| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
PIK5-12d targets PIKfyve for degradation, with a DC50 (half-maximal degradation concentration) of 1.48 nM. It is a high-affinity, selective PIKfyve degrader built from the PIKfyve inhibitor Apilimod and a VHL (von Hippel-Lindau) E3 ligase ligand.
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| ln Vitro |
In vitro, PIK5-12d is a potent PIKfyve degrader with a DC50 of 1.48 nM in VCaP prostate cancer cells after 24 hours of treatment, achieving a Dmax (maximum degradation) of 97.7%. It induces massive cytoplasmic vacuolization, blocks autophagic flux, and inhibits proliferation in multiple prostate cancer cell lines.
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| ln Vivo |
Specific in vivo activity data for PIK5-12d are not detailed in the available literature. However, its potent in vitro anti-proliferative activity against prostate cancer cells suggests potential for in vivo efficacy in animal models of prostate cancer.
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| Enzyme Assay |
Non-cellular assays for PIK5-12d are not typically performed, as it is a PROTAC degrader that functions in a cellular context. Its activity is assessed by measuring the degradation of PIKfyve protein in cells.
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| Cell Assay |
In vitro cellular assays for PIK5-12d involve treating prostate cancer cell lines (e.g., VCaP) with the compound. The degradation of PIKfyve is measured by Western blotting to determine the DC50 and Dmax. The compound's effects on cytoplasmic vacuolization, autophagic flux, and cell proliferation are also assessed.
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| Animal Protocol |
In vivo animal experiments for PIK5-12d would likely involve administering the compound to mouse models of prostate cancer. Endpoints would include tumor growth inhibition, analysis of PIKfyve degradation in tumor tissues, and assessment of biomarkers related to autophagy and cell proliferation.
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| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties for PIK5-12d are not detailed in the available literature. As a PROTAC molecule, its PK profile would be important for determining its oral bioavailability, half-life, and tissue distribution for potential therapeutic applications.
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| Toxicity/Toxicokinetics |
Toxicological data for PIK5-12d are not provided in the available sources. As a research compound, its safety profile has not been extensively characterized. It is intended for research use only and not for human consumption.
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| References | |
| Additional Infomation |
PIK5-12d is a PROTAC PIKfyve degrader with a DC50 of 1.48 nM. Its CAS number is 3036457-38-9. It is supplied for research purposes only.
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| Molecular Formula |
C52H64N10O7S
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|---|---|
| Molecular Weight |
973.19
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| Appearance |
Off-white to light yellow solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0275 mL | 5.1377 mL | 10.2755 mL | |
| 5 mM | 0.2055 mL | 1.0275 mL | 2.0551 mL | |
| 10 mM | 0.1028 mL | 0.5138 mL | 1.0275 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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