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| 25mg |
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Purity: ≥98%
EHop-016 (EHOP016; EHop 016) is a novel, potent and selective small molecule inhibitor of Rac GTPase with potential antineoplastic activity. In MDA-MB-435 and MDA-MB-231 cells, it inhibits Rac GTPase with an IC50 of 1.1 μM for Rac1, and it is also as effective in inhibiting Rac3. The metastatic cancer cell MDA-MB-435, which overexpressed Rac and inhibited high endogenous Rac activity, showed decreased Rac activity in response to Ehop-016. Moreover, it controlled the migration of metastatic cancer cells and lessened the effects of the Rac downstream protein p21-activated kinase 1. The Rho GTPase Rac controls the reorganization of the actin cytoskeleton to create lamellipodia, which are extensions of the cell surface needed for cell invasion and migration during cancer metastasis. Since Rac hyperactivation and overexpression are linked to aggressive cancers, one effective way to inhibit Rac activity is to interfere with Rac's interaction with GEFs, which are Rac's direct upstream activators.
| Targets |
Rac1 (IC50 = 1.1 μM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The MDA-MB-435 and MDA-MB-231 human metastatic cancer cell lines' lysates are used to measure Rac activity. For a full day, cancer cells grown in culture medium (DMEM, 10% FBS, pH 7.5) are exposed to either a vehicle (0.1% DMSO) or different concentrations of EHop-016 (0–10 μM). With the G-LISA Rac1 activation assay kit, Rac1 activity is measured.
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| Cell Assay |
For 24 hours, mammary epithelial cells (MDA-MB-231, MDA-MB-435, or MCF-10A) are cultured in 0.1% DMSO vehicle or different concentrations of EHop-016 (0–10 μM). Following the manufacturer's instructions, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide cell survival and proliferation kit is used to measure cell viability.
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| Animal Protocol |
KITD814V-bearing mice.
2.5 μM KITD814V-bearing 32D cells with EHop-016 are administered by i.v. injection. |
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| References |
| Molecular Formula |
C25H30N6O
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| Molecular Weight |
430.55
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| Exact Mass |
430.25
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| Elemental Analysis |
C, 69.74; H, 7.02; N, 19.52; O, 3.72
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| CAS # |
1380432-32-5
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CCN1C2=C(C=C(C=C2)NC3=NC(=NC=C3)NCCCN4CCOCC4)C5=CC=CC=C51
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| InChi Key |
AFTZZRFCMOAFCR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30N6O/c1-2-31-22-7-4-3-6-20(22)21-18-19(8-9-23(21)31)28-24-10-12-27-25(29-24)26-11-5-13-30-14-16-32-17-15-30/h3-4,6-10,12,18H,2,5,11,13-17H2,1H3,(H2,26,27,28,29)
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| Chemical Name |
4-N-(9-ethylcarbazol-3-yl)-2-N-(3-morpholin-4-ylpropyl)pyrimidine-2,4-diamine
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.81 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 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: ≥ 2.5 mg/mL (5.81 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO +30% PEG 300 +5% Tween 80 +ddH2O: 5mg/mL Solubility in Formulation 5: 10 mg/mL (23.23 mM) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3226 mL | 11.6131 mL | 23.2261 mL | |
| 5 mM | 0.4645 mL | 2.3226 mL | 4.6452 mL | |
| 10 mM | 0.2323 mL | 1.1613 mL | 2.3226 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.
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 Synthesis and docking of EHop-016 into the putative GEF binding pocket of Rac1.J Biol Chem.2012 Apr 13;287(16):13228-38. |
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