Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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Targets |
CDK8/CycC 4.4 nM (IC50) CDK19/CycC 10.4 nM (IC50) CDK9/cycT 1070 nM (IC50)
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ln Vitro |
SEL120-34A monohydrochloride is an ATP-competitive, selective CDK8 inhibitor that inhibits the kinase activities of CDK8/CycC and CDK19/CycC complexes. Its Kd for CDK8 is 3 nM, and its IC50s are 4.4 nM and 10.4 nM, respectively. Although SEL120-34A monohydrochloride has no discernible activity against CDK1, 2, 4, 6, 5, 7, it slightly inhibits CDK9 (IC50=1070 nM)[1]. SEL120-34A (1.6 nM-5 μM) is not harmful to S726 negative MOLM13 AML cells, however it suppresses the development of STAT5 S726 positive KG-1 AML cells[1]. The phosphorylation of STAT1 S727 and STAT5 S726 is inhibited by SEL120-34A monohydrochloride, which also reduces the expression of IRF9 and STAT1 mRNA and mitogen-induced IER[1].
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ln Vivo |
SEL120-34A monohydrochloride (30, 60 mg/kg, po once a day) suppresses growth of AML tumors in a dose-dependent manner in SCID mice after treatment for 17 days[1].
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References |
[1]. Rzymski T, et al. SEL120-34A is a novel CDK8 inhibitor active in AML cells with high levels of serine phosphorylation of STAT1 and STAT5 transactivation domains. Oncotarget. 2017 May 16;8(20):33779-33795.
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Molecular Formula |
C15H19BR2CLN4
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Molecular Weight |
450.60
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CAS # |
2443816-41-7
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Related CAS # |
SEL120-34A HCl;1609452-30-3;SEL120-34A;1609522-33-9
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Solubility (In Vitro) |
H2O : 50 mg/mL (110.96 mM)
DMSO : 16.67 mg/mL (37.00 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.67 mg/mL (3.71 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 16.7 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: ≥ 1.67 mg/mL (3.71 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 16.7 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: ≥ 1.67 mg/mL (3.71 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 14.29 mg/mL (31.71 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2193 mL | 11.0963 mL | 22.1926 mL | |
5 mM | 0.4439 mL | 2.2193 mL | 4.4385 mL | |
10 mM | 0.2219 mL | 1.1096 mL | 2.2193 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.