Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
CKIα CDK7 0.31 nM (Kd) CDK9 5.4 nM (Kd)
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ln Vitro |
At 160 nM or less, the casein kinase inhibitor A86 is very effective in causing leukemia cells to undergo apoptosis, primarily due to its ability to stabilize p53[1]. MYC, MDM2, and the anti-apoptotic oncogene MCL1 are all eliminated by the casein kinase inhibitor A86 (0.08-2 μM; 6.5 hours). The Wnt targets AXIN2 and CCND1 (Cyclin D1) are expressed more when the casein kinase inhibitor A86 is used, although the mRNA expression of MYC and MDM2 is significantly reduced[1].
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ln Vivo |
Rapid oral absorption is shown in pharmacokinetic investigations with the Casein Kinase inhibitor A86 at 20 mg/kg, with Tmax values of 0.2-0.5 hours, Cmax values of 1115 ng/mL, T1/2 values of 4.3 hours, and area under the curve (AUC) values of 2606 (ng*hr/mL)[1].
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Cell Assay |
Cell Viability Assay[1]
Cell Types: MV4-11 cells Tested Concentrations: 0.08 μM, 0.6 μM, 2 μM Incubation Duration: 6.5 hrs (hours) Experimental Results: Abolishes the expression of MYC, MDM2, and the anti-apoptotic oncogene MCL1. |
References |
[1]. Waleed Minzel, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018 Sep 20;175(1):171-185.e25.
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Molecular Formula |
C18H25FN6
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Molecular Weight |
344.43
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CAS # |
2079069-01-3
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
FC1=CN=C(N=C1C1C=NN(C)C=1CC1CC1)NC1CCC(CC1)N
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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 : 12.5 mg/mL (36.29 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.63 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 12.5 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: ≥ 1.25 mg/mL (3.63 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 12.5 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: ≥ 1.25 mg/mL (3.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.9033 mL | 14.5167 mL | 29.0335 mL | |
5 mM | 0.5807 mL | 2.9033 mL | 5.8067 mL | |
10 mM | 0.2903 mL | 1.4517 mL | 2.9033 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.