every 2 days for 14 days) causes tumor growth curtailment in mice. It has anti-angiogenesis and anti-cancer activity, reducing tumor growth and metastasis. |
| Enzyme Assay |
The in vitro assay for MYLS22 involves measuring its effect on cell proliferation and angiogenesis. AML cells are treated with MYLS22 (10-30 μM; 7-10 days), and clonal development is assessed. Angiogenesis is evaluated by measuring the formation of capillary-like structures in endothelial cell cultures.
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| Cell Assay |
Cellular assays for MYLS22 are performed using AML cells or endothelial cells. Cells are treated with the compound at various concentrations. Cell viability and proliferation are assessed using standard assays. Angiogenic gene expression is measured by RT-qPCR.
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| Animal Protocol |
In vivo animal studies for MYLS22 are conducted in mice. The compound is administered via peritumoral injection at 10 mg/kg every 2 days for 14 days. Tumor growth is measured to assess anti-tumor efficacy.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for MYLS22 are not available in the provided sources. The compound has a molecular weight of approximately 480.54 g/mol. It is soluble in DMSO. Specific PK parameters such as half-life, bioavailability, and clearance have not been reported.
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| Toxicity/Toxicokinetics |
Toxicity data for MYLS22 indicate that it is a non-toxic small molecule inhibitor. Specific toxicological profiles are not provided in the available sources. The compound is intended for research use only.
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| References | |
| Additional Infomation |
MYLS22 is a research compound being investigated for its anti-cancer and anti-angiogenic properties. It is a first-in-class OPA1 inhibitor that targets endothelial OPA1 to curtail tumor growth. The compound is available from commercial suppliers for research purposes only.
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| Molecular Formula |
C24H21N5O2S
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|---|---|
| Molecular Weight |
443.520843267441
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| Exact Mass |
443.141
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| CAS # |
306959-01-3
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| PubChem CID |
1142445
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| Appearance |
Off-white to yellow solid powder
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| LogP |
5.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
32
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| Complexity |
776
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C(C(NC2C(N(C3C=CC=CC=3)N(C)C=2C)=O)=O)=CC2C(C)=NN(C3C=CC=CC=3)C1=2
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| InChi Key |
WIEJADKUYLLKPX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H21N5O2S/c1-15-19-14-20(32-24(19)28(26-15)17-10-6-4-7-11-17)22(30)25-21-16(2)27(3)29(23(21)31)18-12-8-5-9-13-18/h4-14H,1-3H3,(H,25,30)
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| Chemical Name |
N-(1,5-dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-3-methyl-1-phenyl-1H-thieno[2,3-c]pyrazole-5-carboxamide
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| Synonyms |
MYLS-22 MYLS22 MYLS 22
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| HS Tariff Code |
2934.99.9001
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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 (~56.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 12.5 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: ≥ 1.25 mg/mL (2.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2547 mL | 11.2734 mL | 22.5469 mL | |
| 5 mM | 0.4509 mL | 2.2547 mL | 4.5094 mL | |
| 10 mM | 0.2255 mL | 1.1273 mL | 2.2547 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.
Products are for research use only; We do not sell to patients
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