| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
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| Targets |
CDK9-IN-10 targets cyclin-dependent kinase 9 (CDK9), a member of the cyclin-dependent kinase family involved in transcriptional regulation. CDK9 is a key component of the positive transcription elongation factor b (P-TEFb) complex, which regulates transcriptional elongation by phosphorylating RNA polymerase II. Inhibition of CDK9 leads to suppression of transcription and induction of apoptosis in cancer cells. CDK9-IN-10 is also used as a ligand in PROTACs for targeted CDK9 degradation.
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| ln Vitro |
In vitro, CDK9-IN-10 demonstrates potent inhibitory activity against CDK9. It has shown strong inhibitory activity in cellular models. The compound is used to study transcriptional regulation, apoptosis, and tumor progression. As a PROTAC ligand, it enables the development of CDK9 degraders that induce proteasomal degradation of CDK9. The compound is widely applied in oncology, epigenetics, and transcription biology to probe CDK9-dependent signaling.
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| ln Vivo |
In vivo, CDK9-IN-10 has been used as a tool to study the role of CDK9 in cancer and other diseases. CDK9 inhibition has shown antitumor effects in various preclinical models. As a PROTAC ligand, CDK9-IN-10 is used to synthesize CDK9 degraders that may have improved efficacy and selectivity compared to traditional inhibitors. In vivo studies evaluate the ability of CDK9 degraders to inhibit tumor growth and induce apoptosis.
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| Enzyme Assay |
Non-cellular enzyme/receptor binding assay protocols for CDK9-IN-10 involve measuring CDK9 inhibition. CDK9 kinase activity is assessed using kinase assays with recombinant CDK9/cyclin T1 and peptide substrates. The IC50 is determined by measuring the inhibition of kinase activity at various concentrations of the compound. Selectivity assays against other CDKs and kinases are performed to confirm specificity. Binding studies can be performed using SPR or ITC.
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| Cell Assay |
Cellular assay protocols for CDK9-IN-10 involve treating cancer cell lines with the compound. Cells are incubated with various concentrations of CDK9-IN-10 for 24-72 hours. CDK9 inhibition is assessed by measuring phosphorylation of RNA polymerase II and downstream targets by western blot. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is measured by Annexin V staining or caspase activity assays. Cell cycle analysis is performed by flow cytometry.
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| Animal Protocol |
In vivo animal experiment protocols for CDK9-IN-10 or CDK9 degraders incorporating this ligand typically involve tumor xenograft models in immunodeficient mice. The compound is administered orally or intraperitoneally at various doses. Tumor volume is measured regularly to assess antitumor efficacy. Body weight is monitored for toxicity assessment. At study termination, tumors are collected for PK/PD analysis, including measurement of compound concentrations and assessment of CDK9 inhibition and downstream effects.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of CDK9-IN-10 have been characterized. As a small molecule (MW 360.36 g/mol), it is expected to have reasonable bioavailability. Storage conditions: 4°C, sealed storage, away from moisture and light; in solvent: -80°C for 6 months, -20°C for 1 month. Further PK studies would be needed to fully characterize its absorption, distribution, metabolism, and excretion profile.
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| Toxicity/Toxicokinetics |
Toxicity of CDK9-IN-10 has not been extensively reported. As a CDK9 inhibitor, it may affect normal cellular processes involving transcription. Standard toxicological evaluation would include acute and sub-chronic toxicity studies in rodents, genotoxicity testing, and cardiovascular safety assessments. The compound is for research use only and not for human therapeutic applications.
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| References | |
| Additional Infomation |
CDK9-IN-10 (CAS: 3542-63-0) has a molecular formula of C22H16O5 and a molecular weight of 360.36 g/mol. It is a potent CDK9 inhibitor and serves as the ligand for the PROTAC CDK9 degrader-2. It has shown strong inhibitory activity in cellular models and is widely applied in oncology, epigenetics, and transcription biology. Storage: 4°C, sealed storage, away from moisture and light; in solvent: -80°C for 6 months, -20°C for 1 month. This product is for research use only.
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| Molecular Formula |
C₂₂H₁₆O₅
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|---|---|
| Molecular Weight |
360.36
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| Exact Mass |
360.1
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| CAS # |
3542-63-0
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| PubChem CID |
15108688
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| Appearance |
Yellow to brown solid powder
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| LogP |
4.45
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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 |
4
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| Heavy Atom Count |
27
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| Complexity |
547
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)COC2=C(C3=C(C(=C2)O)C(=O)C=C(O3)C4=CC=CC=C4)O
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| InChi Key |
OQHAZMRRNANBMN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H16O5/c23-16-11-18(15-9-5-2-6-10-15)27-22-20(16)17(24)12-19(21(22)25)26-13-14-7-3-1-4-8-14/h1-12,24-25H,13H2
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| Chemical Name |
5,8-dihydroxy-2-phenyl-7-phenylmethoxychromen-4-one
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| Synonyms |
CDK9IN10; CDK9 IN 10
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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: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 (~277.50 mM)
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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 | 2.7750 mL | 13.8750 mL | 27.7500 mL | |
| 5 mM | 0.5550 mL | 2.7750 mL | 5.5500 mL | |
| 10 mM | 0.2775 mL | 1.3875 mL | 2.7750 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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