| ln Vitro |
In cell-free TR-FRET assays, the IC50 value of IBA-11 binding to CRBN was 2285 nM[1]. IBA-11 effectively inhibited the viability of MV-4-11 cells with an IC50 value of 82.11 nM, while exhibiting very low activity against MM.1S and Mino cells[1]. IBA-11 (0.1–2.5 nM; 8 h) dose-dependently induced the degradation of CK1α in MV-4-11 and Mino cells, but did not affect the degradation of IKZF1/2/3 or GSPT1[1]. IBA-11 (500 nM; 2–16 h) induced rapid, near-complete degradation of CK1α in Mino cells within 2 hours[1]. IBA-11 (500 nM; 3 h)-induced CK1α degradation in Mino cells is dependent on the CRBN-mediated ubiquitin-proteasome system, as confirmed by rescue experiments in MLN4924, PS341, and MG132 [1]. IBA-11 (0.2–2 μM)-induced CK1α degradation is strictly dependent on CRBN, as this degradation process is inhibited in CRBN-knockout HEK293T cells [1]. IBA-11 exhibits good in vitro metabolic stability in rat liver microsomes with low cardiotoxicity risk, as evidenced by its minimal inhibitory effect on hERG channels (IC50 > 40 μM) [1].
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| Cell Assay |
Western Blot Analysis [1]
Cell Types: MV-4-11, Mino Tested Concentrations: 0.1, 0.5, 2.5 nM Incubation Duration: 8 hours Experimental Results: CK1α was induced in both MV-4-11 and Mino cells. IKZF1/2/3 and GSPT1 were largely unaffected at all tested concentrations. Western Blot Analysis [1] Cell Types: Mino Tested Concentrations: 500 nM Incubation Duration: 2, 4, 8, 16 hours Experimental Results: CK1α was almost completely depleted within 2 hours of treatment. Time-dependent degradation was induced. |
| References |
| Appearance |
Typically exists as solids at room temperature
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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.) |
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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