| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
RUVBL1/2 ATPase-IN-1 targets RUVBL1 and RUVBL2, which are highly conserved AAA ATPases involved in a variety of cellular activities, including chromatin remodeling, DNA repair, and cell cycle regulation. These proteins are highly related to the progression of cancer. The compound inhibits the ATPase activity of RUVBL1/2, thereby affecting their cellular functions.
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|---|---|
| ln Vitro |
In vitro, RUVBL1/2 ATPase-IN-1 has been shown to be a potent and selective inhibitor of RUVBL1/2 ATPase with IC₅₀ values of 6.0 μM for the RUVBL1/2 complex and 7.7 μM for RUVBL1. The compound inhibits the ATPase activity of these enzymes, which are involved in various cellular processes. It is used to study the role of RUVBL1/2 in cancer progression.
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| ln Vivo |
In vivo, RUVBL1/2 ATPase-IN-1 has been studied for its potential anticancer activity. The compound has potential for the research of cancer diseases. Detailed in vivo data regarding dosage, administration routes, and specific efficacy endpoints are limited in the available literature.
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| Enzyme Assay |
RUVBL1/2 ATPase-IN-1's enzyme inhibition activity has been characterized using purified RUVBL1/2 proteins or cell lysates. The compound inhibits ATPase activity with IC₅₀ values of 6.0 μM for the RUVBL1/2 complex and 7.7 μM for RUVBL1. Binding assays typically involve measuring the inhibition of ATP hydrolysis using standard ATPase assays.
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| Cell Assay |
In vitro cell experiments with RUVBL1/2 ATPase-IN-1 typically use cancer cell lines to study the effects of RUVBL1/2 inhibition on cell proliferation, apoptosis, and other cellular processes. Cells are treated with the compound at various concentrations, and cell viability, ATPase activity, and downstream signaling pathways are assessed. The compound's effects on cancer cell growth and survival are evaluated.
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| Animal Protocol |
In vivo animal studies with RUVBL1/2 ATPase-IN-1 have been conducted using rodent models of cancer. The compound is typically administered via oral gavage or intraperitoneal injection. Detailed protocols regarding dosage, treatment duration, and specific animal models are not extensively reported in the available literature.
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| ADME/Pharmacokinetics |
Pharmacokinetic data specific to RUVBL1/2 ATPase-IN-1 are limited in the available literature. As a small molecule inhibitor, the compound is expected to have reasonable bioavailability and tissue penetration. Further pharmacokinetic studies are needed to fully characterize its absorption, distribution, metabolism, and excretion properties.
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| Toxicity/Toxicokinetics |
Toxicological data for RUVBL1/2 ATPase-IN-1 are limited. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be handled under standard laboratory safety practices with appropriate precautions.
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| References | |
| Additional Infomation |
RUVBL1/2 ATPase-IN-1 (compound 18) is a potent and specific RUVBL1/2 ATPase inhibitor with IC₅₀ values of 6.0 μM for the RUVBL1/2 complex and 7.7 μM for RUVBL1. It has a molecular formula of C₂₈H₂₈F₃N₅O and a molecular weight of 507.55. The compound has potential for cancer research and is stored under recommended conditions.
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| Molecular Formula |
C28H28F3N5O
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|---|---|
| Molecular Weight |
507.55
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| Exact Mass |
507.224
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| CAS # |
423128-55-6
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| PubChem CID |
4103510
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| Appearance |
White to off-white solid powder
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| LogP |
5.3
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
37
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| Complexity |
780
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=C(C=C1)CC2=C(N3C(=C(C=N3)C(=O)N4CCN(CC4)C5=CC=CC(=C5)C(F)(F)F)N=C2C)C
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| InChi Key |
DWMRUZCWNNNCJM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H28F3N5O/c1-18-7-9-21(10-8-18)15-24-19(2)33-26-25(17-32-36(26)20(24)3)27(37)35-13-11-34(12-14-35)23-6-4-5-22(16-23)28(29,30)31/h4-10,16-17H,11-15H2,1-3H3
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| Chemical Name |
[5,7-dimethyl-6-[(4-methylphenyl)methyl]pyrazolo[1,5-a]pyrimidin-3-yl]-[4-[3-(trifluoromethyl)phenyl]piperazin-1-yl]methanone
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~10 mg/mL (~19.70 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.97 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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 mg/mL (1.97 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 10.0 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 | 1.9702 mL | 9.8512 mL | 19.7025 mL | |
| 5 mM | 0.3940 mL | 1.9702 mL | 3.9405 mL | |
| 10 mM | 0.1970 mL | 0.9851 mL | 1.9702 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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