| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
CDK9-IN-15 targets cyclin-dependent kinase 9 (CDK9). CDK9 is a key enzyme involved in regulating transcriptional elongation by phosphorylating RNA polymerase II. By inhibiting CDK9, the compound blocks the phosphorylation of the C-terminal domain of RNA Polymerase II, thereby inhibiting transcription and rapidly reducing intracellular mRNA levels, which leads to apoptosis of tumor cells.
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|---|---|
| ln Vitro |
In vitro, CDK9-IN-15 is a potent CDK9 inhibitor. It blocks the phosphorylation of RNA Polymerase II, inhibits transcription, and rapidly reduces the level of intracellular mRNA. This leads to the apoptosis of tumor cells. However, specific IC50 values for CDK9 inhibition are not detailed in the available literature.
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| ln Vivo |
In vivo, CDK9-IN-15 is expected to show antitumor efficacy in animal models by inhibiting CDK9 and inducing apoptosis in tumor cells. However, specific in vivo efficacy data and detailed animal study results are not extensively reported in the available literature. The compound is primarily used as a research tool.
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| Enzyme Assay |
In vitro enzyme assays for CDK9-IN-15 involve kinase activity assays using purified recombinant CDK9/cyclin T1 complex. The compound is incubated with the enzyme, ATP, and a specific peptide substrate (e.g., a peptide derived from the C-terminal domain of RNA Polymerase II). The phosphorylation of the substrate is measured using techniques such as radioactive (33P-ATP) or luminescence-based detection methods.
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| Cell Assay |
In vitro cellular assays for CDK9-IN-15 are performed using cancer cell lines. Cells are treated with various concentrations of the compound. The inhibition of RNA Polymerase II phosphorylation is assessed by Western blotting. Cell viability and proliferation are measured using MTT or CellTiter-Glo assays. Apoptosis is assessed by measuring caspase-3/7 activity or by Annexin V staining.
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| Animal Protocol |
In vivo animal studies with CDK9-IN-15 would typically be conducted in mouse xenograft models of cancer to evaluate its antitumor efficacy. The compound would be administered, and tumor growth inhibition would be assessed. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of CDK9-IN-15 are not extensively reported. It has a molecular weight of 293.34. It is soluble in DMSO at 125 mg/mL. Specific parameters such as oral bioavailability, half-life, and tissue distribution are not detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of CDK9-IN-15 is not extensively reported in the available literature. As a research compound, it is for research use only and not for human therapeutic use. No specific toxicity data are detailed.
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| Additional Infomation |
CDK9-IN-15 (compound 50) is a potent CDK9 inhibitor that blocks RNA Polymerase II phosphorylation, inhibits transcription, and induces apoptosis in tumor cells. It is used in cancer research to study the role of CDK9 in transcriptional regulation and tumor cell survival. The compound is available for research purposes only.
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| Molecular Formula |
C16H11N3OS
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|---|---|
| Molecular Weight |
293.343041658401
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| Exact Mass |
293.062
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| CAS # |
852678-17-2
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| PubChem CID |
4782564
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| Appearance |
Brown to black solid powder
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| LogP |
3.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
21
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| Complexity |
369
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC2=C(C=CC=C2O)C(=C1)NC3=C4C=CSC4=NC=N3
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| InChi Key |
WGOSYBWTPRPCIR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H11N3OS/c20-14-6-2-3-10-11(14)4-1-5-13(10)19-15-12-7-8-21-16(12)18-9-17-15/h1-9,20H,(H,17,18,19)
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| Chemical Name |
5-(thieno[2,3-d]pyrimidin-4-ylamino)naphthalen-1-ol
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 : ~125 mg/mL (~426.13 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.09 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4090 mL | 17.0451 mL | 34.0901 mL | |
| 5 mM | 0.6818 mL | 3.4090 mL | 6.8180 mL | |
| 10 mM | 0.3409 mL | 1.7045 mL | 3.4090 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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