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| ln Vitro |
AH078 can effectively bind CK1δ in permeabilized cells, with an EC50 of 3.2 nM[3]. AH078 can degrade CK1δ in MV4-11 HiBiT-CK1δ cells, with a DC50 of 0.55 μM and a Dmax of 70.1% after 6 hours of incubation[3]. AH078 (3-10 μM; 9 hours) can dose-dependently slow down the cell cycle progression of MEC-1 WT cells. At a concentration of 10 μM, it can reduce the accumulation of cells at the G2/M phase junction and increase the proportion of cells in the S phase[2]. AH078 (3-10 μM; 9 hours) can dose-dependently slow down the cell cycle progression of HG-3 WT cells, reduce the accumulation of cells at the G2/M phase junction, and increase the proportion of cells in the S phase at a concentration of 10 μM[2]. AH078 (3-10 μM; 6 days) significantly inhibited microenvironment-induced proliferation of primary human chronic lymphocytic leukemia (CLL) cells in a dose-dependent manner, with the strongest inhibitory effect observed at 10 μM for 6 days [2]. AH078 (0.01-30 μM; 6 hours) effectively degraded endogenous CK1δ (DC50=200 nM) and CK1ε in HEK293 cells after 6 hours of incubation, but its degradation effect on CK1α was weak only at concentrations ≥10 μM [3]. The CK1δ degradation mediated by AH078 (0.03-1.19 μM; 6 hours) was dependent on the functional Cullin cyclic ligase, and experimental results confirmed that the degradation process was reversible after treatment with the neddylation inhibitor MLN4924 [3].
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| Cell Assay |
Cell cycle analysis [2]
Cell Types: HG-3 WT and MEC-1 WT cells Tested Concentrations: 3 μM; 10 μM Incubation Duration: 9 hours Experimental Results: Compared with cells treated with nocodazole alone, at a concentration of 10 μM, the accumulation of G2/M phase cells was significantly reduced, and the proportion of S phase cells was significantly increased. Compared with the control group treated with nocodazole alone, at a concentration of 3 μM, the proportion of S phase cells and G2/M phase cells in MEC-1 WT cells was not significantly reduced. Western Blot Analysis [3] Cell Types: HEK293 cells (endogenous CK1δ, CK1ε, CK1α) Tested Concentrations: 0.01-30 μM Incubation Duration: 6 hours Experimental Results: Significant dose-dependent degradation of endogenous CK1δ and CK1ε was induced, with almost complete degradation at concentrations of 0.3-1 μM. Degradation of CK1α was weaker, detected only at concentrations of 10 μM and above. The DC50 of CK1δ was 200 nM, while that of CK1ε was slightly weaker. Both CK1δ and CK1ε showed a hook effect (reduced degradation) at a concentration of 30 μM. |
| References |
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| Molecular Formula |
C51H60F2N10O5S
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|---|---|
| Molecular Weight |
963.15
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| CAS # |
3110370-06-1
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| Related CAS # |
AH081
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| Appearance |
White to off-white solid
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| SMILES |
O=C([C@H]1N(C([C@@H](NC(CCCCCCC(N2CCC(CN3C(C4=C5C(NC=C5)=NC=C4)=C(C6=NC=C(F)C=C6)N=C3)(F)CC2)=O)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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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 : ~100 mg/mL (~103.83 mM; with sonication)
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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 | 1.0383 mL | 5.1913 mL | 10.3826 mL | |
| 5 mM | 0.2077 mL | 1.0383 mL | 2.0765 mL | |
| 10 mM | 0.1038 mL | 0.5191 mL | 1.0383 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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